Uprosertib hydrochloride (GSK2141795 hydrochloride) 是一种有效的，选择性的 Akt 广谱抑制剂，抑制 Akt1/Akt2/Akt3 的活性，IC50 值分别为 180/328/38 nM。
CAS：1047635-80-2
分子式：C18H17Cl3F2N4O2
分子量：465.71
纯度：98%
存储：Store at -20°C

Background:

Uprosertib hydrochloride (GSK2141795 hydrochloride) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively. Akt1|180 nM (IC50)|Akt2|328 nM (IC50)|Akt3|38 nM (IC50)|CDK7|2100 nM (IC50)|ROCK1|1570 nM (IC50)|ROCK2|1850 nM (IC50)

Uprosertib inhibits Akt1/2/3 with the Kd values of 16/49/5 nM, respectively. Uprosertib potently inhibits only the PKC family members PRKACA and PRKACB as well as the cGMP-dependent protein kinase PRKG1 aqpart from the Akts. Protein targets that bind Uprosertib in the lysate show a dose-dependent reduction in binding to the kinobeads, while proteins unaffected by the drug show no reduction in binding[1].

[1]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800.