您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > 3CAI
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
3CAI
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
3CAI图片
CAS NO:28755-03-5
规格:98%
分子量:193.63
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
AKT inhibitor
CAS:28755-03-5
分子式:C10H8ClNO
分子量:193.63
纯度:98%
存储:Store at -20°C

Background:

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].


Reference:
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.