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受注：045-509-1970 |
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化学情報
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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 |
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| 分子量 | 467.49 | CAS No. | 187389-52-2 | |
| Solubility (25°C)* | 体外 | DMSO | 93 mg/mL (198.93 mM) | |
| Ethanol | 2 mg/mL warmed with 50ºC water bath (4.27 mM) | |||
| Water | Insoluble | |||
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* <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. |
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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。 |
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| in vitro | Z-VAD-FMK (10 μM) inhibits apoptosis in THP.1 cells. Z-VAD-FMK (10 μM) inhibits activation of PARP protease activity in control THP.1 cell lysates. Z-VAD-FMK (10 μM) inhibits the processing of CPP32 in intact THP.1 and Jurkat cells. [1] Z-VAD-FMK (50 μM) cotreatment abolishes the apoptotic morphology of camptothecin-treated HL60 cells. Z-VAD-FMK (50 μM) blocks camptothecin-induced DNA fragmentation in HL60 cells. [2] Z-VAD-FMK (50 μM) inhibits cell death following dSMN dsRNA-induced apoptosis in S2 cells. Z-VAD-FMK (50 μM) increases the percentage of transfected cells surviving from 26% to 63% in S2 cells. [3] Z-VAD-FMK (> 100 μM) enhances TNFα-induced neutrophil apoptosis, lower concentrations (1-30 μM) completely blocks TNFα-stimulated apoptosis in human neutrophils. [4] Z-VAD-FMK (10 mM) inhibits apoptosis in anterior stromal keratocytes. Z-VAD-FMK (10 mM) inhibits apoptosis in anterior stromal keratocytes detected with the TUNEL assay. [5] |
| 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 Z-VAD-FMK delays preterm delivery in mice. In OVA-sensitized mice,treatment of z-VAD-fmk inhibits allergen-induced leukocyte infiltration. Systemic injection of the pan-caspase inhibitor z-VAD-fmk immediately before OVA challenge reduced inflammatory cell accumulation, mucus hypersecretion, and Th2 cytokine release in OVA-sensitized/challenged mice. Treatment with z-VAD-fmk blocked terminal differentiation of lens epithelial cells and keratinocytes, the differentiation of monocytes into macrophages, and the differentiation of erythroid progenitors. z-VAD-fmk attenuated allergen-induced airway inflammation and hyperreactivity. Treatment with z-VAD-fmk in vivo also prevented subsequent T cell activation ex vivo[7]. |
| 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) |
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| 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 with etoposide (50 μg/ml) and/or Z-VAD-FMK (50 μM) 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 Z-VAD-FMK. 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. |
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| 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
カスタマーフィードバック
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Data from [Acta Pharmacol Sin, 2014, 35(4):531-9]
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Data from [Data independently produced by , , Science, 2018, 10(441), doi: 10.1126/scitranslmed.aao4680]
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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：
| 7-Dehydrocholesterol dictates ferroptosis sensitivity [ Nature, 2024, 626(7998):411-418.] | PubMed: 38297130 |
| Plasticity-induced repression of Irf6 underlies acquired resistance to cancer immunotherapy in pancreatic ductal adenocarcinoma [ Nat Commun, 2024, 15(1):1532] | PubMed: 38378697 |
| EFHD2 suppresses intestinal inflammation by blocking intestinal epithelial cell TNFR1 internalization and cell death [ Nat Commun, 2024, 15(1):1282] | PubMed: 38346956 |
| Targeting of vulnerabilities of drug-tolerant persisters identified through functional genetics delays tumor relapse [ Cell Rep Med, 2024, 5(3):101471] | PubMed: 38508142 |
| Heterogeneous ferroptosis susceptibility of macrophages caused by focal iron overload exacerbates rheumatoid arthritis [ Redox Biol, 2024, 69:103008] | PubMed: 38142586 |
| Induction of IFIT1/IFIT3 and inhibition of Bcl-2 orchestrate the treatment of myeloma and leukemia via pyroptosis [ Cancer Lett, 2024, 588:216797] | PubMed: 38462032 |
| Synergism of non-thermal plasma and low concentration RSL3 triggers ferroptosis via promoting xCT lysosomal degradation through ROS/AMPK/mTOR axis in lung cancer cells [ Cell Commun Signal, 2024, 22(1):112] | PubMed: 38347507 |
| Blocking CIRP protects against acute pancreatitis by improving mitochondrial function and suppressing pyroptosis in acinar cells [ Cell Death Discov, 2024, 10(1):156] | PubMed: 38538578 |
| PKCiota Inhibits the Ferroptosis of Esophageal Cancer Cells via Suppressing USP14-Mediated Autophagic Degradation of GPX4 [ Antioxidants (Basel), 2024, 13(1)114] | PubMed: 38247539 |
| The cell fate regulator DACH1 modulates ferroptosis through affecting P53/SLC25A37 signaling in fibrotic disease [ Hepatol Commun, 2024, 8(3)e0396] | PubMed: 38437058 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。