Stem Cell/Wnt - MedchemExpress.com...Stem Cell/Wnt Stem cells are required for continuous tissue maintenance within diverse organs, stem cell activity is often externally dictated

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Inhibitors, Agonists, Screening Librarieswww.MedChemExpress.com

Stem Cell/Wnt

Stem cells are required for continuous tissue maintenance within diverse organs, stem cell activity is often externallydictated by the microenvironment (the niche) so that stem cell output is precisely shaped to meet homeostatic needs orregenerative demands. Several key signaling pathways have been shown to play essential roles in this regulatory capacity.Specifically, the JAK/STAT, Hedgehog, Wnt, Notch, Smad, PI3K/phosphatase and tensin homolog, and NK-κB signalingpathways have all been shown experimentally to mediate various stem cell properties, such as self-renewal, cell fatedecisions, survival, proliferation, and differentiation.Recent studies mainly focus on cancer stem cell, induced pluripotent stem cell, neural stem cell and maintenance ofembryonic stem cell pluripotency. Cancer stem cells (CSCs) have been believed to be responsible for tumor initiation,growth, and recurrence. Numerous agents have been developed to specifically target CSCs by suppressing the expressionof pluripotency maintaining factors Nanog, Oct-4, Sox-2, and c-Myc and transcription of GLI. Induced pluripotent stemcells (iPSCs) have the capacity to differentiate into various types of cells, and a self-renewing resource, and scientists canexperiment with an unlimited number of pluripotent cells to perfect the process of targeted differentiation,transplantation, and more, for personalized medicine. Novel pathological mechanisms have been elucidated, new drugsoriginating from iPSC screens are in the pipeline and the first clinical trial using human iPSC-derived products has beeninitiated. References:[1] Clevers H, et al. Science. 2014 Oct 3;346(6205):1248012.[2] Matsui WH. Medicine (Baltimore). 2016 Sep;95(1 Suppl 1):S8-S19.[3] Koury J, et al. Stem Cells Int. 2017;2017:2925869.

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• Casein Kinase 3

• ERK 6

• Gli 12

• GSK-3 14

• Hedgehog 18

• Hippo (MST) 20

• JAK 22

• Notch 32

• Oct3/4 35

• PKA 37

• Porcupine 40

• ROCK 42

• sFRP-1 47

• Smo 49

• STAT 52

• TGF-beta/Smad 58

• Wnt 61

• YAP 66

• β-catenin 68

• γ-secretase 71

Inhibitors, Agonists, Screening Librarieswww.MedChemExpress.com

Target List in Stem Cell/Wnt

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

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Casein Kinase

Casein Kinases (CKs) are serine/threonine-selective enzymes thatfunction as regulators of signal transduction pathways in mosteukaryotic cell types.

https://www.MedChemExpress.com/Targets/Casein Kinase.html

Purity: 99.92%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

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Purity: 99.92%Clinical Data: Phase 2Size: 1 g, 5 g


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Casein Kinase Inhibitors & Modulators

Bioactivity: Casein Kinase II Inhibitor IV is a small-molecule inducer ofepidermal keratinocyte differentiation.

Bioactivity: Casein Kinase II Inhibitor IV Hydrochloride is asmall-molecule inducer of epidermal keratinocytedifferentiation.

Bioactivity: CK1-IN-1 is a inhibitor extracted fromcasein kinase 1 (CK1)patent WO2015119579A1, compound 1c, has s of 15 nM, 16 nM,IC5073 nM for CK1δ, and CK1ε, p38σ MAPK, respectively .[1]

Bioactivity: D4476 is a potent, selective and cell-permeable inhibitor ofcasein kinase 1( ) with an value of 0.3 μM .CK1 IC50 in vitro

Bioactivity: DMAT is a potent and specific inhibitor with an CK2 IC50value of 130 nM.

Bioactivity: Ellagic acid is a natural antioxidant, and acts as a potentand ATP-competitive inhibitor, with an of 40 nM andCK2 IC50a of 20 nM.Ki

Bioactivity: Emodin is a broad-spectrum anticancer agent. Emodin inhibits II (CKII) activity with of 2 μM.casein kinase IC50

Bioactivity: IC261 is a selective, ATP-competitive inhibitor, withCK1s of 1 μM, 1 μM, 16 μM for , and Ckiα1,IC50 Ckiδ Ckiε

respectively.

Bioactivity: LH846 is a selective inhibitor of , with an of 290 nM,CKIδ IC50and less potently inhibits CKIα and CKIε, with s of 2.5 μMIC50and 1.3 μM, respectively.

Bioactivity: Longdaysin is a , , and CK1α CK1δ extracellular inhibitor with s of 5.6signal-regulated kinase 2 (ERK2) IC50

µM, 8.8 µM, and 52 µM, respectively .[1] [2]


Casein Kinase II Inhibitor IV Cat. No.: HY-111378

Casein Kinase II Inhibitor IV Hydrochloride Cat. No.: HY-111378A

CK1-IN-1 Cat. No.: HY-111820

D4476 (Casein Kinase I Inhibitor) Cat. No.: HY-10324

DMAT (Casein kinase II Inhibitor; CK2 Inhibitor) Cat. No.: HY-15535

Ellagic acid Cat. No.: HY-B0183

Emodin (Frangula emodin) Cat. No.: HY-14393

IC261 Cat. No.: HY-12774

LH846 Cat. No.: HY-15704

Longdaysin Cat. No.: HY-18285

https://www.MedChemExpress.com/Targets/Casein Kinase.htmlhttps://www.MedChemExpress.com/Casein_Kinase_II_Inhibitor_IV.htmlhttps://www.MedChemExpress.com/Casein_Kinase_II_Inhibitor_IV_Hydrochloride.htmlhttps://www.MedChemExpress.com/ck1-in-1.htmlhttps://www.MedChemExpress.com/D4476.htmlhttps://www.MedChemExpress.com/DMAT.htmlhttps://www.MedChemExpress.com/Ellagic-acid.htmlhttps://www.MedChemExpress.com/Emodin.htmlhttps://www.MedChemExpress.com/IC261.htmlhttps://www.MedChemExpress.com/LH846.htmlhttps://www.MedChemExpress.com/longdaysin.html



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Bioactivity: NCC007 is a dual and inhibitorcasein kinase Iα (CKIα) δ (CKIδ)with s of 1.8 and 3.6 μM, respectively, and can be used inIC50research of modulating mammalian circadian rhythms .[1]

Bioactivity: PF-4800567 is a potent and selective inhibitor of caseinkinase 1ϵ ( ), with an of 32 nM, which is greaterCK1ϵ IC50than 20-fold selectivity over CK1δ ( , 711 nM).IC50

Bioactivity: PF-670462 is a potent and selective inhibitor of casein kinase, with s of 7.7 nM and 14 nM,( and )CK1ε CK1δ IC50

respectively.

Bioactivity: Silmitasertib (CX-4945) is an orally bioavailable, highlyselective and potent inhibitor, with values of 1 nMCK2 IC50against CK2α and CK2α'.

Bioactivity: Silmitasertib sodium salt is an orally bioavailable, highlyselective and potent inhibitor, with values of 1 nMCK2 IC50against CK2α and CK2α'.

Bioactivity: SR-3029 is a potent and ATP competitive and CK1δ CK1εinhibitor, with s of 44 nM and 260 nM, respectively, andIC50

s of 97 nM for both kinases.Ki

Bioactivity: TA-01 is a potent and inhibitor, with sCK1 p38 MAPK IC50of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK,respectively.

Bioactivity: TBB is a cell-permeable and ATP-competitive inhibitorCK2with an of 0.15 μM for rat liver CK2.IC50

Bioactivity: TTP 22 is a potent inhibitor, with an of 100 nM andCK2 IC50a of 40 nM.Ki

NCC007 Cat. No.: HY-128677

PF-4800567 Cat. No.: HY-12470

PF-670462 Cat. No.: HY-15490

Silmitasertib (CX-4945) Cat. No.: HY-50855

Silmitasertib sodium salt (CX-4945 (sodium salt)) Cat. No.: HY-50855B

SR-3029 Cat. No.: HY-100011

TA-01 Cat. No.: HY-100114

TBB (NSC 231634; Casein Kinase II Inhibitor I) Cat. No.: HY-14394

TTP 22 Cat. No.: HY-15479

https://www.MedChemExpress.com/ncc007.htmlhttps://www.MedChemExpress.com/PF-4800567.htmlhttps://www.MedChemExpress.com/PF-670462.htmlhttps://www.MedChemExpress.com/CX-4945.htmlhttps://www.MedChemExpress.com/CX-4945-sodium-salt.htmlhttps://www.MedChemExpress.com/SR-3029.htmlhttps://www.MedChemExpress.com/TA-01.htmlhttps://www.MedChemExpress.com/TBB.htmlhttps://www.MedChemExpress.com/TTP-22.html

ERKExtracellular signal regulated kinases

ERKs (Extracellular-signal-regulated kinases) are widely expressedprotein kinase intracellular signalling molecules that are involved infunctions including the regulation of meiosis, mitosis, and postmitoticfunctions in differentiated cells. Many different stimuli, includinggrowth factors, cytokines, virus infection, ligands for heterotrimeric Gprotein-coupled receptors, transforming agents, and carcinogens,activate the ERK pathway. In the MAPK/ERK pathway, Ras activatesc-Raf, followed by mitogen-activated protein kinase kinase(abbreviated as MKK, MEK, or MAP2K) and then MAPK1/2 (below).Ras is typically activated by growth hormones through receptortyrosine kinases and GRB2/SOS, but may also receive other signals.

