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Z-VAD-FMK

Z-VAD-FMK

产品编号 T7020   CAS 161401-82-7
别名: Z-VAD(OH)-FMK, Caspase Inhibitor VI, Z-VAD

Z-VAD-FMK (Caspase Inhibitor VI) 是一种 caspase 的广谱抑制剂,具有不可逆性。Z-VAD-FMK 与活化的 caspase 结合,从而抑制细胞凋亡

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Z-VAD-FMK Chemical Structure
Z-VAD-FMK, CAS 161401-82-7
规格 价格/CNY 货期 数量
1 mg ¥ 698 现货
5 mg ¥ 2,551 现货
10 mg ¥ 3,170 现货
25 mg ¥ 5,200 现货
1 mL * 10 mM (in DMSO) ¥ 2,555 现货
其他形式的 Z-VAD-FMK:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Z-VAD-FMK (T7020)
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选择批次  
纯度: 99.44%
纯度: 98.63%
纯度: 98.63%
纯度: 98.24%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Z-VAD-FMK (Caspase Inhibitor VI) is a broad-spectrum inhibitor of caspases with irreversible properties. Z-VAD-FMK binds to activated caspases, thereby inhibiting apoptosis.
体外活性 方法:中性粒细胞用 Z-VAD-FMK (0.03-300 µM) 处理 30 min,再加入在加入 200 U/mL TNFα 孵育 6 h,使用 Flow Cytometry 方法检测细胞凋亡情况。
结果:Z-VAD-FMK 对 TNFα 刺激的中性粒细胞凋亡具有双相作用。Z-VAD-FMK 100μM或以上时增强了 TNFα 诱导的凋亡程度,而在 30 μM 及以下时抑制凋亡。[1]
方法:人结直肠癌细胞 HCT116 和 SW480 用 Z-VAD-FMK (20 μM) 预处理 1 h,再加CPT (10-1000 ng/mL) 和 5-FU (5-12.5 μg/mL) 孵育 48 h 诱导凋亡,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:CPT 和 5-FU 诱导 cleaved caspase-3、caspase-8 和 PARP 显著上调,Z-VAD-FMK 预处理消除了凋亡相关蛋白的激活。[2]
方法:人T淋巴细胞白血病细胞 Jurkat 在脉冲后用 Z-VAD-FMK (10-200 μM) 处理 24 h,使用碘化丙啶检测细胞活力。
结果:Z-VAD-FMK 的最佳浓度为50 µM,与未处理的对照组相比,细胞活力从 35% 增加到 74%。[3]
体内活性 方法:为检测体内抗肿瘤活性,用 RT (2 Gy 局部照射肿瘤,第 8/9/10 天)、DTIC (2 mg/只腹腔注射,第 8/10 天)、将 Z-VAD-FMK (2  mg/kg 腹腔注射,第 8/9/10 天) 和 HT (放射后进行 4 h,第 8/10 天) 联合治疗携带小鼠黑色素瘤肿瘤 B16 的 C57/BL6 小鼠。
结果:RT、DTIC 和 HT 联合 Z-VAD-FMK 的多模式肿瘤治疗以 T 细胞依赖的方式延缓肿瘤生长。[4]
方法:为研究 Z-VAD-FMK 在内毒素休克中的作用,将 Z-VAD-FMK (5-20 μg/g) 单次腹腔注射给 LPS 诱导内毒素休克的 C57BL/6 小鼠。
结果:Z-VAD-FMK 治疗可以显著延长小鼠的存活时间数小时,并提高存活率。Z-VAD-FMK 治疗显著降低了用不同剂量 LPS 治疗的小鼠的死亡率。[5]
别名 Z-VAD(OH)-FMK, Caspase Inhibitor VI, Z-VAD
分子量 453.46
分子式 C21H28FN3O7
CAS No. 161401-82-7

存储

store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 83 mg/mL (183 mM)

