LY 364947 | Receptor Serine / Threonine Kinases (RSTKs) | Selective Inhibitor Of TGF-b Type-I Receptor (TGF-b RI, ALK-5) | HTS 466284 | LY364947

Category:

Enzyme-Linked Receptors

Receptor Serine/Threonine Kinases (RSTKs)

TGF-beta

Cat.No.

Product Name

2718

LY 364947

Alternative name(s):

HTS 466284

LY 364947 C17H12N4 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline

Price and Availability

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LY 364947

Chemical Name: 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline

Biological Activity:

Selective inhibitor of TGF-β type-I receptor (TGF-β RI, TGFR-I, TβR-I, ALK-5) (IC₅₀ values are 59, 400 and 1400 nM for TGR-β RI, TGF-β RII and MLK-7K respectively). Inhibits TGF-β-dependent luciferase production in mink lung cells (p3TP lux) and growth in mouse fibroblasts (NIH 3T3) (IC₅₀ values are 47 and 89 nM respectively). Suppresses invasion of MDA-MB-231 breast cancer cells in a matrigel invasion assay.

Technical Data:

M.Wt:	272.31
Formula:	C₁₇H₁₂N₄
Storage:	Store at RT
Solubility:	Soluble to 100 mM in DMSO
Purity:	>99%
CAS No:	[396129-53-6]

Resources:

Certificate of Analysis / MSDS:

Certificate of Analysis: View current batch

Product/Material Safety Data Sheet: View current batch

References:

Sawyer et al (2003) Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain. J.Med.Chem. 46 3953. Li et al (2006) Dihydropyrrolopyrazole transforming growth factor-β type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-β type II receptor kinase and mixed lineage kinase 7. J.Med.Chem. 49 2138. Shiou et al (2006) Smad4-dependent regulation of urokinase plasminogen activator secretion and RNA stability associated with invasiveness by autocrine and paracrine transforming growth factor-β. J.Biol.Chem. 281 33971.

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Keywords: LY 364947, Receptor Serine / Threonine Kinases (RSTKs), Selective Inhibitor Of TGF-b Type-I Receptor (TGF-b RI, ALK-5), HTS 466284, LY364947, Tocris Bioscience

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Product Feature

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