Cat. No.: HY-129122

VBIT-4

20 Cited Publications

Customer Review

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 (K_d) 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.

For research use only. We do not sell to patients.

Purity: 99.29%
CAS No.: 2086257-77-2
Formula: C₂₁H₂₃ClF₃N₃O₃
Molecular Weight:457.87

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

VBIT-4 Chemical Structure

CAS No.: 2086257-77-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (20)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

VDAC1

All VDAC Isoforms :

In Vitro

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.

Apoptosis Analysis^[1]

Cell Line:

HEK-293 cells
Concentration:

0.1, 1, and 10 μM
Incubation Time:
Result:

Inhibited apoptosis with an IC₅₀ of 2.9±0.12 μM.

Chemical Information

CAS No. 2086257-77-2
Appearance Solid
Molecular Weight 457.87
Formula C₂₁H₂₃ClF₃N₃O₃
Color Light yellow to yellow
SMILES

O=C(NC1=CC=C(Cl)C=C1)CC(CO)N2CCN(C3=CC=C(OC(F)(F)F)C=C3)CC2
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (20)

All WBCell Imaging/Staining

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Journal Impact Factor

Cell

TDP-43 Triggers Mitochondrial DNA Release via mPTP to Activate cGAS/STING in ALS. [Abstract]

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.
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

Heterozygous de novo dominant negative mutation of REXO2 results in interferonopathy. [Abstract]

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.
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.
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

STING-OPTN signaling confers cytoprotection through TBK1-dependent mitophagy. [Abstract]

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

USP18 enhances dengue virus replication by regulating mitochondrial DNA release. [Abstract]

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

Cell autonomous inflammation in VEXAS is mediated by cGAS-STING. [Abstract]

2026 May 29:2026.05.26.727520. PMID: 42244578
SSRN

2025 Dec 15.
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
University of Alberta

2025.

Solvent & Solubility

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1840 mL

10.9201 mL

21.8403 mL

5 mM

0.4368 mL

2.1840 mL

4.3681 mL

10 mM

0.2184 mL

1.0920 mL

2.1840 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Saline

Solubility: 5 mg/mL (10.92 mM); Suspended solution; Need ultrasonic

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ben-Hail D, et al. Novel Compounds Targeting the Mitochondrial Protein VDAC1 Inhibit Apoptosis and Protect against Mitochondrial Dysfunction. J Biol Chem. 2016 Nov 25;291(48):24986-25003. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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.

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VBIT-4

Membrane Transporter/Ion Channel Compound Library

Anti-Cardiovascular Disease Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) VBIT-4

All VDAC Isoforms

Biological Activity

Chemical Information

Publications (20)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

VBIT-4

Membrane Transporter/Ion Channel Compound Library

Anti-Cardiovascular Disease Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) VBIT-4

All VDAC Isoforms

Biological Activity

Chemical Information

Publications (20)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

VBIT-4 Related Classifications

HY-129122 Related Classifications