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Z-VAD(OMe)-FMK

Catalog No. T6013 CAS 187389-52-2

Synonyms: Z-VAD-FMK, Z-Val-Ala-Asp(OMe)-FMK

Z-VAD(OMe)-FMK (Z-Val-Ala-Asp(OMe)-FMK) is a broad-spectrum inhibitor of caspases that is cell-permeable and irreversible. Z-VAD(OMe)-FMK binds to activated caspases, thereby inhibiting apoptosis.

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Z-VAD(OMe)-FMK, CAS 187389-52-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 52.00
2 mg	In stock	$ 80.00
5 mg	In stock	$ 147.00
10 mg	In stock	$ 247.00
25 mg	In stock	$ 368.00
50 mg	In stock	$ 497.00
100 mg	In stock	$ 693.00
200 mg	In stock	$ 982.00
1 mL * 10 mM (in DMSO)	In stock	$ 148.00

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Purity: 99.41%

Purity: 98%

Purity: 95.92%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Z-VAD(OMe)-FMK (Z-Val-Ala-Asp(OMe)-FMK) is a broad-spectrum inhibitor of caspases that is cell-permeable and irreversible. Z-VAD(OMe)-FMK binds to activated caspases, thereby inhibiting apoptosis.
In vitro	METHODS: Human leukemia cells HL60 were treated with Z-VAD(OMe)-FMK (50 µM) and camptothecin (50 M) for 3 h. Cell morphology was observed by electron microscopy. RESULTS: Cells treated with camptothecin exhibited typical apoptotic features including cell shrinkage, chromatin condensation and nuclear fragmentation.Z-VAD(OMe)-FMK combination treatment eliminated the camptothecin-induced apoptotic pattern. Z-VAD(OMe)-FMK alone did not affect cell morphology. [1] METHODS: Cholangiocarcinoma cells KKU100, KKU213A and KKU213B were pretreated with Z-VAD(OMe)-FMK (20 µM) for 1 h, followed by CH-MSCs (0%, 50% and 75%) for 24 h. Apoptosis was detected using Flow Cytometry. RESULTS: Z-VAD(OMe)-FMK pretreatment prevented the apoptosis induced by CH-MSCs. [2] METHODS: Human ovarian teratoma cells PA-1 were treated with Z-VAD(OMe)-FMK (50 μM) and UVB (100 J/m2) for 16 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: Z-VAD(OMe)-FMK eliminated PARP cleavage induced by UVB. [3]
In vivo	METHODS: To investigate whether in vivo administration of Z-VAD(OMe)-FMK prevents infection-induced preterm labor, a single intraperitoneal injection of Z-VAD(OMe)-FMK (10 mg/kg) was administered to CD1 mice in which preterm labor was induced by heat-killed group B streptococcus (HK-GBS). RESULTS: Z-VAD(OMe)-FMK pretreatment delayed but did not prevent HK-GBS-induced preterm labor in a pregnant mouse model. [4] METHODS: To prevent LPS-induced acute lung injury, Z-VAD(OMe)-FMK (0.25 mg 15 min before LPS stimulation, 0.1 mg three times per hour) was injected intravenously into ICR mice with LPS-induced apoptosis and acute lung injury. RESULTS: Z-VAD(OMe)-FMK inhibited caspase-3 activity in lung tissues. Z-VAD(OMe)-FMK significantly prolonged the survival of mice. Apoptosis may play an important role in acute lung injury, and thus inhibition of caspase activity may provide a new therapeutic approach for the treatment of this disease. [5]
Cell Research	The human monocytic tumour cell line, THP.1 and the leukaemic T-cell line, Jurkat (clone E-6) were maintained in RPMI 1640 supplemented with 10% (v/v) heat-inactivated fetal calf serum, 100 units/ml penicillin and 100 μg/ml streptomycin in an atmosphere of 5% CO2 in air at 37 °C. The cells were maintained in logarithmic growth phase by routine passage every 2–3 days. To induce apoptosis in THP.1 cells, 2×10^6 cells/ml were incubated either alone or in the presence of cycloheximide (25 μM) and TLCK (100 μM) as previously described. In order to assess the possible effects of various ICE-like protease inhibitors, THP.1 cells were also pretreated for 1 h with Z-VAD.FMK (10 μM), Ac-DEVD-CHO (20 μM) and Ac-YVAD-CHO (20 μM) before being exposed to the apoptotic stimulus. To induce apoptosis in Jurkat cells, 2×10^6 cells/ml were stimulated with 200 ng/ml anti-human Fas as described previously [1].
Animal Research	Mice used in this study were 5- to 6-week-old (20 to 22 g) ICR males. Mice were injected with 30 mg/kg LPS from E. coli serotype O111:B4 through the tail vein. Z-VAD.fmk was dissolved at 2 mg/ml in 1% dimethyl sulfoxide in sterile saline, and administered to mice by the method of Rodriguez et al. A single intravenous injection of Z-VAD.fmk (0.25 mg) was made 15 minutes before LPS injection, followed by three intravenous injections of Z-VAD.fmk (0.1 mg each) per hour. Control mice were injected with the same volume of 1% DMSO in sterile saline [4].

