MK-2206 2HCl

Description: MK-2206 dihydrochloride (2HCl) is a novel, potent, orally bioavailable and highly selective allosteric inhibitor of the serine/threonine protein kinase Akt1/2/3 with potential anticancer activity. It inhibits Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; it has no/little inhibitory activities against 250 other protein kinases observed. MK-2206 has potential anticancer activity by inhibiting the phosphorylation of Thr308 and Ser 473 of Akt. MK-2206 suppresses Akt signalling pathway and promoting cancer cell death as a single agent as well as in combination with other chemotherapeutic agents. MK-2206 enhance the sensitivity to through apoptosis and enhance the sensitivity to rapamycin via reactive oxygen species.

References: Mol Cancer Ther. 2010 Jul; 9(7):1956-67; Cancer Res. 2011 Apr 1; 71(7):2654-63.

Related CAS: 1032349-77-1 (HCl); 1032350-13-2 (2HCl); 1032349-93-1 (free base);