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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-SGK-GSK650394
GSK650394

Chemical Structure : GSK650394

CAS No.: 890842-28-1

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GSK650394 (GSK-650394, GSK 650394)

货号: PC-49625Not For Human Use, Lab Use Only.

GSK650394 (GSK 650394) is a potent, competitive inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1) with IC50 of 62 nM and 103 nM for enzymatic activity of SGK1 and SGK2 repectively, in vitro activity-based scintillation proximity assay (SPA).

规格 价格 库存 数量
5 mg ￥780 In stock
10 mg ￥1180 In stock
25 mg ￥1980 In stock
50 mg ￥3280 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

GSK650394 (GSK 650394) is a potent, competitive inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1) with IC50 of 62 nM and 103 nM for enzymatic activity of SGK1 and SGK2 repectively, in vitro activity-based scintillation proximity assay (SPA).
GSK650394 inhibited SGK1-mediated epithelial transport with an IC50 of 0.6 uM in ldosterone-stimulated short circuit current cellular assay (SCC).
GSK650394 displays 60-fold selective for SGK1 over the upstream AGC kinase PDK1 and , >30-fold selectivity over Akt and other related kinases.
GSK650394 also potently inhibits CAMKK2 enzyme with pIC50 of 9.2.
GSK650394 repressed the androgen-mediated enhancement of Nedd4-2 phosphorylation in LNCaP cells, inhibited the androgen-stimulated growth of LNCaP cells with IC50 of 1 uM and completely abrogated androgen-mediated growth at 10 uM.

物理化学性质&存储条件

分子量 382.46
分子式 C25H22N2O2
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

10 mM in DMSO
Chemical Name/SMILES

2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid

参考文献

1. Sherk AB, et al. Cancer Res. 2008 Sep 15;68(18):7475-83.

2. Thomas SV, et al. J Biol Chem. 2011 Sep 16;286(37):32074-85.

3. Borst O, et al. Blood. 2012 Jan 5;119(1):251-61.

4. Carrow Wells, et al. Cells. 2023 Jan 11;12(2):287.

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