Home Transmembrane Transporters VDAC inhibitor - IFN inhibitor VBIT-4 For research use only.

VBIT-4

VBIT-4 is a voltage-dependent anion channel (VDAC) oligomerization inhibitor that decreases mitochondrial DNA (mtDNA) release, type I interferon (IFN) signaling, neutrophil extracellular traps, and disease severity in a mouse model of systemic lupus erythematosus.

VBIT-4 Chemical Structure

VBIT-4 Chemical Structure

CAS No. 2086257-77-2

Purity & Quality Control

Products often used together with VBIT-4

VBIT-12

VBIT-4 and VBIT-12 prevent mitochondrial dysfunction and apoptosis in T2D and lupus models by inhibiting VDAC1 oligomerization and correcting protein misdirection to the plasma membrane.

Shoshan-Barmatz V, et al. Biomolecules. 2020 Oct 26;10(11):1485.

BAI1

VBIT-4 rescues the decreased inner mitochondrial membrane (IMM) protein levels after endolysosomal damage in human iPSC-derived macrophages (iPSDM) better than BAI1.

Bussi C, et al. Nat Commun. 2022 Nov 28;13(1):7338.

IFN alpha-IFNAR-IN-1 hydrochloride

VBIT-4 and IFN α-IFNAR-IN-1 with MnCl2 decrease the release of mitochondrial DNA and reduce lipid peroxidation and ROS levels in MC38 cells.

Zhang S, et al. Free Radic Biol Med. 2022 Nov 20;193(Pt 1):202-212.

Z-VAD-FMK

VBIT-4 and ZVAD treatment demonstrate a robust response to anti-CD3 + anti-CD28 stimulation in COVID-A T cells.

Thompson EA, et al. MedRxiv (2020).

VBIT-4 Related Products

Biological Activity

Description VBIT-4 is a voltage-dependent anion channel (VDAC) oligomerization inhibitor that decreases mitochondrial DNA (mtDNA) release, type I interferon (IFN) signaling, neutrophil extracellular traps, and disease severity in a mouse model of systemic lupus erythematosus.
Targets
VDAC [1] mtDNA [1] IFN [1]
In vitro
In vitro

VBIT-4 rapidly inhibits the loss of ATP, which is a consequence of its translocation to the plasma membrane caused by VDAC1 overexpression, in plVdac1-expressing INS-1 cells.[2]
Cell Research Cell lines INS-1 cells transfected with plVdac1
Concentrations 20 μM
Incubation Time 1 h
Method

Effect of VDAC1 antibody (VDAC1-ab, 10 nM), the VDAC1 inhibitors AKOS022075291 and VBIT-4 (20 μM each) on ATP release after 1 hr exposure at 1 mM glucose of INS-1 cells transfected with control plasmid or plVdac1. ATP content and release from isolated mouse or human islets or from INS-1 cells after transfection with mitochondrial targeted VDAC1 (mtVDAC1) or plasma membrane targeted VDAC1 (plVDAC1) plasmids was determined using a luminometric assay kit. After incubation of islets (50/vial) or INS-1 cells for 60 min, an aliquot of the media was removed for subsequent measurements of released ATP. Then the islets or INS-1 cells were washed 3 times and the lysates were used for measurements of ATP and protein contents.
In Vivo
In vivo

VBIT-4 prevents increases in water consumption and polyuria in the db/db mice, also counteracts VDAC1 overexpression, preventing mistargeting to the β cell surface under glucotoxic conditions. Through the prevention of VDAC1 gene expression, VBIT-4 may have disease-modifying actions.[2]
Animal Research Animal Models db/db, c57/bl mice
Dosages 25 mg/kg body
Administration i.p.

Chemical Information & Solubility

Molecular Weight 457.87 Formula

C21H23ClF3N3O3
CAS No. 2086257-77-2 SDF --
Smiles OCC(CC(=O)NC1=CC=C(Cl)C=C1)N2CCN(CC2)C3=CC=C(OC(F)(F)F)C=C3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 92 mg/mL ( (200.93 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 92 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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