VBIT-4
Based on 20 publication(s) in Google Scholar
VBIT-4 is an inhibitor of voltage-dependent anion channel 1 (VDAC1) oligomerization with a binding affinity (Kd) of 17 μM. VBIT-4, as an apoptosis inhibitor, can be used for therapeutic purposes in apoptosis-associated disorders, such as neurodegenerative and cardiovascular diseases.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.29%
- CAS 番号: 2086257-77-2
- 分子式: C21H23ClF3N3O3
- 分子量:457.87
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Membrane Transporter/Ion Channel Compound Library
HY-L011
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Anti-Cardiovascular Disease Compound Library
HY-L046
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Highly Selective Inhibitors Library
HY-L158
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Ion Channel Compound Library
HY-L166
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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
MedChemExpress（MCE）の使用を引用している文献 VBIT-4
More- Cell. 2020 Oct 29;183(3):636-649.e18. [Abstract]
- Immunity. 2022 Aug 9;55(8):1370-1385.e8. [Abstract]
- Autophagy. 2021 Nov;17(11):3444-3460. [Abstract]
- Nat Commun. 2024 Aug 6;15(1):6685. [Abstract]
- Nat Commun. 2023 Feb 16;14(1):872. [Abstract]
- Nucleic Acids Res. 2024 Aug 1:gkae654. [Abstract]
- Alzheimers Dement. 2026 Apr;22(4):e71423. [Abstract]
- Environ Sci Technol. 2025 Aug 5;59(30):15705-15719. [Abstract]
- Cell Commun Signal. 2025 Mar 20;23(1):146. [Abstract]
- Cell Commun Signal. 2024 Nov 26;22(1):566. [Abstract]
- Free Radic Biol Med. 2025 Sep 11:S0891-5849(25)00975-X. [Abstract]
- Cell Rep. 2026 Jun 9;45(6):117515. [Abstract]
- Cell Rep. 2025 Dec 10;44(12):116673. [Abstract]
- Am J Physiol Cell Physiol. 2025 Sep 12. [Abstract]
- Sci Rep. 2023 Nov 17;13(1):20126. [Abstract]
- J Immunol. 2021 Apr 15;206(8):1890-1900. [Abstract]
- bioRxiv. 2026 May 29:2026.05.26.727520. [Abstract]
- SSRN. 2025 Dec 15.
- bioRxiv. 2025 Oct 30:2025.10.29.685328. [Abstract]
- University of Alberta. 2025.
Customer Validation & Images
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Cell Imaging/Staining
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Cell Imaging/Staining
生物活性
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VDAC1 |
VBIT-4 targets the mitochondrial protein VDAC1, inhibiting apoptosis and protecting against mitochondria dysfunction. VBIT-4 (0.1-10 μM) inhibits VDAC1 oligomerization, Cyto c release from mitochondria and apoptosis in HEK-293 cells with IC50s of 1.9±0.08 μM, 1.8±0.24 μM, and 2.9±0.12 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK-293 cells
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Concentration:0.1, 1, and 10 μM
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Incubation Time:
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Result:Inhibited apoptosis with an IC50 of 2.9±0.12 μM.
化学情報
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CAS 番号 2086257-77-2
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性状 Solid
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分子量 457.87
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分子式 C21H23ClF3N3O3
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=C(Cl)C=C1)CC(CO)N2CCN(C3=CC=C(OC(F)(F)F)C=C3)CC2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (20)
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Journal Impact Factor
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Most Recent
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Cell
2020 Oct 29;183(3):636-649.e18. PMID: 33031745 -
Immunity
Oxidized DNA fragments exit mitochondria via mPTP- and VDAC-dependent channels to activate NLRP3 inflammasome and interferon signaling. [Abstract]2022 Aug 9;55(8):1370-1385.e8. PMID: 35835107
VBIT-4 purchased from MedChemExpress. Usage Cited in: Immunity. 2022 Aug 9;55(8):1370-1385.e8. [Abstract]
VDAC oligomerization in BMDMs that were pretreated with or without VBIT-4 (10 μM, 16 h), primed with or without LPS (200 ng/mL, 4 h), and stimulated with or without ATP (4 mM, 1 h) was determined by IB analysis of cell lysates incubated with the cross-linking agent EGS (200 μM, 40 min, 30°C) to stabilize VDAC oligomers.
VBIT-4 purchased from MedChemExpress. Usage Cited in: Immunity. 2022 Aug 9;55(8):1370-1385.e8. [Abstract]
Relative calcein fluorescence in BMDM pretreated with or without CsA (1 μM, 16 h) or VBIT-4 (10 μM, 16 h), followed by priming with or without LPS (200 ng/mL, 4 h) and stimulation with or without ATP (4 mM, 1 h). The calcein-quenching assay measured mPTP opening.
VBIT-4 purchased from MedChemExpress. Usage Cited in: Immunity. 2022 Aug 9;55(8):1370-1385.e8. [Abstract]
Representative fluorescent microscopy images of BMDM, pretreated ± VBIT-4 (10 μM, 16 h), primed ± LPS (200 ng/mL, 4 h), stimulated ± ATP (4 mM, 1 h) or nigericin (10 μM, 1 h), and co-stained for Atp5b and ASC were shown. Arrows indicated ASC specks. Scale bar, 5 μm.
