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BHPI Catalog No.GC33011

Size Price Stock Qty
10mM*1mLinDMSO
$218.00
In stock
2mg
$119.00
In stock
5mg
$166.00
In stock
10mg
$239.00
In stock
50mg
$1,011.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 56632-39-4 SDF Download SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES O=C1NC2=C(C=CC=C2C)C1(C3=CC=C(O)C=C3)C4=CC=C(O)C=C4
Formula C21H17NO3 M.Wt 331.36
Solubility DMSO : ≥ 150 mg/mL (452.68 mM) Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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Background

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.

[1]. Andruska ND, et al. Estrogen receptor α inhibitor activates the unfolded protein response, blocks protein synthesis, and induces tumor regression. Proc Natl Acad Sci U S A. 2015 Apr 14;112(15):4737-42.