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LY364947

Cayman Chemical Item Number 13341

TGF-β RI Kinase Inhibitor; HTS 466284 (CAS 396129-53-6)

LY364947 (CAS 396129-53-6)

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Description

Transforming growth factor-β (TGF-β) signals through a cell surface heteromeric complex involving type I (TGF-β RI) and type II (TGF-β RII) receptors. Downstream signal transduction is mediated by the TGF-β RI kinase domain through the phosphorylation of Smad proteins. LY364947 is a selective inhibitor of TGF-β RI (TGFR-I, TβR-I, ALK-5), with an IC50 value of 59 nM.1 LY364947 less effectively inhibits TGF-β RII (IC50 = 400 nM), p38 MAPK (IC50 = 740 nM), and mixed lineage kinase-7 (MLK-7; IC50 = 1,400 nM).1,2 It inhibits TGF-β-induced cell growth (IC50 = 89 nM) in NIH 3T3 mouse fibroblasts1 and TGF-β-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.3

1 Sawyer, J.S., Anderson, B.D., Beight, D.W., et al. Synthesis and activity of new aryl- and heteroaryl-substituted pyrazoleInhibitors of the transforming growth factor-b type I receptor kinase domain. J Med Chem 46(19) 3953-3956 (2003).

2 Li, H., Wang, Y., Heap, C.R., et al. Dihydropyrrolopyrazole transforming growth factor-b type I receptor kinase domain inhibitors: A novel benzimidazole series with selectivity versus transforming growth factor-b type II receptor kinase and mixed lineage kinase-7. J Med Chem 49 2138-2142 (2006).

3 Shiou, S., Datta, P.K., Dhawan, P., et al. Smad4-dependent regulation of urokinase plasminogen activator secretion and RNA stability associated with invasiveness by autocrine and paracrine transforming growth facto. J Biol Chem 281(45) 33971-33981 (2006).

Synonyms
  • TGF-β RI Kinase Inhibitor
  • HTS 466284
Formal Name 4-​[3-​(2-​pyridinyl)-​1H-​pyrazol-​4-​yl]-​quinoline
CAS Number 396129-53-6
Molecular Formula C17H12N4
Formula Weight 272.3
Formulation A crystalline solid
Purity ≥98%
λmax 229, 283 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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C1(C2=CC=NC3=C2C=CC=C3)​=CNN=C1C4=NC=CC=C4

Background Reading

Sawyer, J.S., Anderson, B.D., Beight, D.W., et al. Synthesis and activity of new aryl- and heteroaryl-substituted pyrazoleInhibitors of the transforming growth factor-b type I receptor kinase domain. J Med Chem 46(19) 3953-3956 (2003).

Li, H., Wang, Y., Heap, C.R., et al. Dihydropyrrolopyrazole transforming growth factor-b type I receptor kinase domain inhibitors: A novel benzimidazole series with selectivity versus transforming growth factor-b type II receptor kinase and mixed lineage kinase-7. J Med Chem 49 2138-2142 (2006).

Shiou, S., Datta, P.K., Dhawan, P., et al. Smad4-dependent regulation of urokinase plasminogen activator secretion and RNA stability associated with invasiveness by autocrine and paracrine transforming growth facto. J Biol Chem 281(45) 33971-33981 (2006).

LY364947 is available in the following screening library:

Size Price Quantity Subtotal
5 mg $74.00 $0.00
10 mg $141.00 $0.00
25 mg $333.00 $0.00
50 mg $592.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-05-26. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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