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BHPI

BHPI
BHPI is a potent ERα inhibitor that blocks nuclear estrogen–ERα-regulated gene expression effectively. It triggers sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, notably the unfolded protein response (UPR), and consistently inhibits protein synthesis. With an IC50 value targeting ERα, BHPI's mechanism involves the rapid hyperactivation of PLCγ on the plasma membrane in ERα(+) cancer cells, which produces inositol 1,4,5-triphosphate (IP3). This, in turn, opens EnR IP3R calcium channels, leading to a rapid depletion of EnR Ca(2+) stores. SIGNIFICANTLY, BHPI alters estrogen-ERα's usual effect of causing mild and transient UPR activation by inducing a severe and prolonged UPR activation, transforming the UPR from a protective to a toxic response.
Catalog No. T14553Cas No. 56632-39-4

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BHPI

Catalog No. T14553Cas No. 56632-39-4

BHPI is a potent ERα inhibitor that blocks nuclear estrogen–ERα-regulated gene expression effectively. It triggers sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, notably the unfolded protein response (UPR), and consistently inhibits protein synthesis. With an IC50 value targeting ERα, BHPI's mechanism involves the rapid hyperactivation of PLCγ on the plasma membrane in ERα(+) cancer cells, which produces inositol 1,4,5-triphosphate (IP3). This, in turn, opens EnR IP3R calcium channels, leading to a rapid depletion of EnR Ca(2+) stores. SIGNIFICANTLY, BHPI alters estrogen-ERα's usual effect of causing mild and transient UPR activation by inducing a severe and prolonged UPR activation, transforming the UPR from a protective to a toxic response.
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Pack SizePriceAvailabilityQuantity
2 mg$896-8 weeks
50 mg$7556-8 weeks
100 mg$1,2406-8 weeks
1 mL x 10 mM (in DMSO)$1976-8 weeks
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Product Introduction

Bioactivity
Description
BHPI is a potent ERα inhibitor that blocks nuclear estrogen–ERα-regulated gene expression effectively. It triggers sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, notably the unfolded protein response (UPR), and consistently inhibits protein synthesis. With an IC50 value targeting ERα, BHPI's mechanism involves the rapid hyperactivation of PLCγ on the plasma membrane in ERα(+) cancer cells, which produces inositol 1,4,5-triphosphate (IP3). This, in turn, opens EnR IP3R calcium channels, leading to a rapid depletion of EnR Ca(2+) stores. SIGNIFICANTLY, BHPI alters estrogen-ERα's usual effect of causing mild and transient UPR activation by inducing a severe and prolonged UPR activation, transforming the UPR from a protective to a toxic response.
Chemical Properties
Molecular Weight331.36
FormulaC21H17NO3
Cas No.56632-39-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 150 mg/mL (452.68 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.0179 mL15.0893 mL30.1787 mL150.8933 mL
5 mM0.6036 mL3.0179 mL6.0357 mL30.1787 mL
10 mM0.3018 mL1.5089 mL3.0179 mL15.0893 mL
20 mM0.1509 mL0.7545 mL1.5089 mL7.5447 mL
50 mM0.0604 mL0.3018 mL0.6036 mL3.0179 mL
100 mM0.0302 mL0.1509 mL0.3018 mL1.5089 mL

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