MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed.

Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival as well as angiogenesis. MK 2206 is an orally active, allosteric Akt inhibitor that is equally potent toward purified human recombinant Akt1 and Akt2 (IC50s = 5 and 12 nM, respectively) and approximately 5-fold less potent against human Akt3 (IC50 = 65 nM). In combination with other anticancer agents including topoisomerase inhibitors, antimetabolites, antimicrotubule agents, DNA cross-linkers or growth factor inhibitors, MK 2206 has been shown to synergistically inhibit cell proliferation of human cancer cell lines. At 5 μM, MK 2206 significantly enhances apoptosis in hematopoietic cells treated with chemotherapeutics.

3CAI

A-443654

A-674563

Afuresertib

AKT inhibitor VIII

AT13148

AT7867

AZD5363

CCT128930

Deguelin

GDC-0068