BHPI [56632-39-4]

TargetMol Chemicals

BHPI [56632-39-4]

14

56632-39-4

Chemical

Research Use Only

BHPI

C21H17NO3

331.36

BHPI is a potent ERalpha inhibitor that blocks nuclear estrogen-ERalpha-regulated gene expression effectively. It triggers sustained ERalpha-dependent activation of the endoplasmic reticulum (EnR) stress sensor, notably the unfolded protein response (UPR), and consistently inhibits protein synthesis. With an IC50 value targeting ERalpha, BHPIs mechanism involves the rapid hyperactivation of PLCgamma on the plasma membrane in ERalpha(+) cancer cells, which produces inositol 1,4,5-triphosphate (IP3). This, in turn, opens EnR IP3R calcium channels, leading to a rapid depletion of EnR Ca(2+) stores. SIGNIFICANTLY, BHPI alters estrogen-ERalphas usual effect of causing mild and transient UPR activation by inducing a severe and prolonged UPR activation, transforming the UPR from a protective to a toxic response.

3 years

Cc1cccc2c1NC(=O)C2(c1ccc(O)cc1)c1ccc(O)cc1

-20°C

12352200