ERKs are known to activate many transcription factors, such as ELK1, and some downstream protein kinases.Disruption of the ERK pathway is common in cancers, especially Ras, c-Raf and receptors such as HER2.


https://www.MedChemExpress.com/Targets/ERK.html



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ERK Inhibitors & Modulators

Bioactivity: AG126 is a which can prevent thetyrosine kinase inhibitoractivation of mitogen-activated protein kinase (p42MAPK

).ERK2

Bioactivity: Astragaloside IV, an active component isolated from Astragalus, suppresses the activation of andmembranaceus ERK1/2

, and downregulates matrix metalloproteases JNK (MMP)-2, in MDA-MB-231 breast cancer cells.(MMP)-9

Bioactivity: AX-15836 is a potent and selective inhibitor with anERK5 of 8 nM.IC50

Bioactivity: AZD-0364 is a potent and selective inhibitor extractedERK2from patent WO2017080979A1, compound example 18, has an IC50of 0.6 nM.

Bioactivity: BAY885 is a novel inhibitor.ERK5 Bioactivity: BIX02188 is a potent -selective inhibitor with an MEK5 IC50of 4.3 nM. BIX02188 inhibits catalytic activity, with anERK5

of 810 nM.IC50

Bioactivity: BIX02189 is a potent and selective inhibitor with anMEK5 of 1.5 nM. BIX02189 also inhibits catalyticIC50 ERK5

activity with an of 59 nM.IC50

Bioactivity: CC-90003 is an irreversible and selective inhibitor of ERK with antitumor activity.1/2

Bioactivity: Corynoxeine, isolated from the hook of , isUncaria rhynchophyllaa potent / inhibitor of key PDGF-BB-inducedERK1 ERK2vascular smooth muscle cells (VSMCs) proliferation.

Bioactivity: DEL-22379 is an Inhibitor. DEL-22379ERK dimerizationreadily binds to ERK2 with a K estimated in the lowdmicromolar range, though binding is detectable even at lownanomolar concentrations. …ERK2 dimerization

AG126 (Tyrphostin AG126) Cat. No.: HY-108330

Astragaloside IV Cat. No.: HY-N0431

AX-15836 Cat. No.: HY-101846

AZD-0364 Cat. No.: HY-111483

BAY885 Cat. No.: HY-112082

BIX02188 Cat. No.: HY-12055

BIX02189 Cat. No.: HY-12056

CC-90003 Cat. No.: HY-112570

Corynoxeine Cat. No.: HY-N0590

DEL-22379 Cat. No.: HY-18932

https://www.MedChemExpress.com/Targets/ERK.htmlhttps://www.MedChemExpress.com/AG126.htmlhttps://www.MedChemExpress.com/Astragaloside-IV.htmlhttps://www.MedChemExpress.com/AX-15836.htmlhttps://www.MedChemExpress.com/AZD-0364.htmlhttps://www.MedChemExpress.com/BAY885.htmlhttps://www.MedChemExpress.com/BIX02188.htmlhttps://www.MedChemExpress.com/BIX02189.htmlhttps://www.MedChemExpress.com/CC-90003.htmlhttps://www.MedChemExpress.com/Corynoxeine.htmlhttps://www.MedChemExpress.com/DEL-22379.html


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Purity: >98%Clinical Data: No Development ReportedSize: 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

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Purity: 99.0%Clinical Data: No Development ReportedSize: 5 mg

Bioactivity: Deltonin, a steroidal saponin, isolated from Dioscorea, with antitumor activity; Deltoninzingiberensis Wright

inhibits and activation.ERK1/2 AKT

Bioactivity: ERK-IN-1 (compound B) is a and inhibitor in theRAF ERK1/2treatment of a proliferative disease characterized byactivating mutations in the MAPK pathway. The activity isparticularly related to the treatment of KRAS-mutant NSCLC(non-small celllung cancer), BRAF-mutant NSCLC, KRAS-mutant…

Bioactivity: ERK1/2 inhibitor 1 is a potent, orally bioavailable / ERK1 2inhibitor, showing 60% inhibition at 1 nM and an of 3.0IC50nM against ERK1 and ERK2, respectively .[1]

Bioactivity: ERK2 IN-1 is a selective inhibitor with an of 7 nMERK2 IC50.[1]

Bioactivity: ERK5-IN-1 is a potent inhibitor with an of 87±7 nM.ERK5 IC50ERK5-IN-1 also inhibits [G2019S] with an of 26 nM.LRRK2 IC50

Bioactivity: FR 180204 is an ATP-competitive, selective inhibitor with of 0.31 μM and 0.14 μMERK Ki

for ERK1 and ERK2, respectively.

Bioactivity: Honokiol is a bioactive, biphenolic phytochemical thatpossesses potent antioxidative, anti-inflammatory,antiangiogenic, and anticancer activities by targeting avariety of signaling molecules. It inhibits the activation of

and enhances the phosphorylation of .Akt ERK1/ERK2

Bioactivity: KO-947 is a potent and selective inhibitor of kinasesERK1/2with potential clinical utility in MAPK pathway dysregulatedtumors.

Bioactivity: LM22B-10 is an activator of neurotrophin receptor,TrkB/TrkCand can induce , , and activation in vitroTrkB TrkC AKT ERKand in vivo.

Bioactivity: Longdaysin is a , , and CK1α CK1δ extracellular inhibitor with s of 5.6signal-regulated kinase 2 (ERK2) IC50

µM, 8.8 µM, and 52 µM, respectively .[1] [2]


Deltonin Cat. No.: HY-N2283

ERK-IN-1 Cat. No.: HY-114491

ERK1/2 inhibitor 1 Cat. No.: HY-112287

ERK2 IN-1 Cat. No.: HY-112300

ERK5-IN-1 Cat. No.: HY-14403

FR 180204 Cat. No.: HY-12275

Honokiol (NSC 293100) Cat. No.: HY-N0003

KO-947 Cat. No.: HY-112181

LM22B-10 Cat. No.: HY-104047

Longdaysin Cat. No.: HY-18285

https://www.MedChemExpress.com/Deltonin.htmlhttps://www.MedChemExpress.com/ERK-IN-1.htmlhttps://www.MedChemExpress.com/ERK1-2_inhibitor_1.htmlhttps://www.MedChemExpress.com/ERK2_IN-1.htmlhttps://www.MedChemExpress.com/ERK5-IN-1.htmlhttps://www.MedChemExpress.com/FR-180204.htmlhttps://www.MedChemExpress.com/honokiol.htmlhttps://www.MedChemExpress.com/KO-947.htmlhttps://www.MedChemExpress.com/LM22B-10.htmlhttps://www.MedChemExpress.com/longdaysin.html



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Purity: 98.0%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

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Bioactivity: Loureirin B, a flavonoid extracted from Dracaena, is an inhibitor of plasminogen activatorcochinchinensis

inhibitor-1 , with an IC of 26.10μM; Loureirin B(PAI-1) 50also inhibits , the phosphorylation of and KATP ERK JNK

Bioactivity: LY3214996 is a highly selective inhibitor of and ,ERK1 ERK2with of 5 nM for both enzymes in biochemical assays.IC50

Bioactivity: Magnolin, a major component of flos (Shin-Yi),Magnoliainhibits the Ras/ERKs/RSK2 signaling axis by targeting theactive pocket of and with s of 87 nM and 16.5ERK1 ERK2 IC50nM, respectively.

Bioactivity: Methylthiouracil is an antithyroid agent. Methylthiouracilsuppresses the production and , and the activationTNF-α IL-6of and .NF-κB ERK1/2

Bioactivity: MK-8353 (SCH900353) is a potent, selective and orallyavailable inhibitor, with s of 23.0 nM and 8.8 nM,ERK1/2 IC50respectively; MK-8353 has antitumor activity.

Bioactivity: Mogrol is a biometabolite of mogrosides, and acts viainhibition of the and pathways, or reducingERK1/2 STAT3

activation and activating signaling.CREB AMPK

Bioactivity: Omtriptolide (PG490-88) is a water soluble derivative prodrugof triptolide purified from the Chinese herb.

Bioactivity: Pachymic acid is a lanostrane-type triterpenoid from P. cocos.Pachymic acid inhibits and signaling pathways.Akt ERK

Bioactivity: Piperlongumine is a natural alkaloid isolated from Piper Linn , possesses ant-inflammatory,longum [1]

antibacterial, antiangiogenic, antioxidant, antitumor, andantidiabetic activities . Piperlongumine induces ROS, …[2]

Bioactivity: Pluripotin is a dual inhibitor of and with sERK1 RasGAP KDof 98 nM and 212 nM, respectively. Pluripotin also inhibits

, , , and with s of 0.5, 2.5, 3.3,RSK1 RSK2 RSK3 RSK4 IC50and 10.0 µM, respectively.

