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STEMCELL Technologies is committed to making your research work. As Scientists Helping Scientists, we support you with novel products of consistent, unfailing quality and unparalleled technical support. Small Molecules for Cancer Research With demonstrated effects on survival, proliferation, migration, invasion or differentiation of cancer cells, or immunomodulation of host cells, small molecules are increasingly transforming cancer research projects. Small molecules from STEMCELL Technologies are being widely used in high impact research to target key pathways in cancer biology. For more information and examples of how these molecules are being used in cancer cell research, visit www.stemcell.com/smallmolecules. DOCUMENT #27001 | VERSION 1.0.0 Detection of Cancer Stem Cells To detect cancer stem and precursor cells in multiple tissue types, use ALDEFLUOR . A highly effective tool for non-immunological identification, the ALDEFLUOR fluorescent reagent system offers a novel approach to identify, evaluate and isolate stem and progenitor cells based on their expression of aldehyde dehydrogenase enzyme. Isolation of Rare Cell Types Our innovative cell isolation products provide a simple, fast and effective method for isolating rare cell types with high purity and recovery. Use RosetteSep , EasySep and RoboSep cell isolation platforms to enrich circulating tumor cells (CTCs) from whole blood or PBMCs; multiple myeloma cells from bone marrow or whole blood; or untouched B cells from chronic lymphoid leukemia (B-CLL) patient samples for downstream analysis and research. Culture of Cancer Cells Perform functional studies on cancer cells to evaluate how these cells respond to cytotoxic compounds and to study the mechanisms of malignant transformation and tumor progression, using STEMCELL’s specialized media and cultureware for a wide variety of tissue types. AggreWell plates for 3D spheroid and tumorsphere formation MammoCult media for the study of breast cancer cells MethoCult semi-solid methylcellulose media for the study of leukemic cells StemSpan serum-free media for the study of leukemic cells NeuroCult media for the study of brain tumor stem cells GLUCOCORTICOID RECEPTOR WNT WNT RHO AKT mTOR GSK3 PI3K PDK1 MEK1/2 RAS RAS-GAP RAF AC PDE2 PKA PKC ERK1/2 ERK1/2 ROCK MYOSIN ACTIN PCN SMAD 2/3 DSH SMAD 1/5/8 SMAD4 cAMP DAG βCAT TCF/LEF SMAD ACTIVIN TGFβ1 NODAL βCAT GLI SMAD4 EZH2 G9a LSD1 AXIN TNKS1/2 GSK3 APC ANOIKIS TGFβRII TGFβRI ALK4/5/7 BMPRI ALK2/3/6 BMPRII TFs TFs FRIZZLED HH CYTOKINE CYTOKINE Ca 2+ Ca 2+ PATCHED GPCR GPCR GPCR SMO CADHERIN CADHERIN INTEGRIN RTK 5-HT γ-SECRETASE DELTA JAGGED NOTCH NICD NICD ECM Me HDACs HATs Ac ADENYLYL CYCLASE PORCUPINE EXTRACELLULAR MATRIX DNMTs Me FAK RECEPTOR JAK STAT STAT IKK NF-κβ PRAS40 JMJD SRC ABL AMPK RSK Raptor IKB ESTROGEN ER ER GPCR NF-κβ ESTROGEN