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首页-小分子抑制剂&激动剂-TGF-beta/Smad-TGF beta Receptor (TGFBR)-SB-525334
SB-525334

Chemical Structure : SB-525334

CAS No.: 356559-20-1

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SB-525334 (SB 525334, SB525334)

货号: PC-42858Not For Human Use, Lab Use Only.

SB-525334 (SB525334) is a potent and selective inhibitor of TGF-β1 receptor (ALK5) inhibitor with IC50 of 14,5 nM, 4-fold less potent against ALK4 and inactive for ALK2, ALK3, and ALK6 (IC50>10 uM).

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10 mg ￥780 In stock
25 mg ￥1380 In stock
50 mg ￥2180 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SB-525334 (SB525334) is a potent and selective inhibitor of TGF-β1 receptor (ALK5) inhibitor with IC50 of 14,5 nM, 4-fold less potent against ALK4 and inactive for ALK2, ALK3, and ALK6 (IC50>10 uM).
SB 525334 blocks TGFβ1-induced phosphorylation and nuclear translocation of Smad2/3 in renal proximal tubule cells and inhibits TGFβ1-induced increases in PAI-1 and procollagen α1 mRNA expression in A498 renal epithelial carcinoma cells at 1 uM.
SB 525334 significantly inhibits PAN-induced proteinuria in rat model of nephritis-induced renal fibrosis.

物理化学性质&存储条件

分子量 343.4249
分子式 C21H21N5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 46 mg/mL
Chemical Name/SMILES

Quinoxaline, 6-[2-(1,1-dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]-

参考文献

1. Grygielko ET, et al. J Pharmacol Exp Ther. 2005 Jun;313(3):943-51.

2. Laping NJ, et al. Clin Cancer Res. 2007 May 15;13(10):3087-99.

3. Thomas M, et al. Am J Pathol. 2009 Feb;174(2):380-9.

4. Kim YJ, et al. Anticancer Res. 2012 Mar;32(3):799-806.

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