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Autophagy
Autophagy restricts mitochondrial DNA damage-induced release of ENDOG (endonuclease G) to regulate genome stability. [Abstract]2021 Nov;17(11):3444-3460. PMID: 33465003 -
Nat Commun
2024 Aug 6;15(1):6685. PMID: 39107301 -
Nat Commun
Oxidized mitochondrial DNA induces gasdermin D oligomerization in systemic lupus erythematosus. [Abstract]2023 Feb 16;14(1):872. PMID: 36797275
VBIT-4 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 16;14(1):872. [Abstract]
Both IMT1 (10 μM; 24 h) and CsA (1 μM; 2 h) with VBIT-4 (10 μM; 2 h) inhibits GSDMD oligomerization in PBMCs.
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Nucleic Acids Res
Loss of the DNA repair protein, polynucleotide kinase/phosphatase, activates the type 1 interferon response independent of ionizing radiation. [Abstract]2024 Aug 1:gkae654. PMID: 39087523 -
Alzheimers Dement
Endothelial NAD+ depletion drives vascular senescence and neuroinflammation via mtDNA-cGAS/STING-CD38 signaling in Alzheimer's disease. [Abstract]2026 Apr;22(4):e71423. PMID: 42033099 -
Environ Sci Technol
Chronic Dietary Exposure to Environmental Levels of Glyphosate Increases the Risk of Reproductive Dysfunction in Male Mice. [Abstract]2025 Aug 5;59(30):15705-15719. PMID: 40698942 -
Cell Commun Signal
Induction of LY6E regulates interleukin-1β production, potentially contributing to the immunopathogenesis of systemic lupus erythematosus. [Abstract]2025 Mar 20;23(1):146. PMID: 40114200
VBIT-4 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Mar 20;23(1):146. [Abstract]
BMDMs were treated with different inhibitors targeting LY6E-regulated and IFN-α- and IC-activated downstream signaling pathways, including 5 µM CsA or 10 µM VBIT-4 for 2 h, followed by stimulation with IFN-α or ICs for 24 h.
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Cell Commun Signal
Cadmium exposure triggers alveolar epithelial cell pyroptosis by inducing mitochondrial oxidative stress and activating the cGAS-STING pathway. [Abstract]2024 Nov 26;22(1):566. PMID: 39587603 -
Free Radic Biol Med
VDAC1 Oligomerization-Mediated mtDNA Release under Sublethal Oxidative Stress: A Novel Inflammatory Mechanism in Vitiligo. [Abstract]2025 Sep 11:S0891-5849(25)00975-X. PMID: 40945624 -
Cell Rep
2026 Jun 9;45(6):117515. PMID: 42268710 -
Cell Rep
Aryl hydrocarbon receptor-induced activation of AIM2 inflammasome is mediated by MOMP and MPT: A vital therapeutic pathway for inflammation. [Abstract]2025 Dec 10;44(12):116673. PMID: 41385364 -
Am J Physiol Cell Physiol
Mitochondrial DNA-driven senescence-associated secretory phenotype promotes the development of bronchopulmonary dysplasia. [Abstract]2025 Sep 12. PMID: 40938804 -
Sci Rep
2023 Nov 17;13(1):20126. PMID: 37978268 -
J Immunol
Loss of Mitochondrial Protease CLPP Activates Type I IFN Responses through the Mitochondrial DNA-cGAS-STING Signaling Axis. [Abstract]2021 Apr 15;206(8):1890-1900. PMID: 33731338 -
bioRxiv
2026 May 29:2026.05.26.727520. PMID: 42244578 -
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bioRxiv
Chronic sensing of host-derived lipids is an all-in-one signal that primes and activates NLRP3. [Abstract]2025 Oct 30:2025.10.29.685328. PMID: 41279623 -
溶剤 & 溶解度
DMSO : 125 mg/mL (273.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1 mg/mL (2.18 mM; ultrasonic and adjust pH to 3 with HCl)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 90% Saline
Solubility: 5 mg/mL (10.92 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
純度とドキュメンテーション
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データシート (276 KB)
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取扱説明書 (2659 KB)
参考文献
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 2.1840 mL | 10.9201 mL | 21.8403 mL | 54.6007 mL |
| DMSO | 5 mM | 0.4368 mL | 2.1840 mL | 4.3681 mL | 10.9201 mL |
| 10 mM | 0.2184 mL | 1.0920 mL | 2.1840 mL | 5.4601 mL | |
| 15 mM | 0.1456 mL | 0.7280 mL | 1.4560 mL | 3.6400 mL | |
| 20 mM | 0.1092 mL | 0.5460 mL | 1.0920 mL | 2.7300 mL | |
| 25 mM | 0.0874 mL | 0.4368 mL | 0.8736 mL | 2.1840 mL | |
| 30 mM | 0.0728 mL | 0.3640 mL | 0.7280 mL | 1.8200 mL | |
| 40 mM | 0.0546 mL | 0.2730 mL | 0.5460 mL | 1.3650 mL | |
| 50 mM | 0.0437 mL | 0.2184 mL | 0.4368 mL | 1.0920 mL | |
| 60 mM | 0.0364 mL | 0.1820 mL | 0.3640 mL | 0.9100 mL | |
| 80 mM | 0.0273 mL | 0.1365 mL | 0.2730 mL | 0.6825 mL | |
| 100 mM | 0.0218 mL | 0.1092 mL | 0.2184 mL | 0.5460 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
VBIT-4 関連分類
HY-129122 関連分類
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