ESTROGEN RECEPTOR MKK3/6 p38 MAPK p53 SCD1 STEAROYL-CoA APOPTOSIS OLEOYL-CoA Stress JNK MKK7 MKK4 TRANSCRIPTION FACTORS ESTROGEN ) ( 5-HYDROXYTRYPTAMINE (SEROTONIN RECEPTOR) RA RA RETINOIC ACID RECEPTOR TYROSINE KINASE RXR RA TFs NICD G G GLUCOCORTICOID G GR SMAD GR RAR RAR GLI BMP PATHWAY OR TARGET SMALL MOLECULES Glucocorticoid Activator: Dexamethasone Estrogen Modulators: Tamoxifen, Raloxifene Activin/Nodal/TGFβ Inhibitors: SB431542, LY364947, RepSox Activators: IDE1, IDE2 BMP Inhibitors: Dorsomorphin, LDN193189 WNT Inhibitors: IWP-2, IWP-3, IWP-4, XAV939, IWR-1-endo, KY02111 Activators: CHIR99021, BIO, Kenpaullone, SB216763, TWS119, CHIR98014 Modulators: IQ-1, ID-8 Notch Inhibitors: DAPT, LY411575, DBZ RHO/ROCK Inhibitors: Y-27632, Thiazovivin, (-)-Blebbistatin, Pyrintegrin Activator: 1-Oleoyl Lysophosphatidic Acid FAK Inhibitor: FAK Inhibitor 14 JAK/STAT Inhibitors: AG-490, Ruxolitinib, TG101348, WHI-P131, WHI-P154 NF-κB Inhibitors: CAY10512, (S)-MG132, QNZ, Resveratrol AMPK Activators: A769662, Metformin, AICAR Tyrosine Kinases (broad range) Inhibitors: Vandatenib, SU5416 EGFR Inhibitors: AG-490, Gefitinib, Lapatinib FGFR Inhibitor: PD173074 MET Inhibitors: SU11274, Tivantinib ABL Inhibitors: Dasatinib, Nilotinib, Imatinib mTOR Inhibitors: AZD8055, Everolimus, Ku-0063794, Rapamycin, Torin1 PI3K/AKT Inhibitors: Akt Inhibitor VIII, Akt Inhibitor X, GDC-0941, KP372-1, LY294002, Wortmannin Activator: PS-48 MEK/ERK Inhibitors: PD0325901, PD98059, Pluripotin, Reversine, AZD6244, Refametinib, Trametinib, U-0126 Ras/Raf Inhibitors: AZ628, Dabrafenib, PLX4032 SRC Inhibitors: Dasatinib, PP1 cAMP Inhibitor: HA-100 Activators: Prostaglandin E2, Forskolin, EHNA, IBMX, Rolipram p38 MAPK Inhibitors: SB203580, BIRB-796, SB202190 JNK/c-Jun Inhibitor: SP600125 p53 Inhibitors: Cyclic Pifithrin-α, Pifithrin-μ Oleic Acid Biosynthesis Inhibitor: PlurSln-1 PKC Inhibitors: (+)-Bay K8644, HA-100, Gö6983 Activators: Prostaglandin E2, (-)-Indolactam V Hedgehog Inhibitors: Cyclopamine, HPI-1 Activators: Purmorphamine, GSA10, SAG Retinoids Activators: 9-cis Retinoic Acid, All-Trans Retinoic Acid, CD437, TTNPB, AM580, EC23 DNA Methyltransferase Inhibitors: 5-Azacytidine, RG108, Zebularine, RSC-133 Histone Methyltransferase Inhibitors: 3-Deazaneplanocin A, BIX01294 Histone Demethylase Inhibitors: Tranylcypromine, KP372-1, JIB-04 Histone Acetyltransferase Inhibitor: Garcinol Histone Deacetylase Inhibitors: Sodium Butyrate, Trichostatin A, Valproic Acid Mircotubule Organization Inhibitor: Paclitaxel HIF-1 Inhibitor: CAY10585 Protein Trafficking Inhibitor: Brefeldin A Aurora Kinase Inhibitor: MK0457 Cyclin/CDK Inhibitor: SU9516 FOR RESEARCH USE ONLY. NOT INTENDED FOR HUMAN OR ANIMAL DIAGNOSTIC OR THERAPEUTIC USES. STEMCELL TECHNOLOGIES INC.’S QUALITY MANAGEMENT SYSTEM IS CERTIFIED TO ISO 13485 MEDICAL DEVICE STANDARDS. Small Molecules, Big Impact In Cancer Research

