56632-39-4
56632-39-4 structure
- Name: BHPI
- Chemical Name: 3,3-bis(4-hydroxyphenyl)-7-methyl-1H-indol-2-one
- CAS Number: 56632-39-4
- Molecular Formula: C21H17NO3
- Molecular Weight: 331.36500
- Catalog: Research Areas Cancer
- Create Date: 2016-07-05 13:35:49
- Modify Date: 2024-01-08 18:25:35
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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.
| Name | 3,3-bis(4-hydroxyphenyl)-7-methyl-1H-indol-2-one |
|---|---|
| Synonyms |
HMS2153B10
7-methyl-oxyphenisatine BHPI |
| Description | 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. |
|---|---|
| Related Catalog | |
| References |
| Molecular Formula | C21H17NO3 |
|---|---|
| Molecular Weight | 331.36500 |
| Exact Mass | 331.12100 |
| PSA | 73.05000 |
| LogP | 3.77780 |
| Storage condition | 2-8℃ |
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56632-39-4 |
| Literature: Uddin, Muhammed K.; Reignier, Serge G.; Coulter, Tom; Montalbetti, Christian; Granaes, Charlotta; Butcher, Steven; Krog-Jensen, Christian; Felding, Jakob Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 10 p. 2854 - 2857 |
