| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| 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.
|
|---|---|
| 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.
|
| 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.
|
| 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.
|
| 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.
|
| 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.
|
| 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).
|
| 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.
|
| 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.
|
| Molecular Formula |
C188H291N53O40S2
|
|---|---|
| Molecular Weight |
3997.78
|
| Appearance |
White to off-white solid powder
|
| Synonyms |
Hxk2VBD peptide, cell-permeable
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 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
|
|---|---|
| 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 | 0.2501 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
