LY364947
货号：
13341-50mg 基本售价：
8288.0 元 规格：
50 mg
产品信息
概述| 货号 | 13341-50mg |
| 描述 | 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 (MLK7; 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 |
| 别名 | HTS 466284;TGF-β RI Kinase Inhibitor; |
性能| 供应商 | Cayman |
| 应用文献 |
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. Journal of Medicinal Chemistry 46(19), 3953-3956 (2003).
2.Li, H.y.,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. Journal of Medicinal Chemistry 49, 2138-2142 (2006).
3.Shiou, S.R.,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. The Journal of Biological Chemisty 281(45), 33971-33981 (2006).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 272.3 |
| 分子式 | C17H12N4 |
| CAS号 | 396129-53-6 |
| 稳定性 | ≥ 2 years |
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