LY364947

Transforming growth factor-beta (TGF-beta) signals through a cell surface heteromeric complex involving type I (TGF-beta RI) and type II (TGF-beta RII) receptors. Downstream signal transduction is mediated by the TGF-beta RI kinase domain through the phosphorylation of Smad proteins. LY364947 is a selective inhibitor of TGF-beta RI (TGFR-I, TbetaR-I, ALK-5), with an IC50 value of 59 nM. LY364947 less effectively inhibits TGF-beta RII (IC50 = 400 nM), p38 MAPK (IC50 = 740 nM), and mixed-lineage kinase 7 (MLK7, IC50 = 1,400 nM). It inhibits TGF-beta-induced cell growth (IC50 = 89 nM) in NIH 3T3 mouse fibroblasts and TGF-beta-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.Formal Name: 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-quinoline. CAS Number: 396129-53-6. Synonyms: HTS 466284, TGF-beta RI Kinase Inhibitor. Molecular Formula: C17H12N4. Formula Weight: 272.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 1 mg/ml. lambdamax: 229, 283 nm. SMILES: C1(C2=CC=NC3=C2C=CC=C3)=CNN=C1C4=NC=CC=C4. InChi Code: InChI=1S/C17H12N4/c1-2-6-15-13(5-1)12(8-10-19-15)14-11-20-21-17(14)16-7-3-4-9-18-16/h1-11H,(H,20,21). InChi Key: IBCXZJCWDGCXQT-UHFFFAOYSA-N.