DMSO: 83 mg/mL (183 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.2053 mL 11.0263 mL 22.0527 mL 55.1317 mL
5 mM 0.4411 mL 2.2053 mL 4.4105 mL 11.0263 mL
10 mM 0.2205 mL 1.1026 mL 2.2053 mL 5.5132 mL
20 mM 0.1103 mL 0.5513 mL 1.1026 mL 2.7566 mL
50 mM 0.0441 mL 0.2205 mL 0.4411 mL 1.1026 mL
100 mM 0.0221 mL 0.1103 mL 0.2205 mL 0.5513 mL

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TargetMol Library Books参考文献

1. Cowburn AS, et al. z-VAD-fmk augmentation of TNF alpha-stimulated neutrophil apoptosis is compound specific and does not involve the generation of reactive oxygen species. Blood. 2005 Apr 1;105(7):2970-2. 2. Sun T, et al. Effects of Recombinant Circularly Permuted Tumor Necrosis Factor (TNF)-Related Apoptosis-Inducing Ligand (TRAIL) (Recombinant Mutant Human TRAIL) in Combination with 5-Fluorouracil in Human Colorectal Cancer Cell Lines HCT116 and SW480. Med Sci Monit. 2018 Apr 26;24:2550-2561. 3. Wang C, et al. Inhibition of Caspases Improves Non-Viral T Cell Receptor Editing. Cancers (Basel). 2020 Sep 11;12(9):2603. 4. Werthmöller N, et al. Modulation of radiochemoimmunotherapy-induced B16 melanoma cell death by the pan-caspase inhibitor zVAD-fmk induces anti-tumor immunity in a HMGB1-, nucleotide- and T-cell-dependent manner. Cell Death Dis. 2015 May 14;6(5):e1761. 5. Li X, et al. The Caspase Inhibitor Z-VAD-FMK Alleviates Endotoxic Shock via Inducing Macrophages Necroptosis and Promoting MDSCs-Mediated Inhibition of Macrophages Activation. Front Immunol. 2019 Aug 2;10:1824.

