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BHPI
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。
BHPI图片
CAS NO:56632-39-4
规格:98%
分子量:331.36
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议

产品介绍
BHPI是核内受体ER_alpha_抑制剂,可抑制癌细胞蛋白合成和活化未折叠蛋白反应(UPR)。
CAS:56632-39-4
分子式:C21H17NO3
分子量:331.36
纯度:98%
存储:Store at -20°C

Background:

BHPI is a potent inhibitor of nuclear estrogen-ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.IC50 value:Target: ERα inhibitorBHPI is effective because it elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis. BHPI distorts a newly described action of estrogen-ERα: mild and transient UPR activation. In contrast, BHPI elicits massive and sustained UPR activation, converting the UPR from protective to toxic. In ERα(+) cancer cells, BHPI rapidly hyperactivates plasma membrane PLCγ, generating inositol 1,4,5-triphosphate (IP3), which opens EnR IP3R calcium channels, rapidly depleting EnR Ca(2+) stores.




[1]. Andruska ND, et al. Estrogen receptor α inhibitor activates the unfolded protein response, blocks protein synthesis, and induces tumor regression. Proc Natl Acad Sci U S A. 2015 Apr 14;112(15):4737-42.