BHPI - ≥98%, high purity , CAS No.56632-39-4

Item Number

B288704

• Synonyms: BHPI|56632-39-4|3,3-bis(4-hydroxyphenyl)-7-methyl-1,3-dihydro-2H-indol-2-one|MLS000573319|3,3-bis(4-hydroxyphenyl)-7-methyl-1H-indol-2-one|SMR000194821|1,3-Dihydro-3,3-bis(4-hydroxyphenyl)-7-methyl-2H-indol-2-one|3,3-bis-(4-hydroxy-phenyl)-7-methyl-1,3-di
• Specifications & Purity: ≥98%
• Biochemical and Physiological Mechanisms: Estrogen receptor (ER) α inhibitor. Inhibits proliferation of drug-resistant ERα-positive breast and ovarian cancer cells. Induces sustained activation of the unfolded protein response. Activein vivo.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads

Product 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 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.