A cell-permeable Akti-1/2- (sc-202048) derived allosteric inhibitor pair (1:1 regioisomeric mixture) with much improved aqueous solubility (10 mg/ml in a pH 7.4 saline) and Akt2 selectivity (IC50 = 805 nM for Akt2, >10 µM for Akt1/3, and >50 µM for PKA/PKC/SGK). The inhibition is PH domain-dependent and non-competitive with ATP.
1. Zhao, Z., Robinson, R.G., Barnett, S.F., Defeo-Jones, D., Jones, R.E., Hartman, G.D., Huber, H.E., Duggan, M.E. and Lindsley, C.W. 2008. Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity. Bioorg. Med. Chem. Lett. 18(1): 49-53. PMID: 18054229