Z-VAD-FMK

製品コードS7023 バッチS702304

印刷

化学情報

 Chemical Structure Synonyms Z-VAD(OMe)-FMK Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C22H30FN3O7

分子量 467.49 CAS No. 187389-52-2
Solubility (25°C)* 体外 DMSO 93 mg/mL (198.93 mM)
Water Insoluble
Ethanol 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 Z-VAD-FMK (Z-VAD(OMe)-FMK) は、細胞透過性で不可逆的な汎カスパーゼ阻害剤であり、THP.1 および Jurkat T 細胞のアポトーシス (apoptosis) をブロックします。
in vitro

Z-VAD-FMK (10 μM) inhibits apoptosis in THP.1 cells. This compound (10 μM) inhibits activation of PARP protease activity in control THP.1 cell lysates. It (10 μM) inhibits the processing of CPP32 in intact THP.1 and Jurkat cells. This chemical (50 μM) cotreatment abolishes the apoptotic morphology of camptothecin-treated HL60 cells. It (50 μM) blocks camptothecin-induced DNA fragmentation in HL60 cells. The compound (50 μM) inhibits cell death following dSMN dsRNA-induced apoptosis in S2 cells. It (50 μM) increases the percentage of transfected cells surviving from 26% to 63% in S2 cells. This inhibitor (> 100 μM) enhances TNFα-induced neutrophil apoptosis, lower concentrations (1-30 μM) completely blocks TNFα-stimulated apoptosis in human neutrophils. It (10 mM) inhibits apoptosis in anterior stromal keratocytes. The chemical (10 mM) inhibits apoptosis in anterior stromal keratocytes detected with the TUNEL assay.

in vivo

In vivo Z-VAD-FMK administration has been shown previously to be nontoxic and to prevent apoptosis in animal models. Intraperitoneal HK-GBS injection leads to preterm delivery, and pretreatment with this compound delays preterm delivery in mice. In OVA-sensitized mice,treatment of this chemical inhibits allergen-induced leukocyte infiltration. Systemic injection of this compound immediately before OVA challenge reduced inflammatory cell accumulation, mucus hypersecretion, and Th2 cytokine release in OVA-sensitized/challenged mice. Treatment with this compound blocked terminal differentiation of lens epithelial cells and keratinocytes, the differentiation of monocytes into macrophages, and the differentiation of erythroid progenitors. This chemical attenuated allergen-induced airway inflammation and hyperreactivity. Treatment with this compound in vivo also prevented subsequent T cell activation ex vivo.

特徴 A key compound for apoptosis studies.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 human granulosa cell lines (GC1a, HGL5, COV434)
濃度 50 μM
反応時間 48 h
実験の流れ

To validate the efficacy of Z-VAD-FMK, three human granulosa cell lines (GC1a, HGL5, COV434) were treated for 48 h under normoxic conditions. To mimic the ischemic phase that occurs after ovarian fragment transplantation, cells were cultured without serum under hypoxia (1 % O2) and treated with this compound. The metabolic activity of the cells was evaluated by WST-1 assay. Cell viability was determined by FACS analyses. The expression of apoptosis-related molecules was assessed by RT-qPCR and Western blot analyses.

動物実験 動物モデル CD1 mice
投薬量 10 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/8670109/
  • https://pubmed.ncbi.nlm.nih.gov/9264376/
  • https://pubmed.ncbi.nlm.nih.gov/12783893/
  • https://pubmed.ncbi.nlm.nih.gov/15572588/
  • https://pubmed.ncbi.nlm.nih.gov/10973731/
  • https://pubmed.ncbi.nlm.nih.gov/26169075/
  • https://pubmed.ncbi.nlm.nih.gov/20069051/

カスタマーフィードバック

Data from [Acta Pharmacol Sin, 2014, 35(4):531-9]

Data from [Data independently produced by , , Science, 2018, 10(441), doi: 10.1126/scitranslmed.aao4680]

Data from [Data independently produced by , , Cancer Res, 2017, 77(4):926-936]

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:

NINJ1 regulates plasma membrane fragility under mechanical strain [ Nature, 2025, 10.1038/s41586-025-09222-5] PubMed: 40490006
Radiotherapy promotes cuproptosis and synergizes with cuproptosis inducers to overcome tumor radioresistance [ Cancer Cell, 2025, S1535-6108(25)00132-1] PubMed: 40215978
The noncanonical function of liver-type phosphofructokinase potentiates the efficacy of HDAC inhibitors in cancer [ Signal Transduct Target Ther, 2025, 10(1):341] PubMed: 41083431
Cytosolic cytochrome c represses ferroptosis [ Cell Metab, 2025, S1550-4131(25)00149-4] PubMed: 40233758
RIPK1 senses S-adenosylmethionine scarcity to drive cell death and inflammation [ Cell Metab, 2025, S1550-4131(25)00294-3] PubMed: 40570842
LINE-1 ORF1p Mimics Viral Innate Immune Evasion Mechanisms in Pancreatic Ductal Adenocarcinoma [ Cancer Discov, 2025, 10.1158/2159-8290.CD-24-1317] PubMed: 39919290
Harnessing the FGFR2/NF2/YAP signaling-dependent necroptosis to develop an FGFR2/IL-8 dual blockade therapeutic strategy [ Nat Commun, 2025, 16(1):4128] PubMed: 40319089
Evidence that mitochondria in macrophages are destroyed by microautophagy [ Nat Commun, 2025, 16(1):8123] PubMed: 40885798
De novo pyrimidine biosynthesis inhibition synergizes with BCL-XL targeting in pancreatic cancer [ Nat Commun, 2025, 16(1):6987] PubMed: 40738904
Ferroptosis-activating metabolite acrolein antagonizes necroptosis and anti-cancer therapeutics [ Nat Commun, 2025, 16(1):4919] PubMed: 40425585

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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