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BHPI

Name: BHPI
Brand: TargetMol
SKU: T14553
Rating: 4.5 (1 reviews)

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Catalog No. T14553Cas No. 56632-39-4

BHPI is a potent inhibitor of nuclear estrogen receptor ERα–regulated gene expression that induces sustained ERα-dependent activation of the endoplasmic reticulum stress sensor and unfolded protein response, leading to persistent inhibition of protein synthesis, and in ERα-positive cancer cells it hyperactivates plasma membrane PLCγ to generate IP3, deplete ER calcium stores via IP3R channels, and convert the normally protective UPR into a toxic response, making BHPI a valuable probe for estrogen signaling and ER stress–based cancer research.

BHPI

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Catalog No. T14553Cas No. 56632-39-4

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$89	6-8 weeks	6-8 weeks
50 mg	$755	6-8 weeks	6-8 weeks
100 mg	$1,240	6-8 weeks	6-8 weeks
1 mL x 10 mM (in DMSO)	$197	6-8 weeks	6-8 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	BHPI is a potent inhibitor of nuclear estrogen receptor ERα–regulated gene expression that induces sustained ERα-dependent activation of the endoplasmic reticulum stress sensor and unfolded protein response, leading to persistent inhibition of protein synthesis, and in ERα-positive cancer cells it hyperactivates plasma membrane PLCγ to generate IP3, deplete ER calcium stores via IP3R channels, and convert the normally protective UPR into a toxic response, making BHPI a valuable probe for estrogen signaling and ER stress–based cancer research.
In vitro	In cellular assays, BHPI inhibited the proliferation of ERα-positive breast, endometrial, and ovarian cancer cells at concentrations between 100 and 1000 nM. It maintained activity (25 nM) in antiestrogen-resistant cell lines harboring ERα mutations (Y537S, D538G) by triggering UPR hyperactivation, protein synthesis inhibition, and apoptosis [1].
In vivo	In MCF-7 breast cancer xenograft models, intraperitoneal (i.p.) administration of BHPI (10-15 mg/kg) resulted in tumor regression. When administered daily for 10 days or every other day, tumor regression was observed in 48 out of 52 treated tumors. This effect is attributed to the sustained activation of UPR stress within the tumor tissue [1].

Chemical Properties

Molecular Weight	331.36
Formula	C₂₁H₁₇NO₃
Cas No.	56632-39-4
Smiles	O=C1NC=2C(=CC=CC2C1(C3=CC=C(O)C=C3)C4=CC=C(O)C=C4)C
Relative Density.	1.320 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (301.79 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 4 mg/mL (12.07 mM), Sonication is recommended.

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

	1mg	5mg	10mg	50mg
1 mM	3.0179 mL	15.0893 mL	30.1787 mL	150.8933 mL
5 mM	0.6036 mL	3.0179 mL	6.0357 mL	30.1787 mL
10 mM	0.3018 mL	1.5089 mL	3.0179 mL	15.0893 mL
20 mM	0.1509 mL	0.7545 mL	1.5089 mL	7.5447 mL
50 mM	0.0604 mL	0.3018 mL	0.6036 mL	3.0179 mL
100 mM	0.0302 mL	0.1509 mL	0.3018 mL	1.5089 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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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BHPI

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