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BHPI
CAS No. : 56632-39-4
Biological Activity：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 inhibitor
BHPI 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.
Research Area：Cancer
Targets：Estrogen Receptor/ERR
Related Screening Libraries:Bioactive Compound Library Plus;Anti-Cancer Compound Library;Anti-Breast Cancer Compound Library;Nuclear Receptor Compound Library;
Related Small Molecules:DS20362725;LSD1/ER-IN-1;Giredestrant;Avobenzone;Estriol-d3;Chrysin;ERRγ Inverse Agonist 1;(R)-DPN;MPP hydrochloride;GPR30 agonist-1;Diethylstilbestrol;Endoxifen;Glicoricone;ERB-196;Dihydroresveratrol;FLTX1;(Rac)-Hexestrol-d6
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