TargetMol Library Books文献引用

1. Yan C, Zheng L, Jiang S, et al.Exhaustion-associated cholesterol deficiency dampens the cytotoxic arm of antitumor immunity.Cancer Cell.2023 2. Hu G, Cui Z, Chen X, et al.Suppressing Mesenchymal Stromal Cell Ferroptosis Via Targeting a Metabolism‐Epigenetics Axis Corrects their Poor Retention and Insufficient Healing Benefits in the Injured Liver Milieu.Advanced Science.2023: 2206439. 3. Wang X, Ji Y, Qi J, et al.Mitochondrial carrier 1 (MTCH1) governs ferroptosis by triggering the FoxO1-GPX4 axis-mediated retrograde signaling in cervical cancer cells.Cell Death & Disease.2023, 14(8): 1-13. 4. Zhu X, Huang N, Ji Y, et al.Brusatol induces ferroptosis in oesophageal squamous cell carcinoma by repressing GSH synthesis and increasing the labile iron pool via inhibition of the NRF2 pathway.Biomedicine & Pharmacotherapy.2023, 167: 115567. 5. Qiu C, Shen X, Lu H, et al.Combination therapy with HSP90 inhibitors and piperlongumine promotes ROS-mediated ER stress in colon cancer cells.Cell Death Discovery.2023, 9(1): 375. 6. Huang F, Liang J, Lin Y, et al.Repurposing of Ibrutinib and Quizartinib as potent inhibitors of necroptosis.Communications Biology.2023, 6(1): 972. 7. Shao H, Xu L, Li G, et al.Analysis on benzothiazole necroptosis inhibitors with chiral substitutions in the solvent-accessible region of RIP kinase domain.Bioorganic Chemistry.2023: 106647. 8. Zeng H, Xie H, Ma Q, et al.Identification of N-(3-(methyl (3-(orotic amido) propyl) amino) propyl) oleanolamide as a novel topoisomerase I catalytic inhibitor by rational design, molecular dynamics simulation, and biological evaluation.Bioorganic Chemistry.2023: 106734. 9. Sun Y, Xu L, Shao H, et al. Discovery of a Trifluoromethoxy Cyclopentanone Benzothiazole Receptor-Interacting Protein Kinase 1 Inhibitor as the Treatment for Alzheimer’s Disease. Journal of Medicinal Chemistry. 2022 10. Xue J, Gruber F, Tschachler E, et al. Crosstalk between oxidative stress, autophagy and apoptosis in Hemoporfin Photodynamic Therapy treated human umbilical vein endothelial cells. Photodiagnosis and Photodynamic Therapy. 2020: 102137.
11. Su G, Yang W, Wang S, et al. SIRT1-autophagy axis inhibits excess iron-induced ferroptosis of foam cells and subsequently increases IL-1Β and IL-18. Biochemical and Biophysical Research Communications. 2021, 561: 33-39. 12. Ning X, Qi H, Yuan Y, et al. Identification of a new small molecule that initiates ferroptosis in cancer cells by inhibiting the system Xc− to deplete GSH. European Journal of Pharmacology. 2022: 175304. 13. Wang F, Xie M, Chen P, et al. Homoharringtonine combined with cladribine and aclarubicin (HCA) in acute myeloid leukemia: A new regimen of conventional drugs and its mechanism. Oxidative Medicine and Cellular Longevity. 2022 14. Wang S, Wang Z, Wang X, et al. Humanized cerebral organoids-based ischemic stroke model for discovering of potential anti-stroke agents. Acta Pharmacologica Sinica. 2022: 1-11. 15. Sun Y, He L, Wang T, et al. Activation of p62-Keap1-Nrf2 Pathway Protects 6-Hydroxydopamine-Induced Ferroptosis in Dopaminergic Cells. Molecular Neurobiology. 2020, 57(11): 4628-4641. 16. Tschuck J, Theilacker L, Rothenaigner I, et al.Farnesoid X receptor activation by bile acids suppresses lipid peroxidation and ferroptosis.Nature Communications.2023, 14(1): 6908. 17. Tian T, Xie X, Yi W, et al.FBXO38 mediates FGL1 ubiquitination and degradation to enhance cancer immunity and suppress inflammation.Cell Reports.2023, 42(11). 18. Wu X, Yi X, Zhao B, et al.The volume regulated anion channel VRAC regulates NLRP3 inflammasome by modulating itaconate efflux and mitochondria function.Pharmacological Research.2023: 107016. 19. Liu S, Tao Y, Wu S, et al.Sanguinarine chloride induces ferroptosis by regulating ROS/BACH1/HMOX1 signaling pathway in prostate cancer.Chinese Medicine.2024, 19(1): 1-18. 20. Chen H, Hu J, Xiong X, et al.AURKA inhibition induces Ewing’s sarcoma apoptosis and ferroptosis through NPM1/YAP1 axis.Cell Death & Disease.2024, 15(1): 99. 21. Tao Y, Lu J, Li L, et al.Raltitrexed induces apoptosis through activating ROS-mediated ER stress by impeding HSPA8 expression in prostate cancer cells.Biochimica et Biophysica Acta (BBA)-Molecular Cell Research.2024: 119684. 22. Li J, Liu X, Liu Y, et al.Saracatinib inhibits necroptosis and ameliorates psoriatic inflammation by targeting MLKL.Cell Death & Disease.2024, 15(2): 122. 23. Li L, Fu S, Wang J, et al.SRT1720 inhibits bladder cancer cell progression by impairing autophagic flux.Biochemical Pharmacology.2024: 116111. 24. Lv S, Pan Q, Lu W, et al.Tenovin 3 induces apoptosis and ferroptosis in EGFR 19del non small cell lung cancer cells.Scientific Reports.2024, 14(1): 7654. 25. Yan J, Gao B, Wang C, et al.Calcified apoptotic vesicles from PROCR+ fibroblasts initiate heterotopic ossification.Journal of Extracellular Vesicles.2024, 13(4): e12425.
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该产品包含在如下化合物库中:
高选择性抑制剂库 抑制剂库 已知活性化合物库 NO PAINS 化合物库 抗衰老化合物库 经典已知活性库 抗癌化合物库

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Keywords

Z-VAD-FMK 161401-82-7 Apoptosis Proteases/Proteasome Caspase inhibit Inhibitor ZVADFMK Hela Z VAD FMK Antiapoptosis cells pan-caspase Z-VAD(OH)-FMK Caspase Inhibitor VI Z-VAD inhibitor

 

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