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. Specification: ≥98% Molecular Formula: C21H17NO3 Molecular Weight: 331.36 PubChem CID: 3860640 Isomeric SMILES: CC1=C2C(=CC=C1)C(C(=O)N2)(C3=CC=C(C=C3)O)C4=CC=C(C=C4)O Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/B288704-SCI_1f0751ec015975cb9399654cd9ecb6df.pdf
- UPC:
- 12352200
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- B288704-1mg
- CAS:
- 56632-39-4
- Product Size:
- 1mg