Loureirin B Cat. No.: HY-N1504

LY3214996 Cat. No.: HY-101494

Magnolin Cat. No.: HY-N1374

Methylthiouracil (MTU) Cat. No.: HY-B0513

MK-8353 (SCH900353) Cat. No.: HY-111407

Mogrol Cat. No.: HY-N2312

Omtriptolide Cat. No.: HY-16363

Pachymic acid (3-O-Acetyltumulosic acid) Cat. No.: HY-N0371

Piperlongumine (Piplartine) Cat. No.: HY-N2329

Pluripotin (SC1) Cat. No.: HY-10579

https://www.MedChemExpress.com/Loureirin_B.htmlhttps://www.MedChemExpress.com/LY3214996.htmlhttps://www.MedChemExpress.com/Magnolin.htmlhttps://www.MedChemExpress.com/methylthiouracil.htmlhttps://www.MedChemExpress.com/MK-8353.htmlhttps://www.MedChemExpress.com/Mogrol.htmlhttps://www.MedChemExpress.com/Omtriptolide.htmlhttps://www.MedChemExpress.com/Pachymic-acid.htmlhttps://www.MedChemExpress.com/Piperlongumine.htmlhttps://www.MedChemExpress.com/Pluripotin.html


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Purity: 97.07%Clinical Data: LaunchedSize: 10mM x 1mL in Water,

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Bioactivity: Ravoxertinib (GDC-0994) is an orally bioavailable kinaseERKinhibitor with an of 6.1 nM and 3.1 nM for andIC50 ERK1

, respectively.ERK2

Bioactivity: Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is anorally bioavailable inhibitor selective for kinaseERKactivity with of 6.1 nM and 3.1 nM for and ,IC50 ERK1 ERK2

respectively.

Bioactivity: Rutin hydrate is a flavonol glycoside, able to cross theblood-brain barrier, and acts by inhibiting and JNK ERK1/2activation and activating signalling.mTOR

Bioactivity: SCH772984 potently inhibits and activity withERK1 ERK2s of 4 and 1 nM, respectively.IC50

Bioactivity: Tauroursodeoxycholate (TUDCA; UR 906; Taurolite) is anendoplasmic reticulum (ER) stress inhibitor.Tauroursodeoxycholate significantly reduces expression ofapoptosis molecules, such as and .caspase-3 caspase-12Tauroursodeoxycholate also inhibits .ERK

Bioactivity: Tauroursodeoxycholate dihydrate (TUDCA dihydrate; UR 906dihydrate; Taurolite dihydrate) is an endoplasmic reticulum(ER) stress inhibitor. Tauroursodeoxycholate significantlyreduces expression of apoptosis molecules, such as caspase-3and . Tauroursodeoxycholate also inhibits …caspase-12 ERK [1]

Bioactivity: Tauroursodeoxycholate Sodium is an endoplasmic reticulum (ER)stress inhibitor. Tauroursodeoxycholate significantly reducesexpression of apoptosis molecules, such as andcaspase-3

. Tauroursodeoxycholate also inhibits .caspase-12 ERK

Bioactivity: TIC10 is a potent, orally active, and stable inducerTRAILwhich acts by inhibiting Akt and ERK, consequently activatingFoxo3a and significantly inducing cell surface TRAIL .

Bioactivity: trans-Zeatin is a plant cytokinin, which plays an importantrole in cell growth, differentiation, and division;trans-Zeatin also inhibits UV-induced activation.MEK/ERK

Bioactivity: Ulixertinib (BVD-523; VRT752271) is a potent, orally active,highly selective, ATP-competitive and reversible covalentinhibitor of kinases, with an of



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Bioactivity: Ulixertinib hydrochloride is a potent, orally active, highlyselective, ATP-competitive and reversible covalent inhibitorof kinases, with an of

Gli

Gli proteins are the effectors of Hedgehog (Hh) signaling and havebeen shown to be involved in cell fate determination, proliferationand patterning in many cell types and most organs during embryodevelopment. The Gli transcription factors activate/inhibittranscription by binding to Gli responsive genes and by interactingwith the transcription complex. The Gli transcription factors have DNAbinding zinc finger domains which bind to consensus sequences ontheir target genes to initiate or suppress transcription. Researchshowed that mutating the Gli zinc finger domain inhibited theproteins effect proving its role as a transcription factor. Gli proteinshave an 18-amino acid region highly similar to the α-helical herpes

simplex viral protein 16 activation domain.


https://www.MedChemExpress.com/Targets/Gli.html



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Gli Inhibitors & Modulators

Bioactivity: GANT 58 is a potent antagonist that inhibits GLI1-inducedGlitranscription with of 5 μM.IC50

Bioactivity: GANT 61 is an inhibitor of and targeting theGli1 Gli2Hedgehog/GLI pathway.

Bioactivity: HhAntag is a small molecule inhibitor of GLI1-mediatedtranscription, an essential down-stream element of theHedgehog (Hh) pathway; antitumor agent.

GANT 58 (NSC 75503) Cat. No.: HY-13282

GANT 61 (NSC 136476) Cat. No.: HY-13901

HhAntag Cat. No.: HY-15412

https://www.MedChemExpress.com/Targets/Gli.htmlhttps://www.MedChemExpress.com/GANT-58.htmlhttps://www.MedChemExpress.com/GANT-61.htmlhttps://www.MedChemExpress.com/HhAntag.html

GSK-3Glycogen synthase kinase-3;Glycogen synthase kinase 3

Glycogen synthase kinase 3 (GSK-3) is a multifunctionalserine/threonine kinase found in all eukaryotes. GSK-3 is one of thefew signaling mediators that play central roles in a diverse range ofsignaling pathways, including those activated by Wnts, hedgehog,growth factors, cytokines, and G protein-coupled ligands. GSK-3targets transcription factors, regulates the activity of metabolic andsignaling enzymes, and controls the half-life of proteins byearmarking them for degradation. GSK-3 exists as two isoforms,GSK-3a (51 kDa) and GSK3b (47 kDa), which are encoded by distinctgenes. These isoforms often have overlapping functions, but they donot always compensate for each other.


https://www.MedChemExpress.com/Targets/GSK-3.html



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GSK-3 Inhibitors & Modulators

Bioactivity: 5-Iodo-indirubin-3'-monoxime is a potent , GSK-3β CDK5/P25and inhibitor, competing with ATP for binding toCDK1/cyclin Bthe catalytic site of the kinase, with s of 9, 20 and 25IC50nM, respectively .[1]

Bioactivity: AR-A014418 is a potent, selective and ATP-competitive GSK3βinhibitor with an of 104 nMIC50

Bioactivity: AZD1080 is a potent and selective inhibitor. AZD1080GSK3inhibits recombinant human and with ( )GSK3α GSK3β pKi IC50of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.

Bioactivity: AZD2858 is a potent, orally active inhibitor, withGSK-3s of 0.9 and 5 nM for and , respectively,IC50 GSK-3α GSK-3β

used in the research of fracture healing.

Bioactivity: Bikinin is a non-steroidal, ATP-competitive inhibitor of plant and activates BR (brassinosteroids)GSK-3/Shaggy-like kinases

signaling.

Bioactivity: BIO-acetoxime (BIA) is a potent and selective GSK-3inhibitor, with s of both 10 nM for GSK-3α/β.IC50BIO-acetoxime has anticonvulsant and anti-infection activity.

Bioactivity: CHIR-98014 is a potent, cell-permeable inhibitor withGSK-3s of 0.65 and 0.58 nM for and ,IC50 GSK-3α GSK-3β

respectively; it shows less potent activities against cdc2 anderk2.

Bioactivity: CHIR-99021 is a inhibitor with an of 10 and 6.7GSK-3α/β IC50nMshowing 500-fold selectivity over its closest homologs CDC2and ERK2, as well as other protein kinases.

Bioactivity: CHIR-99021 monohydrochloride is a inhibitor withGSK-3α/β of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3IC50

versus its closest homologs CDC2 and ERK2, as well as otherprotein kinases.

Bioactivity: CHIR-99021 trihydrochloride is a inhibitor with GSK-3α/β IC50of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versusits closest homologs CDC2 and ERK2, as well as other proteinkinases.

5-Iodo-indirubin-3'-monoxime Cat. No.: HY-111930

AR-A014418 (AR 0133418; GSK 3β inhibitor VIII; AR 014418) Cat. No.: HY-10512

AZD1080 Cat. No.: HY-13862

AZD2858 Cat. No.: HY-15761

Bikinin (Abrasin) Cat. No.: HY-12524

BIO-acetoxime (BIA) Cat. No.: HY-15356

CHIR-98014 Cat. No.: HY-13076

CHIR-99021 (CT99021) Cat. No.: HY-10182

CHIR-99021 monohydrochloride (CT99021 monohydrochloride) Cat. No.: HY-10182A

CHIR-99021 trihydrochloride (CT99021 trihydrochloride) Cat. No.: HY-10182B

https://www.MedChemExpress.com/Targets/GSK-3.htmlhttps://www.MedChemExpress.com/5-iodo-indirubin-3-monoxime.htmlhttps://www.MedChemExpress.com/AR-A014418.htmlhttps://www.MedChemExpress.com/AZD1080.htmlhttps://www.MedChemExpress.com/AZD2858.htmlhttps://www.MedChemExpress.com/Bikinin.htmlhttps://www.MedChemExpress.com/BIO-acetoxime.htmlhttps://www.MedChemExpress.com/CHIR-98014.htmlhttps://www.MedChemExpress.com/CHIR-99021.htmlhttps://www.MedChemExpress.com/CHIR-99021-monohydrochloride.htmlhttps://www.MedChemExpress.com/CHIR-99021-trihydrochloride.html




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1 g, 5 g


1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Bioactivity: CP21R7 is potent inhibitor, with an of 1.8 nM;GSK-3β IC50CP21R7 also shows inhibitory activitiy against , with anPKCα

of 1900 nM.IC50

Bioactivity: Cromolyn sodium is an antiallergic drug. Cromolyn sodium is a inhibitor with an of 2.0 µM.GSK-3β IC50

Bioactivity: EHT 5372 is a strong inhibitor of family kinases, withDYRK’s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively.IC s50

Bioactivity: GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is apotent, selective, reversible and ATP-competitive inhibitor of

and complex with s of 5 nM/320GSK-3α/β CDK1-cyclinB IC50nM/80nM for (GSK-3α/β)/CDK1/CDK5, respectively.

