应用 |
A highly selective pan-Akt inhibitor activated by the pleckstrin homology domain |
产品介绍 |
MK-2206 2HCl是一种高度选择性的Akt1/2/3抑制剂,IC50分别为8 nM/12 nM/65 nM;对250种其他蛋白激酶没有抑制活性。 |
备注 |
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. Phase 2. |
生化机理 |
MK-2206 2HCl is a highly selective inhibitor of Akt1, Akt2, and Akt3 with IC50 values of 8 nM, 12 nM and 65 nM, respectively. MK-2206 is an allosteric inhibitor and is activated by the pleckstrin homology domain. MK-2206 inhibits auto-phosphorylation of both Akt T308 and S473. MK-2206 also prevents Akt-mediated phosphorylation of downstream signaling molecules, including TSC2, PRAS40 and ribosomal S6 proteins. MK-2206 also shows synergistic responses in combination with cytotoxic agents such as erlotinib or lapatinib in lung NCI-H460 or ovarian A2780 tumor cells |
别名 |
MK2206; 8-[4-(1-氨基环丁基)苯基]-9-苯基-1,2,4-三唑并[3,4-f][1,6]萘啶-3(2H)-酮二盐酸盐;MK2206;MK-2206 dihydrochloride;8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride |