BHPI
Based on 1 Customer Validation
BHPI is a nuclear receptor ERα inhibitor. BHPI activates PLCγ and UPR. BHPI has antitumor activity against breast, endometrial, and ovarian cancers.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 56632-39-4
- Formula: C21H17NO3
- Molecular Weight:331.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
All Phospholipase Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hs-578T | IC50 |
34 nM
Compound: BHPI
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Anticancer activity against human Hs-578T cells assessed as cell growth inhibition incubated for 24 hrs
Anticancer activity against human Hs-578T cells assessed as cell growth inhibition incubated for 24 hrs
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[PMID: 35814932] |
| MDA-MB-231 | IC50 |
>3 μM
Compound: 3e
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Antiproliferative activity against human MDA231 cells
Antiproliferative activity against human MDA231 cells
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[PMID: 17368900] |
| MDA-MB-468 | IC50 |
0.027 μM
Compound: 3e
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Antiproliferative activity against human MDA468 cells
Antiproliferative activity against human MDA468 cells
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[PMID: 17368900] |
| T47D | IC50 |
15 nM
Compound: BHPI
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Anticancer activity against human T47D cells assessed as cell proliferation incubated for 4 days by MTS assay
Anticancer activity against human T47D cells assessed as cell proliferation incubated for 4 days by MTS assay
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[PMID: 35814932] |
BHPI (100-1000 nM) completely inhibits proliferation of ERα-positive breast, endometrial, and ovarian cancer cells[1].
BHPI (25 nM; 4 days) completely inhibits cell proliferation in two-dimensional adherent cultures of T47D, ERαY537S-4, and ERαD538G-1 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 56632-39-4
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Appearance Solid
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Molecular Weight 331.36
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Formula C21H17NO3
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Color White to off-white
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SMILES
O=C1NC2=C(C=CC=C2C)C1(C3=CC=C(O)C=C3)C4=CC=C(O)C=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 120 mg/mL (362.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (9.05 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[2]. Mao C, et al. Antiestrogen Resistant Cell Lines Expressing Estrogen Receptor α Mutations Upregulate the Unfolded Protein Response and are Killed by BHPI. Sci Rep. 2016 Oct 7;6:34753. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0179 mL | 15.0893 mL | 30.1787 mL | 75.4466 mL |
| 5 mM | 0.6036 mL | 3.0179 mL | 6.0357 mL | 15.0893 mL | |
| 10 mM | 0.3018 mL | 1.5089 mL | 3.0179 mL | 7.5447 mL | |
| 15 mM | 0.2012 mL | 1.0060 mL | 2.0119 mL | 5.0298 mL | |
| 20 mM | 0.1509 mL | 0.7545 mL | 1.5089 mL | 3.7723 mL | |
| 25 mM | 0.1207 mL | 0.6036 mL | 1.2071 mL | 3.0179 mL | |
| 30 mM | 0.1006 mL | 0.5030 mL | 1.0060 mL | 2.5149 mL | |
| 40 mM | 0.0754 mL | 0.3772 mL | 0.7545 mL | 1.8862 mL | |
| 50 mM | 0.0604 mL | 0.3018 mL | 0.6036 mL | 1.5089 mL | |
| 60 mM | 0.0503 mL | 0.2515 mL | 0.5030 mL | 1.2574 mL | |
| 80 mM | 0.0377 mL | 0.1886 mL | 0.3772 mL | 0.9431 mL | |
| 100 mM | 0.0302 mL | 0.1509 mL | 0.3018 mL | 0.7545 mL |