BH3I-1
Based on 1 Customer Validation
BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 300817-68-9
- Formula: C15H14BrNO3S2
- Molecular Weight:400.31
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Bcl-2 |
Bcl-xL |
Bak |
Bim |
p53/mDM2 5.3 μM (Kd) |
BH3I-1, while inhibiting its reported target Bcl-2/Bim and Bcl-xL/Bim, shows significant inhibition of both the p53/hDM2 and p300/Hif-1α interactions. This surprising promiscuity, displays by a well studied compound leads to further interrogate the p53/hDM2 interaction utilizing a standard fluorescence polarization (FP) assay with purified protein. The results from the FP assay validates the split-luciferase screen and demonstrates that BH3I-1 has a Kd=5.3 μM against the p53/mDM2 pair, which is comparable to its low micromolar potency reported for the BH3 family of receptors[2].
BH3I-1 inhibits interaction between the BH3 domain and Bcl-xL. NMR analyses reveal that BH3I-1 targets the BH3-binding pocket of Bcl-xL with a Ki of 7.8±0.9 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 300817-68-9
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Appearance Solid
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Molecular Weight 400.31
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Formula C15H14BrNO3S2
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Color Light yellow to yellow
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SMILES
O=C(O)C(C(C)C)N(C/1=O)C(SC1=C\C2=CC=C(Br)C=C2)=S
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Synonyms
BHI1
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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 : 100 mg/mL (249.81 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: ≥ 2.5 mg/mL (6.25 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.25 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Protocol
Jurkat cells overexpressing Bcl-xL, FL 5.12 and FL 5.12/Bcl-xL cells (5×104 cells per well) are seeded into white 96-well plates and treated with various concentrations of the compounds (e.g., BH3I-1; 30 μM and 90 μM)for 48 h. For zVAD-FMK protection experiments, cells are preincubated with 100 μM zVAD-FMK for 1 h before the addition of chemicals. Cell viability is determined with an MTS assay with a Victor plate reader. For PI staining experiments, cells are grown in 24-well plates and then incubated with 2 μg/mL PI. Cell death is determined by FACS analysis in a FACSCalibur machine[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang L, et al. Development of dimeric modulators for anti-apoptotic Bcl-2 proteins. Bioorg Med Chem Lett. 2008 Jan 1;18(1):236-40. [Content Brief]
[2]. Degterev A, et al. Identification of small-molecule inhibitors of interaction between the BH3 domain and Bcl-xL. Nat Cell Biol. 2001 Feb;3(2):173-82. [Content Brief]
[3]. Porter JR, et al. Profiling small molecule inhibitors against helix-receptor interactions: the Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2. Chem Commun (Camb). 2010 Nov 14;46(42):8020-2. [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 | 2.4981 mL | 12.4903 mL | 24.9806 mL | 62.4516 mL |
| 5 mM | 0.4996 mL | 2.4981 mL | 4.9961 mL | 12.4903 mL | |
| 10 mM | 0.2498 mL | 1.2490 mL | 2.4981 mL | 6.2452 mL | |
| 15 mM | 0.1665 mL | 0.8327 mL | 1.6654 mL | 4.1634 mL | |
| 20 mM | 0.1249 mL | 0.6245 mL | 1.2490 mL | 3.1226 mL | |
| 25 mM | 0.0999 mL | 0.4996 mL | 0.9992 mL | 2.4981 mL | |
| 30 mM | 0.0833 mL | 0.4163 mL | 0.8327 mL | 2.0817 mL | |
| 40 mM | 0.0625 mL | 0.3123 mL | 0.6245 mL | 1.5613 mL | |
| 50 mM | 0.0500 mL | 0.2498 mL | 0.4996 mL | 1.2490 mL | |
| 60 mM | 0.0416 mL | 0.2082 mL | 0.4163 mL | 1.0409 mL | |
| 80 mM | 0.0312 mL | 0.1561 mL | 0.3123 mL | 0.7806 mL | |
| 100 mM | 0.0250 mL | 0.1249 mL | 0.2498 mL | 0.6245 mL |
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