SB-505124 hydrochloride

  • 化学数据
CAS号 356559-13-2 货号 BCP19172
中文名 SB-505124 hydrochloride
英文名 SB-505124 hydrochloride
中文别名
英文别名 SB 505124 hydrochloride;SB505124 hydrochloride;
分子式 C20H22ClN3O2 分子量 371.86
  • 用途
生物活性 in vitro: SB-505124 was identified as a potent inhibitor of the in vitro kinase activity of ALK5 for its substrate Smad3 with an IC50 of 47 ± 5 nM. This compound was determined to be a reversible ATP competitive inhibitor, because prior incubation of the ALK5 kinase with high concentrations of the inhibitor, followed by dilution to a sub-IC50concentration had no effect on the kinetics of Smad3 phosphorylation (data not shown). SB-505124 demonstrated no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. Selectivity of the SB-505124 inhibitor for type I receptors other than ALK5 was first evaluated against ALK4 and ALK2 in vitro. SB-505124 inhibited the closely related ALK4 with an IC50value of 129 ± 11 nM (about 2.5-fold less sensitive than ALK5) but did not inhibit ALK2 at concentrations up to 10 μM . The in vitro drug release study demonstrated 100% drug release within 12 h. The gel did not show cytotoxicity to the cultured rabbit subconjunctival cells by
信号通路 Angiogenesis/Protein Tyrosine Kinase TGF beta/Smad  
靶 点 BMP/TGF beta Receptor ALK 

结构式

本页面部分数据来自于公开的网络资源,所以瀚香生物不能保证其准确性。
不同批次的产品详情请咨询我们的客服:
全国免费电话:400-099-8200
在线客服:
技术支持:
orders@biochempartner.com
瀚香官网:
www.biochempartner.com
瀚香生物(Biochempartner) 的所有产品和服务仅用于科学研究,禁止用于人体和治疗!