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API-1 NSC 177223

API-1 NSC 177223 36707-00-3
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产品信息
产品名称:API-1 NSC 177223 纯度:98% min
CAS NO:36707-00-3 溶解度:
分子式:C13H15N5O6 包装:可按客户要求包装
分子量:337.28 贮存:-20℃
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备注说明

API-1 is a potent Akt inhibitor, which induces GSK3-dependent, β-TrCP- and FBXW7-mediated Mcl-1 degradation, resulting in induction of apoptosis . API-1 rapidly and potently reduced the levels of Mcl-1 primarily in API-1-senstive lung cancer cell lines. Ectopic expression of Mcl-1 protected cells from induction of apoptosis by API-1. API-1 treatment decreased the half-life of Mcl-1, whereas inhibition of the proteasome with MG132 rescued Mcl-1 reduction induced by API-1. API-1 decreased Mcl-1 levels accompanied with a rapid increase in Mcl-1 phosphorylation (S159/T163). Moreover, inhibition of GSK3 inhibited Mcl-1 phosphorylation and reduction induced by API-1 and antagonized the effect of API-1 on induction of apoptosis.

参考文献
1: Ren H, Koo J, Guan B, Yue P, Deng X, Chen M, Khuri FR, Sun SY. The E3 ubiquitin ligases β-TrCP and FBXW7 cooperatively mediates GSK3-dependent Mcl-1 degradation induced by the Akt inhibitor API-1, resulting in apoptosis. Mol Cancer. 2013 Nov 22;12:146. doi: 10.1186/1476-4598-12-146. PubMed PMID: 24261825.

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