Bioactivity: GSK-3 inhibitor 1 is an inhibitor of .GSK-3 Bioactivity: GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase inhibitor and demonstrates high antidiabetic3β (GSK-3β)

efficacy, with an of 4.9 nM .IC50[1]

Bioactivity: IM-12 is an inhibitor of , with an of 53 nM, andGSK-3β IC50also enhances Wnt signalling.

Bioactivity: Indirubin-3'-monoxime is a potent inhibitor, andGSK-3βweakly inhibits , with s of 22 nM and 7.8-105-Lipoxygenase IC50µM, respectively; Indirubin-3'-monoxime also shows inhibitoryactivities against CDK5/p25 and CDK1/cyclin B, with s…IC50

Bioactivity: Indirubin-3'-monoxime-5-sulphonic acid is a potent andselective inhibitor of , , and with s ofCDK1 CDK5 GSK-3β IC505 nM, 7 nM, and 80 nM, respectively .[1]

Bioactivity: Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK)inhibitor, with values of 55 nM, 35 nM, 150 nM, 300 nMIC50and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E,CDK4/cyclin D1, and CDK5/p35, respectively [1]


CP21R7 (CP21) Cat. No.: HY-100207

Cromolyn sodium (Disodium Cromoglycate; FPL-670) Cat. No.: HY-B0320A

EHT 5372 Cat. No.: HY-111380

GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO; MLS 2052) Cat. No.: HY-10580

GSK-3 inhibitor 1 Cat. No.: HY-13973A

GSK-3β inhibitor 1 Cat. No.: HY-126144

IM-12 Cat. No.: HY-12292

Indirubin-3'-monoxime (Indirubin-3'-oxime) Cat. No.: HY-19807

Indirubin-3'-monoxime-5-sulphonic acid Cat. No.: HY-111931

Indirubin-5-sulfonate Cat. No.: HY-111932

https://www.MedChemExpress.com/CP21R7.htmlhttps://www.MedChemExpress.com/Cromolyn-sodium.htmlhttps://www.MedChemExpress.com/EHT_5372.htmlhttps://www.MedChemExpress.com/BIO.htmlhttps://www.MedChemExpress.com/gsk-3-inhibitor-1.htmlhttps://www.MedChemExpress.com/gsk-3-beta-inhibitor-1.htmlhttps://www.MedChemExpress.com/IM-12.htmlhttps://www.MedChemExpress.com/Indirubin-3_acute_-monoxime.htmlhttps://www.MedChemExpress.com/indirubin-3-monoxime-5-sulphonic-acid.htmlhttps://www.MedChemExpress.com/indirubin-5-sulfonate.html



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10 mg, 50 mg

Purity: 96.90%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: Phase 1Size: 5 mg, 10 mg, 50 mg, 100 mg


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5 mg, 10 mg, 50 mg

Bioactivity: Kenpaullone is a potent inhibitor of andCDK1/cyclin B, with s of 0.4 μM and 23 nM, and also inhibitsGSK-3β IC50

CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with s of 0.68IC50μM, 7.5 μM, 0.85 μM, respectively.

Bioactivity: LY2090314 is a potent inhibitor of glycogen synthase kinase-3 with values of 1.5 nM and 0.9 nM for GSK-3α and(GSK-3) IC50

GSK-3β, respectively.

Bioactivity: RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of , , ,cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

, , and with s of 1,cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TA…



Bioactivity: SB 216763 is potent, selective and ATP-competitive GSK-3inhibitor with s of 34.3 nM for both GSK-3α and GSK-3β.IC50

Bioactivity: SB 415286 is a potent and selective cell permeable inhibitorof , with an of 77.5 nM, and a of 30.75 nM; SBGSK-3α IC50 Ki415286 is equally effective at inhibiting human andGSK-3α

.GSK-3β

Bioactivity: TDZD-8 is an inhibitor of , with an of 2 μM;GSK-3β IC50TDZD-8 shows less potent activities against Cdk-1/cyclinB,CK-II, PKA, and PKC, with all IC s of >100 μM.50

Bioactivity: Tideglusib (NP031112) is an irreversible inhibitor withGSK-3s of 5 nM and 60 nM for (1 h preincubation)IC50 GSK-3β

WT

and (1 h preincubation), respectively.GSK-3βC199A

Bioactivity: TWS119 is a specific inhibitor of , with an of 30GSK-3β IC50nM, and activates the wnt/β-catenin pathway.

Kenpaullone (9-Bromopaullone; NSC-664704) Cat. No.: HY-12302

LY2090314 Cat. No.: HY-16294

RGB-286638 Cat. No.: HY-15504

RGB-286638 free base Cat. No.: HY-15504A

SB 216763 Cat. No.: HY-12012

SB 415286 Cat. No.: HY-15438

TDZD-8 (GSK-3β Inhibitor I; NP 01139) Cat. No.: HY-11012

Tideglusib (NP031112) Cat. No.: HY-14872

TWS119 Cat. No.: HY-10590

https://www.MedChemExpress.com/Kenpaullone.htmlhttps://www.MedChemExpress.com/LY2090314.htmlhttps://www.MedChemExpress.com/RGB-286638.htmlhttps://www.MedChemExpress.com/RGB-286638-free-base.htmlhttps://www.MedChemExpress.com/SB-216763.htmlhttps://www.MedChemExpress.com/sb-415286.htmlhttps://www.MedChemExpress.com/TDZD-8.htmlhttps://www.MedChemExpress.com/Tideglusib.htmlhttps://www.MedChemExpress.com/TWS119.html

Hedgehog

Hedgehog (Hh) is composed of N-terminal and C-terminal domainsthat dissociate in a self-catalyzed proteolytic cleavage reaction. TheN-terminal product HhNp, modified by cholesterol duringself-cleavage, harbors all known Hh signaling activities. Whensynthesized in the absence of the C-terminal domain (and hencelacking cholesterol modification), the N-terminal domain is aberrantlytargeted and released selectively into the retina.Hedgehog signaling pathway is linked to tumorigenesis and isaberrantly activated in a variety of cancers. Hh ligands bind to andsuppress the transmembrane receptor Patched (PTCH), whichsuppresses Smoothened (SMO), a seven-transmembrane-helix protein

that positively regulates the Hh pathway.Sonic hedgehog (Shh) is a morphogen essential to the developing nervous system that continues to play an importantrole in adult life by contributing to cell proliferation and differentiation, maintaining blood-brain barrier integrity, andbeing cytoprotective against oxidative and excitotoxic stress, all features of importance in amyotrophic lateral sclerosis(ALS).Indian hedgehog (Ihh), a signaling molecule that plays a pivotal role in the regulation of chondrocyte proliferation,maturation, and ossification both in long-bone development and digit joint formation, has also been found to beessential for temporomandibular joint (TMJ) development.Desert hedgehog (Dhh), one of the Hedgehog family members, is expressed by Schwann cells of peripheral nerves.


https://www.MedChemExpress.com/Targets/Hedgehog.html



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5 mg, 10 mg


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5 mg, 10 mg, 50 mg, 100 mg

Purity: 99.03%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg



5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Hedgehog Inhibitors & Modulators

Bioactivity: Ciliobrevin A is a ( ) signaling pathwayhedgehog Hhinhibitor with median inhibitory concentration ( ) lessIC50than 10 μM.

Bioactivity: Cyclopamine is a ( ) pathway antagonist with anHedgehog Hh of 46 nM in the Hh cell assay.IC50

Bioactivity: Jervine(11-Ketocyclopamine) is a naturally occuring steroidalalkaloid that causes cyclopia by blocking sonic hedgehog(Shh)signaling; Jervine is an inhibitor of Smo.

Bioactivity: JK184 is a potent pathway inhibitor with Hedgehog (Hh) IC50of 30 nM in mammalian cells.