Small Molecules, Big Impact - Stemcell Technologies...Small Molecules for Cancer Research With demonstrated effects on survival, proliferation, migration, invasion or differentiation

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Page 1: Small Molecules, Big Impact - Stemcell Technologies...Small Molecules for Cancer Research With demonstrated effects on survival, proliferation, migration, invasion or differentiation

STEMCELL Technologies is committed to making your research work. As Scientists Helping Scientists, we support you with novel products of consistent, unfailing quality and unparalleled technical support.

Small Molecules for Cancer ResearchWith demonstrated effects on survival, proliferation, migration, invasion or differentiation of cancer cells, or immunomodulation of host cells, small molecules are increasingly transforming cancer research projects. Small molecules from STEMCELL Technologies are being widely used in high impact research to target key pathways in cancer biology. For more information and examples of how these molecules are being used in cancer cell research, visit www.stemcell.com/smallmolecules.

DOCUMENT #27001 | VERSION 1.0.0

Detection of Cancer Stem CellsTo detect cancer stem and precursor cells in multiple tissue types, use ALDEFLUOR™. A highly effective tool for non-immunological identification, the ALDEFLUOR™ fluorescent reagent system offers a novel approach to identify, evaluate and isolate stem and progenitor cells based on their expression of aldehyde dehydrogenase enzyme.

Isolation of Rare Cell TypesOur innovative cell isolation products provide a simple, fast and effective method for isolating rare cell types with high purity and recovery. Use RosetteSep™, EasySep™ and RoboSep™ cell isolation platforms to enrich circulating tumor cells (CTCs) from whole blood or PBMCs; multiple myeloma cells from bone marrow or whole blood; or untouched B cells from chronic lymphoid leukemia (B-CLL) patient samples for downstream analysis and research.

Culture of Cancer CellsPerform functional studies on cancer cells to evaluate how these cells respond to cytotoxic compounds and to study the mechanisms of malignant transformation and tumor progression, using STEMCELL’s specialized media and cultureware for a wide variety of tissue types.

• AggreWell™ plates for 3D spheroid and tumorsphere formation

• MammoCult™ media for the study of breast cancer cells

• MethoCult™ semi-solid methylcellulose media for the study of leukemic cells

• StemSpan™ serum-free media for the study of leukemic cells

• NeuroCult™ media for the study of brain tumor stem cells

GLUCOCORTICOID RECEPTOR

WNT

WNT

RHO

AKT

mTOR GSK3

PI3K

PDK1 MEK1/2

RAS

RAS-GAP

RAFAC

PDE2PKA

PKC

ERK1/2

ERK1/2

ROCK

MYOSIN

ACTIN

PCN

SMAD2/3

DSH

SMAD1/5/8

SMAD4

cAMP

DAG

βCAT

TCF/LEF

SMAD

ACTIVIN

TGFβ1NODAL

βCAT

GLI

SMAD4

EZH2

G9a

LSD1

AXIN

TNKS1/2

GSK3

APC

ANOIKIS

TGFβRII

TGFβRI

ALK4/5/7

BMPRI

ALK2/3/6

BMPRII

TFs

TFs

FRIZZLED

HH

CYTOKINECYTOKINE

Ca2+

Ca2+

PATCHED

GPCR GPCR

GPCR

SMO

CADHERIN

CADHERIN INTEGRIN RTK 5-HT

γ-SECRETASE

DELTA JAGGED

NOTCH

NICD

NICD

ECM

Me

HDACs

HATs

Ac

ADENYLYL CYCLASE

PORCUPINE

EXTRACELLULAR MATRIX

DNMTs

Me

FAK

RECEPTOR

JAK

STAT

STAT

IKK

NF-κβ

PRAS40

JMJD

SRC

ABL

AMPK

RSK

Raptor

IKB

ESTROGEN

ER

ER

GPCR

NF-κβ

ESTROGEN

ESTROGENRECEPTOR

MKK3/6

p38 MAPK

p53

SCD1

STEAROYL-CoA

APOPTOSIS

OLEOYL-CoA

Stress

JNK

MKK7 MKK4

TRANSCRIPTION FACTORS

ESTROGEN

) (5-HYDROXYTRYPTAMINE(SEROTONIN RECEPTOR)

