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| Targets |
BH3 hydrochloride targets the Bcl-2 family of proteins, which are key regulators of the intrinsic (mitochondrial) apoptotic pathway. It binds to the hydrophobic groove of anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1, and A-1) via their BH3 domain, neutralizing their function. It also directly activates the pro-apoptotic effectors Bax and Bak, promoting their oligomerization and insertion into the mitochondrial outer membrane, leading to cytochrome c release and caspase activation. This dual mechanism makes it a potent apoptosis inducer.
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| ln Vitro |
In vitro, BH3 hydrochloride directly interacts with Bcl-2 family proteins to induce apoptosis. It effectively neutralizes anti-apoptotic proteins and activates pro-apoptotic effectors. The peptide has been shown to induce cell death in a concentration-dependent manner in various cancer cell lines. While specific EC50 values for cell viability inhibition are not detailed in the available product literature, the BH3 peptide is widely recognized as a standard tool for studying apoptosis and for validating targets in the Bcl-2 pathway.
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| ln Vivo |
In vivo activity data for BH3 hydrochloride have not been extensively reported in standard product literature, as the compound is primarily used as a research tool for in vitro cell death studies. However, due to its ability to cross the blood-brain barrier, it has potential for central nervous system applications. Detailed in vivo efficacy, toxicity, and pharmacokinetic studies would be required to characterize its therapeutic potential.
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| Enzyme Assay |
Binding assays for BH3 hydrochloride are performed to assess its interaction with Bcl-2 family proteins. Typically, a fluorescence polarization (FP) assay is used, where a fluorescently labeled BH3 peptide (e.g., FITC-BIM BH3) is incubated with purified recombinant anti-apoptotic proteins (Bcl-2, Bcl-XL, Mcl-1). BH3 hydrochloride competes for binding to these proteins, leading to a decrease in fluorescence polarization. IC50 or Ki values are calculated from competition curves. Alternatively, surface plasmon resonance (SPR) can be used to measure binding affinity.
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| Cell Assay |
Cellular assays for BH3 hydrochloride are conducted using various cancer cell lines (e.g., HeLa, MCF-7, Jurkat). Cells are treated with varying concentrations of BH3 hydrochloride (typically 10-100 microM) for 24-48 hours. Apoptosis is assessed by multiple methods: flow cytometry using Annexin V/PI staining to detect phosphatidylserine externalization; measurement of caspase-3/7 activity using fluorogenic substrates; detection of PARP cleavage by immunoblotting; and assessment of mitochondrial membrane potential (deltaΨm) using dyes like JC-1 or TMRM. Cell viability is measured by MTT or CellTiter-Glo assays.
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| Animal Protocol |
Detailed in vivo animal protocols for BH3 hydrochloride are not described in standard product literature. As the compound is a research tool primarily for in vitro studies, animal model data are not typically provided. However, for potential in vivo applications, administration routes could include intravenous or intracerebroventricular injection due to its reported ability to cross the blood-brain barrier. Standard xenograft tumor models could be used to assess efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for BH3 hydrochloride are not extensively detailed in available literature. The peptide is reported to cross the blood-brain barrier, indicating some degree of CNS penetration. However, specific PK parameters such as half-life, clearance, volume of distribution, and bioavailability have not been characterized in standard product documentation. Comprehensive ADME studies would be required for therapeutic development.
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| Toxicity/Toxicokinetics |
Toxicological data for BH3 hydrochloride are not extensively reported in standard product literature. As a BH3 domain peptide that induces apoptosis, potential toxicities may include off-target effects on healthy cells and systemic cytotoxicity. Standard preclinical safety assessments would be required for therapeutic development. For research use, standard peptide handling precautions, including the use of appropriate personal protective equipment, should be followed.
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| References |
[1]. Guang Yang, et al. Modulating Protein-Protein Interactions In Vivo via Peptide-Lanthanide-Derived Nanoparticles for Hazard-Free Cancer Therapy. J Biomed Nanotechnol. 2019 Sep 1;15(9):1937-1947.
[2]. Shatrunajay Shukla, et al. BH3-only Protein BIM: An Emerging Target in Chemotherapy. Eur J Cell Biol. 2017 Dec;96(8):728-738. |
| Additional Infomation |
BH3 hydrochloride is a synthetic peptide with the sequence Ile-Trp-Ile-Ala-Gln-Glu-Leu-Arg-Arg-Ile-Gly-Asp-Glu-Phe-Asn-Ala-Tyr-Tyr-Ala-Arg-Arg (short form IWIAQELRRIGDEFNAYYARR). It has a molecular weight of 2677.45 and the molecular formula C120H183ClN36O32. The peptide is typically stored as a powder at -20degC for up to 3 years. It is used extensively in apoptosis research to study the intrinsic mitochondrial pathway and to develop targeted therapies that restore apoptotic sensitivity in cancer cells. It is for research use only and not for human therapy.
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| Molecular Formula |
C120H183CLN36O32
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| Molecular Weight |
2677.45
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3735 mL | 1.8674 mL | 3.7349 mL | |
| 5 mM | 0.0747 mL | 0.3735 mL | 0.7470 mL | |
| 10 mM | 0.0373 mL | 0.1867 mL | 0.3735 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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