| Description | Uprosertib hydrochloride is a potent and selective inhibitor of pan-Akt (IC50: 180/328/38 nM for Akt1/Akt2/Akt3, respectively). |
| In vitro | Protein targets that bind Uprosertib in the lysate display a dose-dependent reduction in binding to the kinobeads, while proteins unaffected by the drug display no reduction in binding. Uprosertib inhibits Akt1/2/3 (Kd: 16/49/5 nM, respectively) and it also potently inhibits only the PKC family members PRKACA and PRKACB as well as the cGMP-dependent protein kinase PRKG1 aqpart from the Akts[1]. |
| Target activity | CDK7:2100 nM, Akt3:38 nM, ROCK1:1570 nM, ROCK2:1850 nM, Akt2:328 nM, Akt1:180 nM |
| Synonyms | GSK2141795 (hydrochloride) |
| molecular weight | 465.71 |
| Molecular formula | C18H17Cl3F2N4O2 |
| CAS | 1047635-80-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800. |