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. 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. 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.
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BHPI
CAS number：56632-39-4 molecular formula：C21H17NO3
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| Chinese alias | 1,3-二氢-3,3-双(4-羟苯基)-7-甲基-2H-吲哚-2-一 | 3,3-双（4-羟基苯基）-7-甲基二氢-2-酮 | ||
| English alias | SMR000194821 | BHPI | HY-12825 | A913373 | FABLAHMQSQFDHR-UHFFFAOYSA-N | MLS000573319 | cid_3860640 | 3,3-bis(4-hydroxyphenyl)-7-methyl-1,3-dihydro-2H-indol-2-one | 3,3-bis(4-hydroxyphenyl)-7-methyl-oxindole | AS-16880 | Cambridge id 6373538 | HMS2153B10 | ||
| CAS number | 56632-39-4 | molecular formula | C21H17NO3 |
| molecular weight | 331.36 g/mol | Exact mass | ≥98% |
| PSA | 69.600 Ų | logp | 3.600 |
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