货号 | 2718/10 |
别名 | 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl] |
供应商 | Tocris |
生物活性 | 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. |
运输条件 | Blue Ice |
存放说明 | Ambient |
纯度 | >99 % |
计算分子量 | 272.31 |
分子式 | C17H12N4 |
可溶性/溶解性 | Soluble to 100 mM in DMSO |
CAS号 | 396129-53-6 |
参考文献 | Liet 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. Shiouet 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. Sawyeret 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. |