Akt Inhibitor VIII, Isozyme-Selective, 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, Akti-1/2
A cell-permeable and reversible 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. A 10 mM (1 mg/181 µl) solution of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (Cat. No. 124017) in DMSO is also available.
产品信息
Form Yellow solid
Primary Target Akt1, Akt2, Akt3
Primary Target IC50 58 nM, 210 nM, 2.12 µM respectively
Secondary target PKA, PKC, SGK (all with IC50 = 50 µM)
Molar mass 551.6
Protect from Light 是的
Packaged under inert gas 是的
Cell permeable 是的
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C34H29N7O
CAS number 612847-09-3
商店和运输信息
Storage +2°C to +8°C
Ship Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling |