Cat. No. 2718
Alternative Name: HTS 466284
Chemical Name: 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]
Biological ActivitySelective 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
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. PMID: 16539403.
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. PMID: 16959768.
Sawyer et al (2003) Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-μ type I receptor kinase domain. J.Med.Chem. 46 3953. PMID: 12954047.
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Citations are publications that use Tocris products. Selected citations for LY 364947 include:
Oruqaj et al (2015) Compromised peroxisomes in idiopathic pulmonary fibrosis, a vicious cycle inducing a higher fibrotic response via TGF-β signaling. Proc Natl Acad Sci U S A 112 E2048. PMID: 25848047.
Oshimori et al (2015) TGF-β promotes heterogeneity and drug resistance in squamous cell carcinoma. Cell 160 963. PMID: 25723170.
Jajosky et al (2014) RepSox slows decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression. Stem Cells Transl Med 3 836. PMID: 24855276.
Oerlecke et al (2013) Cyclic AMP enhances TGFβ responses of breast cancer cells by upregulating TGFβ receptor I expression. PLoS One 8 e54261. PMID: 23349840.
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Keywords: LY 364947, supplier, Selective, inhibitors, inhibits, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1Transforming, Growth, Factors, Beta, Receptors, TGF-beta, Receptor, Serine/Threonine, Kinases, RSTKs, LY364947, HTS466284, Tocris Bioscience, TGF-β Receptor Inhibitor products
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November 12 - 16, 2016
San Diego, CA, USA