VBIT-4

Catalog No.S3544 Batch:S354403

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Technical Data

Formula

C21H23ClF3N3O3
Molecular Weight 457.87 CAS No. 2086257-77-2
Solubility (25°C)* In vitro DMSO 92 mg/mL (200.93 mM)
Ethanol 92 mg/mL (200.93 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 90 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

[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), 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 Study:

[2]
  • Animal Models

    db/db, c57/bl mice

  • Dosages

    25 mg/kg body

  • Administration

    i.p.

Selleck's VBIT-4 has been cited by 12 publications

cGAS-STING drives ageing-related inflammation and neurodegeneration [ Nature, 2023, 620(7973):374-380] PubMed: 37532932
cGAS-STING drives ageing-related inflammation and neurodegeneration [ Nature, 2023, 620(7973):374-380] PubMed: 37532932
Non-canonical STING-PERK pathway dependent epigenetic regulation of vascular endothelial dysfunction via integrating IRF3 and NF-κB in inflammatory response [ Acta Pharm Sin B, 2023, 13(12):4765-4784] PubMed: 38045042
Role of mitochondria in the myopathy of juvenile dermatomyositis and implications for skeletal muscle calcinosis [ J Autoimmun, 2023, 138:103061] PubMed: 37244073
HSP90 C-terminal domain inhibition promotes VDAC1 oligomerization via decreasing K274 mono-ubiquitination in Hepatocellular Carcinoma [ Neoplasia, 2023, 44:100935] PubMed: 37717471
HSP90 C-terminal domain inhibition promotes VDAC1 oligomerization via decreasing K274 mono-ubiquitination in Hepatocellular Carcinoma [ Neoplasia, 2023, 44:100935] PubMed: 37717471
[VDAC1 participates in house dust mite-induced asthmatic airway inflammation in mice by inducing ferroptosis of airway epithelial cells] [ Nan Fang Yi Ke Da Xue Xue Bao, 2023, 10.1158/0008-5472.CAN-23-0650] PubMed: 37712269
Lysosomal damage drives mitochondrial proteome remodelling and reprograms macrophage immunometabolism [ Nat Commun, 2022, 13(1):7338] PubMed: 36443305
Cystathionine γ lyase S-sulfhydrates Drp1 to ameliorate heart dysfunction [ Redox Biol, 2022, 58:102519] PubMed: 36327794
Manganese induces tumor cell ferroptosis through type-I IFN dependent inhibition of mitochondrial dihydroorotate dehydrogenase [ Free Radic Biol Med, 2022, 193(Pt 1):202-212] PubMed: 36228830

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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