BHPI

MedChem Express

BHPI [56632-39-4]

5

56632-39-4

Research Use Only

98.0

C21H17NO3

331.36

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

O=C1NC2=C(C=CC=C2C)C1(C3=CC=C(O)C=C3)C4=CC=C(O)C=C4

-20°C,2°C to 8°C

12352200