| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Hexokinase II VDAC binding domain peptide targets hexokinase 2 (HXK2) by competitively binding to the HXK2‑VDAC interaction site on the mitochondrial outer membrane. In cancer cells, HK2 is overexpressed and binds to VDAC, promoting glycolysis and suppressing apoptosis. By disrupting this interaction, the peptide inhibits HK2 translocation to mitochondria, leading to reduced glycolytic flux, decreased ATP production, and enhanced mitochondrial outer membrane permeability, which can promote apoptosis. The peptide also inhibits axon outgrowth mediated by neurotrophic factors.
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| ln Vitro |
In vitro, the peptide inhibits the mitochondrial localization of hexokinase 2 (HXK2). It disrupts the interaction between HK2 and VDAC, reducing the amount of HK2 bound to the mitochondrial outer membrane. This leads to diminished glycolytic activity and can induce apoptosis in cancer cells. The peptide also inhibits neurotrophic factor‑directed axon outgrowth. No specific IC₅0 values are reported. The peptide is cell‑permeable, enabling direct addition to cell culture media without transfection reagents.
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| ln Vivo |
No specific in vivo activity data for Hexokinase II VDAC binding domain peptide are reported in the search results. As a cell‑permeable peptide targeting the HK2‑VDAC interaction, it has potential for evaluation in tumor xenograft models (e.g., glioblastoma, breast cancer, lung cancer). The peptide could be administered intravenously or intratumorally to assess its effects on tumor growth, HK2 localization, and apoptosis. However, no such data are provided.
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| Enzyme Assay |
No enzyme/receptor binding assays are applicable, as the peptide functions by protein‑protein interaction inhibition. The binding of the peptide to VDAC or HK2 can be measured by surface plasmon resonance (SPR) using purified VDAC protein immobilized on a sensor chip. The peptide is flowed over the chip, and the binding affinity (KD) is calculated. Alternatively, co‑immunoprecipitation assays using HK2 and VDAC antibodies can assess disruption of the HK2‑VDAC interaction in cells. No specific affinity data are reported.
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| Cell Assay |
For cellular assays, cancer cell lines (e.g., HeLa, U87MG, A549, MCF‑7) or endothelial cells are seeded in 6‑ or 96‑well plates. The cell‑permeable Hexokinase II VDAC binding domain peptide is added directly to the culture medium at concentrations of 1‑50 microM for 6‑48 hours. Mitochondrial HK2 localization is assessed by subcellular fractionation followed by Western blot for HK2 in mitochondrial fractions. Glycolysis is assessed by measuring lactate production and glucose consumption. Apoptosis is measured by Annexin V/PI staining and caspase‑3/7 activity. ATP levels are measured using a luminescence‑based kit. The inhibition of axon outgrowth is assessed in primary neuronal cultures.
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| Animal Protocol |
No animal experiments for Hexokinase II VDAC binding domain peptide are described in the search results. For in vivo evaluation of antitumor activity, 6‑8‑week‑old female BALB/c nude mice bearing subcutaneous xenografts of cancer cell lines (e.g., U87MG glioblastoma, A549 lung cancer) would be used. The cell‑permeable peptide would be administered intravenously (IV) at doses of 5‑20 mg/kg daily for 2‑4 weeks. Tumor volumes would be measured twice weekly. At the study endpoint, tumors would be collected for analysis of HK2 localization (Western blot), glycolytic markers (lactate, pyruvate), and apoptosis (TUNEL, cleaved caspase‑3). No such data are provided.
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| ADME/Pharmacokinetics |
The peptide (sequence: RQIKIWFQNRRMKWKKMIASHLLAYFFTELN-NH2, C1₈₈H2₉1N₅3O40S2, MW = 3997.78) is a white to off‑white solid powder. For storage, the powder should be kept at -80degC for up to 2 years, or at -20degC for up to 1 year, sealed and protected from moisture. For in vitro use, stock solutions in DMSO (5 mg/mL, 1.25 mM) can be prepared with ultrasonic assistance. Stock solutions in DMSO can be stored at -80degC for up to 6 months or at -20degC for up to 1 month. The peptide is cell‑permeable, eliminating the need for transfection reagents. Purity is typically ≥98% (HPLC).
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| Toxicity/Toxicokinetics |
No specific toxicity data for Hexokinase II VDAC binding domain peptide are reported. As a research‑grade peptide, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling peptides should be followed, including the use of gloves, lab coat, and safety goggles. The peptide has been studied in cell culture at concentrations up to 50 microM without reported cytotoxicity, but no LD₅0 or formal toxicology studies are available.
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| References | |
| Additional Infomation |
Hexokinase II VDAC binding domain peptide (Hxk2VBD peptide) is a cell‑permeable synthetic peptide that disrupts the binding of hexokinase 2 (HK2) to the voltage‑dependent anion channel (VDAC) on the mitochondrial outer membrane. HK2 is a key regulator of the Warburg effect (aerobic glycolysis) in cancer cells, and its interaction with VDAC promotes glycolysis and inhibits apoptosis. Targeting the HK2‑VDAC interaction is a promising strategy for cancer therapy. The peptide has been used in research on cancer metabolism, apoptosis, and diabetic endothelial dysfunction. The cell‑permeable sequence (RQIKIWFQNRRMKWKK) is the penetratin sequence derived from the Drosophila Antennapedia homeodomain, enabling efficient cellular uptake. The compound is for research use only and has not entered clinical trials or received regulatory approval.
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| Molecular Formula |
C188H291N53O40S2
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| Molecular Weight |
3997.78
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| Appearance |
White to off-white solid powder
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| Synonyms |
Hxk2VBD peptide, cell-permeable
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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, avoid exposure to moisture. |
| 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) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (0.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (5.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (0.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (5.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 0.5 mg/mL (0.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (5.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2501 mL | 1.2507 mL | 2.5014 mL | |
| 5 mM | 0.0500 mL | 0.2501 mL | 0.5003 mL | |
| 10 mM | 0.0250 mL | 0.1251 mL | 0.2501 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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