RA

RA

RETINOICACID

RECEPTOR TYROSINEKINASE

RXRRA

TFs

NICD

G

G

GLUCOCORTICOID

GGR

SMAD

GR

RAR

RAR

GLI

BMP

PATHWAY OR TARGET SMALL MOLECULES

Glucocorticoid Activator: Dexamethasone

Estrogen Modulators: Tamoxifen, Raloxifene

Activin/Nodal/TGFβInhibitors: SB431542, LY364947, RepSoxActivators: IDE1, IDE2

BMP Inhibitors: Dorsomorphin, LDN193189

WNT

Inhibitors: IWP-2, IWP-3, IWP-4, XAV939, IWR-1-endo, KY02111Activators: CHIR99021, BIO, Kenpaullone, SB216763, TWS119, CHIR98014Modulators: IQ-1, ID-8

Notch Inhibitors: DAPT, LY411575, DBZ

RHO/ROCK

Inhibitors: Y-27632, Thiazovivin, (-)-Blebbistatin, Pyrintegrin

Activator: 1-Oleoyl Lysophosphatidic Acid

FAK Inhibitor: FAK Inhibitor 14

JAK/STAT Inhibitors: AG-490, Ruxolitinib, TG101348, WHI-P131, WHI-P154

NF-κB Inhibitors: CAY10512, (S)-MG132, QNZ, Resveratrol

AMPK Activators: A769662, Metformin, AICAR

Tyrosine Kinases (broad range) Inhibitors: Vandatenib, SU5416

EGFR Inhibitors: AG-490, Gefitinib, Lapatinib

FGFR Inhibitor: PD173074

MET Inhibitors: SU11274, Tivantinib

ABL Inhibitors: Dasatinib, Nilotinib, Imatinib

mTOR Inhibitors: AZD8055, Everolimus, Ku-0063794, Rapamycin, Torin1

PI3K/AKTInhibitors: Akt Inhibitor VIII, Akt Inhibitor X, GDC-0941, KP372-1, LY294002, WortmanninActivator: PS-48

MEK/ERK Inhibitors: PD0325901, PD98059, Pluripotin, Reversine, AZD6244, Refametinib, Trametinib, U-0126

Ras/Raf Inhibitors: AZ628, Dabrafenib, PLX4032

SRC Inhibitors: Dasatinib, PP1

cAMPInhibitor: HA-100Activators: Prostaglandin E2, Forskolin, EHNA, IBMX, Rolipram

p38 MAPK Inhibitors: SB203580, BIRB-796, SB202190

JNK/c-Jun Inhibitor: SP600125

p53 Inhibitors: Cyclic Pifithrin-α, Pifithrin-μ

Oleic Acid Biosynthesis Inhibitor: PlurSln-1

PKCInhibitors: (+)-Bay K8644, HA-100, Gö6983Activators: Prostaglandin E2, (-)-Indolactam V

HedgehogInhibitors: Cyclopamine, HPI-1Activators: Purmorphamine, GSA10, SAG

Retinoids Activators: 9-cis Retinoic Acid, All-Trans Retinoic Acid, CD437, TTNPB, AM580, EC23

DNA Methyltransferase Inhibitors: 5-Azacytidine, RG108, Zebularine, RSC-133

Histone Methyltransferase Inhibitors: 3-Deazaneplanocin A, BIX01294

Histone Demethylase Inhibitors: Tranylcypromine, KP372-1, JIB-04

Histone Acetyltransferase Inhibitor: Garcinol

Histone Deacetylase Inhibitors: Sodium Butyrate, Trichostatin A, Valproic Acid

Mircotubule Organization Inhibitor: Paclitaxel

HIF-1 Inhibitor: CAY10585

Protein Trafficking Inhibitor: Brefeldin A

Aurora Kinase Inhibitor: MK0457

Cyclin/CDK Inhibitor: SU9516

FOR RESEARCH USE ONLY. NOT INTENDED FOR HUMAN OR ANIMAL DIAGNOSTIC OR THERAPEUTIC USES. STEMCELL TECHNOLOGIES INC.’S QUALITY MANAGEMENT SYSTEM IS CERTIFIED TO ISO 13485 MEDICAL DEVICE STANDARDS.

Small Molecules, Big ImpactIn Cancer Research