CAS:694433-59-5SB-505124

SB505124 is an inhibitor of TGFβ receptor for ALK4 (IC50 = 129 nM) and ALK5 (IC50 = 47 nM). It can also inhibit ALK7.

规格	价格	促销价格	库存

18817579266

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咨询

18817579266

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实验数据

技术信息

CAS号

694433-59-5

储存条件

分子式

C20H21N3O2

运输

蓝冰

分子量

335.40

别名

溶解度

动物实验配方

5%DMSO+40%PEG400+5% tween80+H2O

5 mg/mL

clear

生物活性

描述Transforming growth factor (TGF) -β is a multifunctional cytokine that can inhibit endothelial and epithelial cellular proliferation, stimulate matrix accumulation, and suppress inflammation. Signaling by the TGF-β superfamily is mediated by two types of transmembrane receptor serine/threonine kinases, types I and II, ligand interaction with a homodimer of type II receptors recruits and activates homodimers of type I receptors or activin receptor-like kinases (ALKs). SB505124 is an inhibitor of TGFβ receptor ALK4 and ALK5 with IC₅₀ of 47 nM and 129 nM, respectively. FaO cells or NRP 154 cells were protected from TGF-β–induced apoptosis by SB-505124 (0.01-1µM) in a concentration-dependent manner. Specific inhibition of the TGF-β type I receptor/ALK5 serine-threonine kinase with SB-505124 (500 nM) abolished the effects of TGF-β1 on F-actin assembly in HUVEC cells. Treatment with 0.25 μM-SB505124 in Sh3bp2^KI/KI bone marrow stromal cultures reduced RANKL (a critical regulator of osteoclast formation) expression almost back down to wild type levels.