Bioactivity: RU-SKI 43 is a small molecule inhibitor of Hhat(Hedgehogacyltransferase), the enzyme responsible for the attachment ofpalmitate onto Shh. IC50 value: Target: Hhat inhibitor RU-SKI43 reduced pancreatic cancer cell proliferation and Gli-1activation through Smoothened-independent non-canonical…

Bioactivity: RU-SKI 43 hydrochloride is a small molecule inhibitor ofHhat(Hedgehog acyltransferase), the enzyme responsible for theattachment of palmitate onto Shh. IC50 value: Target: Hhatinhibitor RU-SKI 43 reduced pancreatic cancer cellproliferation and Gli-1 activation through…

Bioactivity: SANT-1 is a potent antagonist, inhibits Smo Hedgehogsignaling, with s of 20 nM and 30 nM in Shh-LIGHT2 andIC50SmoA1-LIGHT2 assay, respectively .[1]

Bioactivity: Vismodegib (GDC-0449) is an orally active pathwayhedgehoginhibitor with an of 3 nM. It also inhibits P-gp, ABCG2IC50with IC values of 3.0 μM and 1.4 μM, respectively.50

Ciliobrevin A (HPI-4) Cat. No.: HY-100790

Cyclopamine (11-Deoxojervine) Cat. No.: HY-17024

Jervine (11-Ketocyclopamine) Cat. No.: HY-N0836

JK184 Cat. No.: HY-13307

RU-SKI 43 Cat. No.: HY-18366

RU-SKI 43 hydrochloride Cat. No.: HY-18366A

SANT-1 Cat. No.: HY-100224

Vismodegib (GDC-0449) Cat. No.: HY-10440

https://www.MedChemExpress.com/Targets/Hedgehog.htmlhttps://www.MedChemExpress.com/Ciliobrevin-A.htmlhttps://www.MedChemExpress.com/Cyclopamine.htmlhttps://www.MedChemExpress.com/Jervine.htmlhttps://www.MedChemExpress.com/JK184.htmlhttps://www.MedChemExpress.com/ru-ski-43.htmlhttps://www.MedChemExpress.com/RU-SKI-43-hydrochloride.htmlhttps://www.MedChemExpress.com/SANT-1.htmlhttps://www.MedChemExpress.com/Vismodegib.html

Hippo (MST)

Hippo signaling pathway, also known as the Salvador/Warts/Hippo(SWH) pathway, controls organ size in animals through the regulationof cell proliferationand apoptosis. The Hippo pathway consists of acore kinase cascade in which Hpo phosphorylates the protein kinaseWarts (Wts) Hpo (MST1/2 in mammals) is a member of the Ste-20family of protein kinases. This highly conserved group ofserine/threonine kinases regulates several cellular processes,including cell proliferation, apoptosis, and various stress responses.


https://www.MedChemExpress.com/Targets/Hippo (MST).html



2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg

Hippo (MST) Inhibitors & Modulators

Bioactivity: EMT inhibitor-1 is an inhibitor of of , , and Hippo TGF-β Wntsignaling pathways with antitumor activities.

Bioactivity: XMU-MP-1 is a reversible and selective inhibitorMST1/2with s of 71.1 and 38.1 nM, respectively.IC50

EMT inhibitor-1 Cat. No.: HY-101275

XMU-MP-1 Cat. No.: HY-100526

https://www.MedChemExpress.com/Targets/Hippo (MST).htmlhttps://www.MedChemExpress.com/EMT_inhibitor-1.htmlhttps://www.MedChemExpress.com/XMU-MP-1.html

JAKJanus kinase

Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosinekinases that transduce cytokine-mediated signals via the JAK-STATpathway. Since members of the type I and type II cytokine receptorfamilies possess no catalytic kinase activity, they rely on the JAKfamily of tyrosine kinases to phosphorylate and activate downstreamproteins involved in their signal transduction pathways. The receptorsexist as paired polypeptides, thus exhibiting two intracellularsignal-transducing domains. JAKs associate with a proline-rich regionin each intracellular domain, which is adjacent to the cell membraneand called a box1/box2 region. After the receptor associates with itsrespective cytokine/ligand, it goes through a conformational change,

bringing the two JAKs close enough to phosphorylate each other. The JAK autophosphorylation induces aconformational change within itself, enabling it to transduce the intracellular signal by further phosphorylating andactivating transcription factors called STATs. The activated STATs dissociate from the receptor and form dimers beforetranslocating to the cell nucleus, where they regulate transcription of selected genes.


https://www.MedChemExpress.com/Targets/JAK.html



5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


1 mg, 2 mg, 5 mg, 10 mg, 50 mg



5 mg, 10 mg, 50 mg


2 mg, 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg


5 mg



JAK Inhibitors & Modulators

Bioactivity: (3R,4S)-Tofacitinib is an enantiomer of Tofacitinib.Tofacitinib inhibits with of 1 nM.JAK3 IC50

Bioactivity: (3S,4R)-Tofacitinib is an enantiomer of Tofacitinib.Tofacitinib inhibits with of 1 nM.JAK3 IC50

Bioactivity: (3S,4S)-Tofacitinib is the S-enantiomer of Tofacitinib.Tofacitinib inhibits with of 1 nM.JAK3 IC50

Bioactivity: Abrocitinib (PF-04965842) is a potent, orally active andselective inhibitor, with s of 29 and 803 nM forJAK1 IC50JAK1 and JAK2, respectively. Abrocitinib (PF-04965842)exhibits less active effect on TYK2 ( , 1.253 μM), …IC50

Bioactivity: AT9283 is a multitargeted kinase inhibitor which potentlyinhibits , ( =1.2 nM, 1.1 nM).aurora kinase A/B JAK2/3 IC50

Bioactivity: Atractylenolide I is a sesquiterpene derived from the rhizomeof Atractylodes macrocephala, possesses diverse bioactivities,such as neuroprotective, anti-allergic, anti-inflammatory andanticancer properties. Atractylenolide I reduces proteinlevels of phosphorylated and in A375 cells, and…JAK2 STAT3

Bioactivity: AZ-3 is a potent and selective inhibitor with an ofJAK1 IC5034 nM.

Bioactivity: AZ960 is a potent and specific inhibitor of the kinaseJAK2with a of 0.45 nM.Ki

Bioactivity: AZD-1480 is an ATP-competitive inhibitor of and JAK1 JAK2with s of 1.3 and


5 mg, 10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg


2 mg, 5 mg, 10 mg, 25 mg, 50 mg


1 mg, 5 mg, 10 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg, 100 mg


2 mg, 5 mg, 10 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: Baricitinib phosphate is a selective orally bioavailable/ inhibitor with of 5.9 nM and 5.7 nM,JAK1 JAK2 IC50

respectively.

Bioactivity: BMS-066 is an pseudokinase inhibitor, with of 9IKKβ/Tyk2 IC s50nM and 72 nM, respectively.

Bioactivity: BMS-911543 is a selective inhibitor, with s of 1.1JAK2 IC50nM, less selective at JAK1, JAK3 and TYK2 ( , 75, 360, 66IC50nM, respectively).

Bioactivity: CEP-33779 is a novel, selective, and orally bioavailableinhibitor of with an of 1.8±0.6 nM.JAK2 IC50

Bioactivity: Cerdulatinib (PRT062070) is a dual and inhibitorJAK SYKwith s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK,IC50respectively.

Bioactivity: CHZ868 is a type II inhibitor with an of 0.17 μM inJAK2 IC50EPOR JAK2 WT Ba/F3 cell.

Bioactivity: Cucurbitacin I is a natural selective inhibitor of, with potent anti-cancer activity.JAK2/STAT3

Bioactivity: Decernotinib is a potent, orally active inhibitor, withJAK3s of 2.5, 11, 13 and 11 nM for , JAK1, JAK2, and TYK2,Ki JAK3

respectively.

Bioactivity: Delgocitinib is a novel and specific inhibitor with sJAK IC50of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2,respectively.

Bioactivity: Fedratinib (TG-101348) is a selective inhibitor of withJAK2an of 3 nM, showing 35- and 334-fold selectivity overIC50JAK1 and JAK3, respectively.


Baricitinib phosphate (INCB028050 (phosphate); LY3009104 (phosphate)) Cat. No.: HY-15315A

BMS-066 Cat. No.: HY-18710

BMS-911543 Cat. No.: HY-15270

CEP-33779 Cat. No.: HY-15343

Cerdulatinib (PRT062070; PRT2070) Cat. No.: HY-15999

CHZ868 Cat. No.: HY-18960

Cucurbitacin I (Elatericin B; JSI-124; NSC-521777) Cat. No.: HY-N1405

Decernotinib (VX-509; VRT-831509) Cat. No.: HY-12469

Delgocitinib (JTE-052) Cat. No.: HY-109053

Fedratinib (TG-101348; SAR 302503) Cat. No.: HY-10409

https://www.MedChemExpress.com/Baricitinib-phosphate.htmlhttps://www.MedChemExpress.com/BMS-066.htmlhttps://www.MedChemExpress.com/BMS-911543.htmlhttps://www.MedChemExpress.com/CEP-33779.htmlhttps://www.MedChemExpress.com/Cerdulatinib.htmlhttps://www.MedChemExpress.com/CHZ868.htmlhttps://www.MedChemExpress.com/Cucurbitacin-I.htmlhttps://www.MedChemExpress.com/Decernotinib.htmlhttps://www.MedChemExpress.com/Delgocitinib.htmlhttps://www.MedChemExpress.com/TG-101348.html



1 mg, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


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5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


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2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Bioactivity: Filgotinib (GLPG0634) is a selective inhibitor with JAK1 IC50of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, andTYK2, respectively.

Bioactivity: FLLL32, a synthetic analog of curcumina, is a dualJAK2/STAT3inhibitor with anti-tumor activity .[1] [2]

Bioactivity: FM381 is a potent covalent reversible inhibitor of JAK3targeting the unique Cys909 at the gatekeeper position +7 inJAK3. FM-381 has an of 127 pM for JAK3, with 410, 2700IC50and 3600-fold selectivity over JAK1, JAK2 and TYK2,respectively.

Bioactivity: Gandotinib (LY2784544) is a potent inhibitor with JAK2 IC50of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4,FGFR2, TYK2, and TRKB with IC of 4, 25, 32, 44, and 95 nM.50

Bioactivity: GLPG0634 (analog) (compound176)is a pan JAK inhibitor withIC50s of 50-200 nM for JAK1/JAK2/JAK3; more information can befound in the reference patents.

Bioactivity: Gusacitinib (ASN-002) is a potent dual inhibitor of spleentyrosine kinase ( ) and janus kinase ( ) with SYK JAK IC50values of 5-46 nM.

