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Target: Akt

IC50: 1 μM

3CAI is a potent allosteric and specific inhibitor of AKT, which directly binds with AKT1 or AKT2 in an ATP noncompetitive manner and shows 60% inhibition of AKT1 kinase activity at 1 μM [1]. The serine/threonine kinase AKT includes three members, AKT1, AKT2, and AKT3. AKT plays a critical role in promoting transformation and chemoresistance through inducing proliferation and inhibiting apoptosis. Therefore, AKT is regarded as a potential target for cancer therapy.

In vitro: 3CAI (1 and 4 μM) significantly inhibited AKT1 kinase activity and decreased expression of AKT direct downstream targets including mTOR and GSK3β, respectively. 3CAI (4 μM) efficiently induced growth inhibition and apoptosis in HCT116 or HCT29 colon cancer cells [1].

In vivo: 3CAI (30 mg/kg, oral administration) significantly suppressed colon cancer growth in an in vivo xenograft mouse model and inhibited the expression of AKT-target protein such as mTOR and GSK3βin HCT116 colon tumor tissues [1].

特别提醒：