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BHPI

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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.

BHPI

BHPI

😃Good
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.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$896-8 weeks6-8 weeks
50 mg$7556-8 weeks6-8 weeks
100 mg$1,2406-8 weeks6-8 weeks
1 mL x 10 mM (in DMSO)$1976-8 weeks6-8 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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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
Relative Density.1.320 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 150 mg/mL (452.68 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 4 mg/mL (12.07 mM), Sonication is recommeded.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Keywords

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