tcsc3087 Uprosertib

Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC₅₀ values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

IC50 & Target: IC50: 180 nM (Akt1), 328 nM (Akt2), 38 nM (Akt3)

In Vitro: Uprosertib (GSK2141795) inhibits Akt1/2/3 with the K_d 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 (GSK2141795) 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].