Each week, we meet to review our new products… and want to share them with you!

Our presentation contains information on each item including structures or diagrams.

To learn more, follow the link in the Product Name to visit our website.

June 16 – June 22, 2015

DAGLα inhibitor

14009 O-7460 A selective inhibitor of 2-AG biosynthesis via

diacylglycerol lipase α (IC50 = 690 nM)

Much weaker inhibition towards human MAGL and rat brain FAAH (IC50s > 10 µM)

Does not bind to CB1 or CB2 cannabinoid receptors (Kis > 10 µM)

0-12 mg/kg, i.p. dose-dependently inhibits high-fat diet intake and reduces body weight in mice

Sodium/Glucose Cotransporter 2 inhibitor

15951 fluoro-Dapagliflozin

An analog of dapagliflozin that displays similar selectivity for inhibiting SGLT2 over SGLT1 (Kis = 5.3 and 330 nM)

10 nM significantly reduces phlorizin-sensitive sugar transport in COS-1 cells expressing human SGLT2

Cancer Research

17546 (S)-α-Methylbenzyl Ricinoleamide

A fatty acid amide derived from ricinoleic acid and methyl benzylamine

Inhibits growth of glioma (U251), breast (MCF-7), ovarian (NCI-ADR/RES and OVCAR-3), kidney (786-0), non-small cell lung (NCI-H460), and prostate (PC-3) cancer cells (mean GI50 = 6.9 µM)

Cancer Research17648 Cdk4 Inhibitor

A cell-permeable, asymmetrical indolocarbazole that selectively blocks cyclin D1/Cdk4 (IC50 = 0.8 μM)

7-fold and 28-fold weaker activity against cyclin E/Cdk2 and cyclin B/Cdk1, with little activity against CaMK II and PKA

Inhibits HCT-116 and NCI-H460 tumor cell growth (IC50s < 3.0 μM), inducing G1 cell cycle arrest

Cancer Research cont.

17860 3MB-PP1 A bulky purine analog that acts as a selective, ATP-competitive,

analog-sensitive polo-like kinase 1 (Plk1) allele inhibitor

10 µM blocks mitotic progression in cells expressing analog-sensitive Plk1 alleles

Used to selectively sensitize Plk1 to small-molecule inhibitors

PPARγ agonist17681 Darglitazone A thiazolidinedione that increases the sensitivity of cells to insulin

Stimulates insulin-induced PI3K activity at >µM concentrations by increasing the expression of the p85 subunit of PI3K

Increases insulin effectiveness in obese non-insulin-dependent diabetes mellitus subjects

Promotes adipocyte differentiation by up-regulating the expression of uncoupling protein-2

Adenylyl Cyclase Type V inhibitor

17777 NKY80 A cell-permeable, selective adenylyl cyclase type V inhibitor (IC50

= 8.3 μM)

Much weaker potency for type II and III isoforms (IC50 = 1.7 mM and 132 μM)

Tissue selective for the adenylyl cyclase catalytic activity in heart and lung tissues

Muscarinic receptor agonist

17802Cevimeline (hydrochloride) A muscarinic receptor agonist

• M1 (EC50 = 23 nM)

• M3 (EC50 = 48 nM)

• M5 (EC50 = 63 nM)

• M2 (EC50 > 1 µM)

• M4 (EC50 > 1 µM)

Stimulates secretion by salivary glands and ameliorates xerostomia (dry mouth)

Ras transformation inhibitor

17804 SCH 51344

Inhibits Ras-induced malignant transformation

Prevents anchorage-independent growth of oncogene transformed fibroblasts

5-25 µM dose-dependently block Ras/Rac-induced membrane ruffling in REF-52 fibroblasts

Does not affect on Ras-induced ERK and JNK kinase activity

Inhibits human mutT homolog MTH1, a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (Kd = 49 nM)

Respiratory syncytial virus inhibitor

17805 VP-14637

A small molecule inhibitor of RSV (EC50 = 1.4 nM)

Interferes directly with RSV fusion (EC50 = 5.4 nM), binding to the viral F protein, which allows simultaneous interaction with both of the heptad repeat domains of the F protein trimer

Metabolic pathway intermediates

17863 α-D-Galactose-1-phosphate (potassium salt ) An intermediate in the interconversion of glucose and galactose

Produced from galactose by galactokinase

17865 DL-Glyceraldehyde 3-phosphate

An intermediate in several metabolic pathways, including glycolysis and gluconeogenesis

Can be derived from fructose 1,6-bisphosphate by fructose bisphosphate aldolase

Processed to 1,3-bisphosphoglycerate by glyceraldehyde phosphate dehydrogenase and NAD+

Free radical scavenger

9001577Salvianolic Acid B Antioxidant and free radical scavenging

compound extracted from S. miltiorrhiza

Cardioprotective and chemopreventative properties:

Reduces leukocyte-endothelial adherence, inhibits inflammation and metalloproteinase expression from aortic smooth muscle cells, and regulates immune function and certain intracellular kinase associated signaling pathways

Pharmaceutical Impurity

17795 Isopropyl Benzenesulfonate

A sulfonate ester genotoxic impurity found in active pharmaceutical ingredients

Potentially exerta toxic effects in bacterial and mammalian cells

Antifungal analytical standard

17803 Voriconazole-d3

An internal standard for the quantification of voriconazole (Item No. 15633) by GC- or LC-mass spectrometry

Voriconazole is a triazole, antifungal agent that inhibits a broad range of pathogenic yeasts

Dasatinib intermediate

17806 CAY10697

An intermediate in the synthesis of dasatinib

Dasatinib (Item No. 11498) is a potent inhibitor of receptor and non-receptor tyrosine kinases, including some drug resistant mutant forms

Forensic Science standards

15620 PF-03550096

A synthetic cannabinoid that selectively targets the peripheral CB2 receptor over the central CB1 receptor (Kis = 7.9 and 1,500 nM for human isoforms)

17947 AB-FUBINACA metabolite 2B A single diastereomer whose relative stereochemistry is unknown

Cayman Chemical products containing Certified Reference Material (CRM) in the name are highly qualified materials manufactured and tested to meet ISO/IEC 17025:2005 and ISO Guide 34:2009 international guidelines for reference materials. These materials are tested using validated analytical methods on qualified instrumentation to ensure traceability to SI units of measure. Cayman’s CRMs are tested for Homogeneity and Stability and are provided with a certificate stating the CRM property value(s) along with the combined uncertainty of the property value(s). These materials are intended for quantitative applications where quantitative accuracy and uncertainty are critical. Cayman Chemical is committed to providing quality products to its customers as evidenced by its accreditation to the ISO/IEC 17025:2005 and ISO Guide 34:2009 standards. For copies of accreditation certificates or more information on Cayman’s CRM product line, please visit our website or contact your local sales representative.

17726 5-fluoro CUMYL-PINACA CRM

Certified Reference Material