Akti-1/2
1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable quinoxaline compound that potently and selectively inhibits Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition appears to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 µM. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo. Purity: ≥95% by HPLC. CAS 612847-09-3. Ref.: Logie, L., et al. 2007. Diabetes 56, 228. Barnett, S.F., et al. 2005. Biochem. J. 385, 399. DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther. 4, 271. Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett. 15, 905. Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett. 15, 761. |