Bioactivity: Ilginatinib (NS-018) is a highly active and orallybioavailable inhibitor, with an of 0.72 nM, 46-,JAK2 IC5054-, and 31-fold selectivity for JAK2 over JAK1 ( , 33IC50nM), JAK3 ( , 39 nM), and Tyk2 ( , 22 nM).IC50 IC50

Bioactivity: Ilginatinib hydrochloride (NS-018 hydrochloride) is a highlyactive and orally bioavailable inhibitor, with an JAK2 IC50of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 overJAK1 ( , 33 nM), JAK3 ( , 39 nM), and Tyk2 ( ,…IC50 IC50 IC50

Bioactivity: Ilginatinib (maleate) (NS-018 (maleate)) is a highly activeand orally bioavailable inhibitor, with an of 0.72JAK2 IC50nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (

, 33 nM), JAK3 ( , 39 nM), and Tyk2 ( , 22 nM).IC50 IC50 IC50

Bioactivity: Itacitinib is a potent and selective inhibitor of , withJAK1>20-fold selectivity for JAK1 over JAK2 and >100-foldover JAK3 and TYK2; Itacitinib is used in the research ofmyelofibrosis.

Filgotinib (GLPG0634) Cat. No.: HY-18300

FLLL32 Cat. No.: HY-100544

FM381 Cat. No.: HY-102046

Gandotinib (LY2784544) Cat. No.: HY-13034

GLPG0634 analog Cat. No.: HY-13961

Gusacitinib (ASN-002) Cat. No.: HY-103018

Ilginatinib (NS-018) Cat. No.: HY-19631A

Ilginatinib hydrochloride (NS-018 hydrochloride) Cat. No.: HY-19631B

Ilginatinib maleate (NS-018 (maleate)) Cat. No.: HY-19631

Itacitinib (INCB039110) Cat. No.: HY-16997

https://www.MedChemExpress.com/GLPG0634.htmlhttps://www.MedChemExpress.com/flll32.htmlhttps://www.MedChemExpress.com/FM381.htmlhttps://www.MedChemExpress.com/LY2784544.htmlhttps://www.MedChemExpress.com/GLPG0634-analog.htmlhttps://www.MedChemExpress.com/ASN-002.htmlhttps://www.MedChemExpress.com/NS-018.htmlhttps://www.MedChemExpress.com/NS-018-hydrochloride.htmlhttps://www.MedChemExpress.com/NS-018-maleate.htmlhttps://www.MedChemExpress.com/Itacitinib.html


5 mg, 10 mg, 50 mg, 100 mg










1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: Itacitinib adipate is a selective inhibitor which hasJAK1been tested for efficacy and safety in a phase II trial inmyelofibrosis.

Bioactivity: JAK-IN-1 is a inhibitor with s of 0.26, 0.8 andJAK1/2/3 IC503.2 nM, respectively. JAK-IN-1 shows improved selectivity forJAK3 over JAK1.

Bioactivity: JAK-IN-3 (compound 22) is a potent inhibitor, with JAK IC50values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 andJAK2, respectively .[1]

Bioactivity: JAK-IN-4 is a prodrug of a inhibitor, effective in murineJAKcollagen induced arthritis model .[1]

Bioactivity: JAK inhibitor 1 is an inhibitor of extracted from patentJAKUS20170121327A1, compound example 283.

Bioactivity: JAK/HDAC-IN-1 is a potent dual inhibitor, exhibitsJAK2/HDACantiproliferative and proapoptotic activities in severalhematological cell lines. JAK/HDAC-IN-1 shows s of 4 and 2IC50nM for JAK2 and HDAC, respectively .[1]

Bioactivity: JAK1-IN-3 is a selective inhibitor, with an of 73JAK1 IC50nM, weakly inhibits JAK2, and shows little inhibition on JAK3( , >14.7, >30 μM, respectively).IC50

Bioactivity: JAK1-IN-4 is a potent and selective inhibitor, withJAK1s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, andIC50

JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylationin NCI-H 1975 cells (IC , 227 nM) .50

[1]

Bioactivity: JAK3 covalent inhibitor-1 is a potent and selective janus covalent inhibitor with an of 11 nM andkinase 3 (JAK3) IC50

shows 246-fold selectivity vs other JAKs .[1]

Bioactivity: JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, alsoinhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM). IC50value: 4.8 nM [1] Target: JAK3 in vitro: JAK3-IN-1 provides aset of useful tools to pharmacologically interrogateJAK3-dependent biology. JAK3-IN-1 completely inhibits IL-4…


Itacitinib adipate Cat. No.: HY-16997A

JAK-IN-1 Cat. No.: HY-13827




JAK/HDAC-IN-1 Cat. No.: HY-126141

JAK1-IN-3 Cat. No.: HY-107361


JAK3 covalent inhibitor-1 Cat. No.: HY-119935


https://www.MedChemExpress.com/Itacitinib_adipate.htmlhttps://www.MedChemExpress.com/JAK-IN-1.htmlhttps://www.MedChemExpress.com/JAK-IN-3.htmlhttps://www.MedChemExpress.com/JAK-IN-4.htmlhttps://www.MedChemExpress.com/JAK_inhibitor_1.htmlhttps://www.MedChemExpress.com/jak-hdac-in-1.htmlhttps://www.MedChemExpress.com/AZD-4205.htmlhttps://www.MedChemExpress.com/JAK1-IN-4.htmlhttps://www.MedChemExpress.com/jak3-covalent-inhibitor-1.htmlhttps://www.MedChemExpress.com/JAK3-IN-1.html




5 mg


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5 mg, 10 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg


1 mg, 5 mg


5 mg, 10 mg, 50 mg



Bioactivity: JAK3-IN-6 is a potent, selective irreversible Janus AssociatedKinase 3 (JAK3) inhibitor, with an of 0.15 nM.IC50

Bioactivity: JAK3-IN-7 is a potent and selective inhibitor extractedJAK3from patent WO2011013785A1, has an of


5 mg, 10 mg, 50 mg, 100 mg



2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Purity: 98.88%Clinical Data:Size: 5 mg


5 mg, 10 mg, 50 mg, 100 mg



5 mg, 10 mg, 25 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: NVP-BSK805 dihydrochloride is an ATP-competitive JAK2inhibitor, with s of 0.48 nM, 31.63 nM, 18.68 nM, andIC5010.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1,and TYK2 JH1, respectively.

Bioactivity: Oclacitinib maleate is a novel inhibitor. Oclacitinib isJAKmost potent at inhibiting ( =10 nM).JAK1 IC50

Bioactivity: Pacritinib is a potent inhibitor of both wild-type (ICJAK2=23 nM) and mutant (IC =19 nM). Pacritinib50 JAK2

V617F50

also inhibits (IC =22 nM) and its mutant FLT3 50 FLT3D835Y

(IC =6 nM).50

Bioactivity: PF-06651600 is a potent -selective inhibitor with an JAK3 IC50of 33.1 nM.

Bioactivity: PF-06700841 is a dual and inhibitor with s ofJAK1 TYK2 IC5017 and 23 nM, respectively. Anti-inflammatory activity .[1]

Bioactivity: PF-06700841 P-Tosylate is a dual and inhibitorJAK1 TYK2with s of 17 and 23 nM, respectively. Anti-inflammatoryIC50activity .[1]

Bioactivity: Protosappanin A (PTA), an immunosuppressive ingredient andmajor biphenyl compound isolated from ,Caesalpinia sappan Lsuppresses -dependent inflammation pathway throughJAK2/STAT3down-regulating the phosphorylation of JAK2 and STAT3 .[1]

Bioactivity: Pyridone 6 is a inhibitor, which potently inhibitspan-JAKthe JAK kinase family, with s of 1 nM for and ,IC50 JAK2 TYK2

5 nM for , and 15 nM for , while displayingJAK3 JAK1significantly weaker affinities (130 nM to >10 mM) forother protein tyrosine kinases.






NVP-BSK805 dihydrochloride (BSK805 dihydrochloride) Cat. No.: HY-14722A

Oclacitinib maleate (PF-03394197 maleate) Cat. No.: HY-13577A

Pacritinib (SB1518) Cat. No.: HY-16379

PF-06651600 Cat. No.: HY-100754

PF-06700841 Cat. No.: HY-112708

PF-06700841 P-Tosylate Cat. No.: HY-112708A

Protosappanin A (PTA) Cat. No.: HY-113573

Pyridone 6 (CMP 6; JAK Inhibitor) Cat. No.: HY-14435

RGB-286638 Cat. No.: HY-15504

RGB-286638 free base Cat. No.: HY-15504A

https://www.MedChemExpress.com/nvp-bsk805-dihydrochloride.htmlhttps://www.MedChemExpress.com/Oclacitinib_maleate.htmlhttps://www.MedChemExpress.com/pacritinib.htmlhttps://www.MedChemExpress.com/PF-06651600.htmlhttps://www.MedChemExpress.com/PF-06700841.htmlhttps://www.MedChemExpress.com/PF-06700841_P-Tosylate.htmlhttps://www.MedChemExpress.com/Protosappanin_A.htmlhttps://www.MedChemExpress.com/Pyridone-6.htmlhttps://www.MedChemExpress.com/RGB-286638.htmlhttps://www.MedChemExpress.com/RGB-286638-free-base.html



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5 mg, 10 mg, 50 mg, 100 mg, 200 mg


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5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: LaunchedSize: 5 mg, 10 mg, 50 mg, 100 mg


1 mg, 5 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g


5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

Bioactivity: Ruxolitinib is a potent and selective inhibitor withJAK1/2s of 3.3 nM and 2.8 nM in cell-free assays, and hasIC50

130-fold selectivity for JAK1/2 over JAK3.

