VBIT-4

製品コードS3544 バッチS354404

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C21H23ClF3N3O3
分子量 457.87 CAS No. 2086257-77-2
Solubility (25°C)* 体外 DMSO 92 mg/mL (200.93 mM)
Ethanol 92 mg/mL (200.93 mM)
Water Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 INS-1 cells transfected with plVdac1
濃度 20 μM
反応時間 1 h
実験の流れ

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.
動物実験 動物モデル db/db, c57/bl mice
投薬量 25 mg/kg body
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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