|3CAI AKT inhibitor|
Sample solution is provided at 25 µL, 10mM.
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Quality Control & MSDS
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|Cas No.||28755-03-5||SDF||Download SDF|
|Solubility||≥6.8mg/mL in DMSO||Storage||Store at -20°C|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
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 . 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 .
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. Kim DJ, Reddy K, Kim MO, Li Y, Nadas J, Cho YY, et al. (3-Chloroacetyl)-indole, a novel allosteric AKT inhibitor, suppresses colon cancer growth in vitro and in vivo. Cancer Prev Res (Phila). 2011;4(11):1842-51.