Bioactivity: Ruxolitinib phosphate is a potent inhibitor with sJAK1/2 IC50of 3.3 nM/2.8 nM, respectively, showing more than 130-foldselectivity over JAK3.

Bioactivity: Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib.Ruxolitinib is the first potent, selective inhibitorJAK1/2to enter the clinic with of 3.3 nM/2.8 nM in cell-freeIC50assays.

Bioactivity: Ruxolitinib sulfate is the first potent, selective JAK1/2inhibitor to enter the clinic with s of 3.3 nM/2.8 nM, andIC50has > 130-fold selectivity for JAK1/2 versus JAK3.

Bioactivity: SAR-20347 is an inhibitor of , , and TYK2 JAK1 JAK2 JAK3with s of 0.6, 23, 26 and 41 nM, respectively.IC50

Bioactivity: SB1317 is a potent inhibitor of , , and forCDK2 JAK2 FLT3the treatment of cancer, with of 13, 73, and 56 nM forIC50CDK2, JAK2 and FLT3, respectively.

Bioactivity: Solcitinib is an orally active, competitive, potent, selective inhibitor, with an of 9.8 nM, and 11-, 55- andJAK1 IC50

23-fold selectivity over JAK2, JAK3 and TYK2, respectively;Solcitinib is used in the research of moderate-to-severeplaque-type psoriasis.

Bioactivity: TG101209 is a selective inhibitor with of 6 nM,JAK2 IC50less potent to and with of 25 nM and 17 nM, apprFlt3 RET IC5030-fold selective for JAK2 than JAK3, and sensitive toJAK2V617F and MPLW515L/K mutations.

Bioactivity: Tofacitinib is a inhibitor with s of 1, 20, andJAK3/2/1 IC50112 nM, respectively.

Bioactivity: Tofacitinib citrate is a inhibitor with s of 1,JAK1/2/3 IC5020, and 112 nM, respectively.

Ruxolitinib (INCB018424) Cat. No.: HY-50856

Ruxolitinib phosphate (INCB018424 phosphate) Cat. No.: HY-50858

Ruxolitinib S enantiomer (S-Ruxolitinib; INCB18424) Cat. No.: HY-50856A

Ruxolitinib sulfate (INCB018424 sulfate) Cat. No.: HY-50859

SAR-20347 Cat. No.: HY-100895

SB1317 (TG02) Cat. No.: HY-15166

Solcitinib (GSK-2586184; GLPG-0778) Cat. No.: HY-16755

TG101209 Cat. No.: HY-10410

Tofacitinib (Tasocitinib; CP-690550) Cat. No.: HY-40354

Tofacitinib citrate (Tasocitinib citrate; CP-690550 citrate) Cat. No.: HY-40354A

https://www.MedChemExpress.com/Ruxolitinib.htmlhttps://www.MedChemExpress.com/Ruxolitinib-phosphate.htmlhttps://www.MedChemExpress.com/ruxolitinib-s-enantiomer.htmlhttps://www.MedChemExpress.com/ruxolitinib-sulfate.htmlhttps://www.MedChemExpress.com/SAR-20347.htmlhttps://www.MedChemExpress.com/SB1317.htmlhttps://www.MedChemExpress.com/Solcitinib.htmlhttps://www.MedChemExpress.com/TG101209.htmlhttps://www.MedChemExpress.com/Tofacitinib.htmlhttps://www.MedChemExpress.com/Tofacitinib-citrate.html



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1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg,500 mg, 1 g, 5 g, 10 g



5 mg, 10 mg, 25 mg, 50 mg, 100 mg



1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: TyK2-IN-2 is an inhibitor of , used for treatment ofTYK2inflammatory and autoimmune diseases.

Bioactivity: Tyk2-IN-3 is a inhibitor, with an ofTyk2 pseudokinase IC50485 nM.

Bioactivity: Tyk2-IN-4 is a selective, potent, allosteric inhibitor oftyrosine kinase 2 ( ).Tyk2

Bioactivity: Tyk2-IN-5 (compound 6) is a highly potent, selective andorally active inhibitor and targets the JH2 domain, withTyk2a of 0.086 nM for Tyk2 JH2 and an of 25 nM for IFNα.Ki IC50Highly effective in inhibiting IFNγ production in a ratpharmacodynamics model and fully efficacious in a rat adjuvant…

Bioactivity: Upadacitinib (ABT-494) is a potent and selective Janus kinase( ) 1 inhibitor with an of 43 nM, being developed forJAK IC50the treatment of several autoimmune disorders.

Bioactivity: WHI-P154 is a potent inhibitor, and also modestly blocksEGFR, with s of 4 nM and 1.8 μM, respectively.JAK3 IC50

Bioactivity: WHI-P97 is a rationally designed potent inhibitor of JAK-3.IC50 value: Target: JAK3 Treatment of mast cells with WHI-P97inhibited the translocation of 5-lipoxygenase (5-LO) from thenucleoplasm to the nuclear membrane and consequently5-LO-dependent leukotriene (LT) synthesis after IgE…

Bioactivity: WP1066 is an inhibitor of and , and also showsJAK2 STAT3effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.

Bioactivity: XL019 is a potent and selective JAK2 inhibitor with IC50 of2.2 nM, 100 fold selectivity over JAK1; shows good biochemicaland cellular potency against JAK2 with good selectivityagainst the Janus Kinase family as well as a broad kinasepanel. IC50 Value: 2.2 nM (JAK2); 214.2 nM (JAK3) [1] XL019…

Bioactivity: ZM39923 is a inhibitor, with a of 7.1; ZM39923JAK3 pIC50also potently inhibits tissue transglutaminase ( ) withTGM2an of 10 nM.IC50


TyK2-IN-2 Cat. No.: HY-101762

Tyk2-IN-3 Cat. No.: HY-18709



Upadacitinib (ABT-494) Cat. No.: HY-19569

WHI-P154 Cat. No.: HY-13895

WHI-P97 Cat. No.: HY-11067

WP1066 Cat. No.: HY-15312

XL019 Cat. No.: HY-13775

ZM39923 Cat. No.: HY-12589A

https://www.MedChemExpress.com/TYK2-IN-2.htmlhttps://www.MedChemExpress.com/Tyk2-IN-3.htmlhttps://www.MedChemExpress.com/BMS-986165.htmlhttps://www.MedChemExpress.com/Tyk2-IN-5.htmlhttps://www.MedChemExpress.com/Upadacitinib.htmlhttps://www.MedChemExpress.com/WHI-P154.htmlhttps://www.MedChemExpress.com/WHI-P97.htmlhttps://www.MedChemExpress.com/WP1066.htmlhttps://www.MedChemExpress.com/xl019.htmlhttps://www.MedChemExpress.com/ZM39923.html



10 mg, 50 mg

Bioactivity: ZM39923 hydrochloride is a inhibitor, with a ofJAK3 pIC507.1; ZM39923 hydrochloride also potently inhibits tissuetransglutaminase ( ) with an of 10 nM.TGM2 IC50

ZM39923 hydrochloride Cat. No.: HY-12589

https://www.MedChemExpress.com/ZM39923-hydrochloride.html

Notch

Notch signaling pathway is a highly conserved cell signaling systempresent in most multicellular organisms. Notch is present in allmetazoans, and mammals possess four different notch receptors,referred to as Notch1, Notch2, Notch3, and Notch4. The notchreceptor is a single-pass transmembrane receptor protein. It is ahetero-oligomer composed of a large extracellular portion, whichassociates in a calcium-dependent, non-covalent interaction with asmaller piece of the notch protein composed of a short extracellularregion, a single transmembrane-pass, and a small intracellular region.Notch signaling promotes proliferative signaling during neurogenesis,and its activity is inhibited by Numb to promote neural differentiation.

The notch signaling pathway is important for cell-cell communication, which involves gene regulation mechanismsthat control multiple cell differentiation processes during embryonic and adult life.


https://www.MedChemExpress.com/Targets/Notch.html


Purity: 98.13%Clinical Data: No Development ReportedSize: 5 mg, 10 mg



5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


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5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg

Notch Inhibitors & Modulators

Bioactivity: Avagacestat (BMS-708163) is a potent inhibitor of, with s of 0.27 nM and 0.30 nM for Aβ42 andγ-secretase IC50

Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD(Notch IntraCellular Domain) with of 0.84 nM and sh…IC50

Bioactivity: BMS-983970 is an oral pan-Notch inhibitor for the treatment ofcancer.

Bioactivity: Crenigacestat (LY3039478) is a novel and potent Notchinhibitor.

Bioactivity: FLI-06 is an inhibitor of signaling with an ofNotch EC502.3 μM.

