VBIT-4

Catalog No.S3544

For research use only.

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

CAS No. 2086257-77-2

Selleck's VBIT-4 has been cited by 1 Publication

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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

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]

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]

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: INS-1 cells transfected with plVdac1
  • Concentrations: 20 μM
  • Incubation Time: 1 h
  • Method:

    Effect of VDAC1 antibody (VDAC1-ab, 10 nM), metformin, or 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.

Animal Research:

[2]

  • Animal Models: db/db, c57/bl mice
  • Dosages: 25 mg/kg body
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 457.87
Formula

C21H23ClF3N3O3

CAS No. 2086257-77-2
Storage 3 years -20°C powder
2 years -80°C in solvent

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