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Z-VAD-FMK

Catalog No. T7020 CAS 161401-82-7

Synonyms: Z-VAD(OH)-FMK, Caspase Inhibitor VI, Z-VAD

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Z-VAD-FMK, CAS 161401-82-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 121.00
5 mg	In stock	$ 257.00
10 mg	In stock	$ 438.00
25 mg	In stock	$ 696.00
1 mL * 10 mM (in DMSO)	In stock	$ 283.00

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Purity: 99.44%

Purity: 98.63%

Purity: 98.24%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	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.
In vitro	METHODS: Neutrophils were treated with Z-VAD-FMK (0.03-300 µM) for 30 min, then incubated with 200 U/mL TNFα for 6 h. Apoptosis was detected by Flow Cytometry. RESULTS: Z-VAD-FMK had a biphasic effect on TNFα-stimulated neutrophil apoptosis. 100 µM or more of Z-VAD-FMK enhanced TNFα-induced apoptosis, whereas 30 µM or less inhibited apoptosis. [1] METHODS: Human colorectal cancer cells HCT116 and SW480 were pretreated with Z-VAD-FMK (20 μM) for 1 h, then incubated with CPT (10-1000 ng/mL) and 5-FU (5-12.5 μg/mL) for 48 h to induce apoptosis, and then the expression levels of target proteins were detected by Western Blot. RESULTS: CPT and 5-FU induced significant up-regulation of cleaved caspase-3, caspase-8 and PARP, and Z-VAD-FMK pretreatment eliminated the activation of apoptosis-related proteins. [2] METHODS: Human T-lymphoblastic leukemia cells Jurkat were treated with Z-VAD-FMK (10-200 µM) for 24 h after pulsing, and cell viability was measured using propidium iodide. RESULTS: The optimal concentration of Z-VAD-FMK was 50 µM, which increased cell viability from 35% to 74% compared to untreated control. [3]
In vivo	METHODS: To detect anti-tumor activity in vivo, C57/BL6 mice bearing mouse melanoma tumor B16 were treated with RT (2 Gy local irradiation of the tumor on day 8/9/10), DTIC (2 mg/pc intraperitoneal injection on day 8/10), and a combination of Z-VAD-FMK (2 mg/kg intraperitoneal injection on day 8/9/10) and HT (4 h post-irradiation on day 8/10). RESULTS: Multimodal tumor therapy with RT, DTIC, and HT in combination with Z-VAD-FMK retarded tumor growth in a T-cell-dependent manner. [4] METHODS: To investigate the role of Z-VAD-FMK in endotoxin shock, Z-VAD-FMK (5-20 μg/g) was administered as a single intraperitoneal injection to LPS-induced endotoxin shock in C57BL/6 mice. RESULTS: Z-VAD-FMK treatment significantly prolonged the survival time of mice for several hours and increased the survival rate. Z-VAD-FMK treatment significantly reduced the mortality rate of mice treated with different doses of LPS. [5]

Synonyms	Z-VAD(OH)-FMK, Caspase Inhibitor VI, Z-VAD
Molecular Weight	453.46
Formula	C21H28FN3O7
CAS No.	161401-82-7

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

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

Ethanol: 83 mg/mL (183 mM)

DMSO: 83 mg/mL (183 mM)

References and Literature

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.

Citations

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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Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Anti-Aging Compound Library Bioactive Compound Library Anti-Cancer Compound Library

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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

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.