Bioactivity: IMR-1 is a novel class of Notch inhibitors targeting thetranscriptional activation with IC50 of 6 μmol/L. target:Notch IC 50: 6 μmol/L In vitro: IMR-1 prevents the recruitmentof Maml1 to the NTC on chromatin, inhibits Notch target genetranscription, and dramatically inhibits tumor growth . A…

Bioactivity: IMR-1A is the metabolite of IMR-1. IMR-1 is a novel class ofNotch inhibitors targeting the transcriptional activation withIC50 of 6 μmol/L. target: Notch IC 50: 6 μmol/L In vitro:IMR-1 prevents the recruitment of Maml1 to the NTC onchromatin, inhibits Notch target gene transcription, and…

Bioactivity: JI051 is a stabilizer for the interaction,Hes1-PHB2interacts with a cancer-associated protein chaperoneprohibitin 2 ( ), induces cell-cycle arrest by inhibitingPHB2the downstream effector gene Hes1. Anti-cancer activityNotch

.[1]

Bioactivity: LY-411575 is a potent inhibitor with ofγ-secretase IC500.078 nM/0.082 nM (membrane/cell-based), and also inhibitsNotch S3 cleavage with of 0.39 nM.IC50

Bioactivity: Notch inhibitor 1 is a potent inhibitor, with s ofNotch IC507.8 and 8.5 nM for Notch 1 and Notch 3, respectively. Used inthe research of cancer .[1]

Bioactivity: Psoralidin, a natural furanocoumarin, is isolated fromPsoralea corylifolia L. possessing anti-cancer properties.IC50 value: Target: Anticancer natural compound in vitro: PSOdramatically decreased the cell viabilities in dose- andtime-dependent manner. Autophagy inhibitor 3-MA blocked the…

Avagacestat (BMS-708163) Cat. No.: HY-50845

BMS-983970 Cat. No.: HY-12419

Crenigacestat (LY3039478) Cat. No.: HY-12449

FLI-06 Cat. No.: HY-15860

IMR-1 Cat. No.: HY-100431

IMR-1A Cat. No.: HY-100431A

JI051 Cat. No.: HY-117113

LY-411575 Cat. No.: HY-50752

Notch inhibitor 1 Cat. No.: HY-12860

Psoralidin Cat. No.: HY-N0232

https://www.MedChemExpress.com/Targets/Notch.htmlhttps://www.MedChemExpress.com/BMS-708163.htmlhttps://www.MedChemExpress.com/BMS-983970.htmlhttps://www.MedChemExpress.com/LY3039478.htmlhttps://www.MedChemExpress.com/FLI-06.htmlhttps://www.MedChemExpress.com/IMR-1.htmlhttps://www.MedChemExpress.com/IMR-1A.htmlhttps://www.MedChemExpress.com/JI051.htmlhttps://www.MedChemExpress.com/ly-411575.htmlhttps://www.MedChemExpress.com/notch-inhibitor-1.htmlhttps://www.MedChemExpress.com/Psoralidin.html


5 mg, 10 mg


2 mg, 5 mg, 10 mg, 25 mg



5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: RO4929097 (RG-4733) is a inhibitor with ofγ secretase IC504 nM, inhibiting cellular processing of Aβ40 and Notch with EC

of 14 nM and 5 nM, respectively.50

Bioactivity: Semagacestat is a inhibitor, inhibitsγ-secretase ( ), and with of 10.9, 12β-amyloid Aβ42 Aβ38 Aβ40 IC50

and 12.1 nM, respectively; also inhibits signaling withNotch of 14.1 nM.IC50

Bioactivity: Tangeretin (Tangeritin), a flavonoid from citrus fruit peels,has been proven to play an important role in anti-inflammatoryresponses and neuroprotective effects in several diseasemodels, and was also selected as a Notch-1 inhibitor.

Bioactivity: tCFA15 is a trimethyl cyclohexenonic long chain fatty alcoholcontaining 15 carbon atoms on the side chain, promotes thedifferentiation of neurons, and may regulates Notchsignaling.

Bioactivity: YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretaseinhibitor with values of 2.92±0.22 and 2.64±0.30 nM forIC50

and cleavage, respectively.Notch APPL

Bioactivity: Z-Ile-Leu-aldehyde(Z-IL-CHO; GSI-XII) is a potentgamma-Secretase inhibitor; Notch signaling inhibitor.


RO4929097 (RG-4733) Cat. No.: HY-11102

Semagacestat (LY450139) Cat. No.: HY-10009

Tangeretin (Tangeritin; NSC53909; NSC618905) Cat. No.: HY-N0133

tCFA15 Cat. No.: HY-104031

YO-01027 (Dibenzazepine; DBZ) Cat. No.: HY-13526

Z-Ile-Leu-aldehyde (Z-IL-CHO; GSI-XII; γ-Secretase inhibitor XII) Cat. No.: HY-12465

https://www.MedChemExpress.com/RO4929097.htmlhttps://www.MedChemExpress.com/Semagacestat.htmlhttps://www.MedChemExpress.com/Tangeretin.htmlhttps://www.MedChemExpress.com/tCFA15.htmlhttps://www.MedChemExpress.com/YO-01027.htmlhttps://www.MedChemExpress.com/Z-Ile-Leu-aldehyde.html


Oct3/4POU5F1;Slc22a3

Oct3/4 (also known as POU5F1 and Oct4) is regarded as one of thekey regulators of pluripotency. Oct-4 is a homeodomain transcriptionfactor of the POU family. This protein is critically involved in theself-renewal of undifferentiated embryonic stem cells. it is frequentlyused as a marker for undifferentiated cells. Oct-4 expression must beclosely regulated; too much or too little will cause differentiation ofthe cells.

https://www.MedChemExpress.com/Targets/Oct3_4.html


10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg, 200 mg

Oct3/4 Inhibitors & Modulators

Bioactivity: O4I1 is as a potent Oct3/4 inducer. Bioactivity: O4I2 is a potent Oct3/4 inducer in various human cell linesincluding human fibroblasts.

Bioactivity: OAC1 is a Octamer-binding transcription factor 4(Oct4)-activating compound; enhances the iPSC reprogrammingefficiency and accelerated the reprogramming process. IC50value: Target: Oct4 activator in vitro: OAC1 enhances theformation of Oct4-GFP+ colonies and accelerates the dynamics…

Bioactivity: OAC2 is an Oct4-activating compound which activates expressionthrough the Oct4 gene promoter.


O4I1 Cat. No.: HY-18771

O4I2 Cat. No.: HY-18772

OAC1 Cat. No.: HY-12303

OAC2 Cat. No.: HY-12884

https://www.MedChemExpress.com/Targets/Oct3_4.htmlhttps://www.MedChemExpress.com/O4I1.htmlhttps://www.MedChemExpress.com/O4I2.htmlhttps://www.MedChemExpress.com/OAC1.htmlhttps://www.MedChemExpress.com/OAC2.html


PKAProtein kinase A

PKA (Protein kinase A) is a family of enzymes whose activity isdependent on cellular levels of cyclic AMP (cAMP). PKA is also knownas cAMP-dependent protein kinase. Protein kinase A has severalfunctions in the cell, including regulation of glycogen, sugar, and lipidmetabolism.

https://www.MedChemExpress.com/Targets/PKA.html



10 mg, 50 mg, 100 mg



1 mg, 5 mg, 10 mg, 50 mg, 100 mg


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50 mg, 100 mg


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5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg

PKA Inhibitors & Modulators

Bioactivity: 8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt), a cyclic AMPanalog, is an activator of cyclic AMP-dependent protein kinase( ) .PKA [1]

Bioactivity: AT13148 is an orally active and ATP-competitive, multi- AGC inhibitor with s of 38 nM/402 nM/50 nM, 8 nM, 3 nM,kinase IC50

and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II,respectively.

Bioactivity: AT7867 is a potent ATP-competitive inhibitor of / /Akt1 Akt2 and / with s of 32 nM/17 nM/47 nM and 85Akt3 p70S6K PKA IC50

nM/20 nM, respectively.

Bioactivity: AT7867 dihydrochloride is a potent ATP-competitive inhibitorof / / and / with s of 32Akt1 Akt2 Akt3 p70S6K PKA IC50nM/17 nM/47 nM and 85 nM/20 nM, respectively.

Bioactivity: Bucladesine calcium salt(DC2797 calcium salt) is a membranepermeable selective activator of PKA. Target: PKA Bucladesine(bilateral infusion of 10 mM or 100 mM) leads to a significantreduction in escape latency and travel distance (showing animprovement in spatial memory) compared to the control, as…

Bioactivity: Bucladesine sodium salt is a cell-permeable cyclic AMP (cAMP)analog that activates cAMP dependent protein kinase ( ).PKA

Bioactivity: CCG215022 is a G protein-coupled receptor kinases ( s)GRKinhibitor with s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1IC50μM for , and , respectively.GRK2 GRK5 GRK1

Bioactivity: CREBtide, a synthetic 13 amino acid peptide, has been reportedas a substrate.PKA

Bioactivity: Daphnetin (7,8-dihydroxycoumarin), one coumarin derivativeisolated from plants of the , is a Genus Daphne protein kinaseinhibitor, with of 7.67 μM, 9.33 μM and 25.01 μM forIC s50EGFR, PKA and PKC , respectively . Daphne…in vitro [1] [2]

Bioactivity: H-89 is a potent inhibitor of cyclic AMP-dependent proteinkinase ( ) with of 48 nM and has weakprotein kinase A IC50inhibition on PKG, PKC, Casein Kinase, and others kinases.


8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt) Cat. No.: HY-12306

AT13148 Cat. No.: HY-16071

AT7867 Cat. No.: HY-12059

AT7867 dihydrochloride Cat. No.: HY-12059A

Bucladesine calcium salt (Dibutyryl-cAMP calcium salt; DC2797 calcium salt) Cat. No.: HY-B0764A

Bucladesine sodium salt (Dibutyryl-cAMP sodium salt; DC2797; Sodium dibutyryl cAMP) Cat. No.: HY-B0764

CCG215022 Cat. No.: HY-18991

CREBtide Cat. No.: HY-P1595

Daph

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Stem Cell/Wnt - MedchemExpress.com...Stem Cell/Wnt Stem cells are required for continuous tissue maintenance within diverse organs, stem cell activity is often externally dictated