Synonyms	Z-VAD-FMK, Z-Val-Ala-Asp(OMe)-FMK
Molecular Weight	467.49
Formula	C22H30FN3O7
CAS No.	187389-52-2

Storage

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

Solubility Information

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

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

DMSO: 93 mg/mL (198.93 mM)

References and Literature

1. Shimizu T, et al. Camptothecin-induced apoptosis in p53-null human leukemia HL60 cells and their isolated nuclei: effects of the protease inhibitors Z-VAD-fmk and dichloroisocoumarin suggest an involvement of both caspases and serine proteases. Leukemia. 1997 Aug;11(8):1238-44. 2. Jantalika T, et al. Human chorion-derived mesenchymal stem cells suppress JAK2/STAT3 signaling and induce apoptosis of cholangiocarcinoma cell lines. Sci Rep. 2022 Jul 5;12(1):11341. 3. Castrogiovanni C, et al. Decrease of mitochondrial p53 during late apoptosis is linked to its dephosphorylation on serine 20. Cancer Biol Ther. 2015;16(9):1296-307. 4. Equils O, et al. Pretreatment with pancaspase inhibitor (Z-VAD-FMK) delays but does not prevent intraperitoneal heat-killed group B Streptococcus-induced preterm delivery in a pregnant mouse model. Infect Dis Obstet Gynecol. 2009;2009:749432. 5. Kawasaki M, et al. Protection from lethal apoptosis in lipopolysaccharide-induced acute lung injury in mice by a caspase inhibitor. Am J Pathol. 2000 Aug;157(2):597-603. 6. Lu Z, Zhang G, Zhang Y, et al. Isoalantolactone induces apoptosis through reactive oxygen species-dependent upregulation of death receptor 5 in human esophageal cancer cells[J]. Toxicology and applied pharmacology. 2018, 352: 46-58. 7. Shao C S, Zhou X H, Zheng X X, et al. Ganoderic acid D induces synergistic autophagic cell death except for apoptosis in ESCC cells[J]. Journal of Ethnopharmacology. 2020, 262: 113213. 8. Wu X, Luo Q, Zhao P, et al. JOSD1 inhibits mitochondrial apoptotic signalling to drive acquired chemoresistance in gynaecological cancer by stabilizing MCL1[J]. Cell Death & Differentiation. 2020, 27(1): 55-70. 9. Zhu Q, Ding L, Zi Z, et al. Viral-Mediated AURKB Cleavage Promotes Cell Segregation and Tumorigenesis[J]. Cell reports. 2019 Mar 26;26(13):3657-3671.e5. 10. Wang S, Li F, Qiao R, et al. Arginine-Rich Manganese Silicate Nanobubbles as a Ferroptosis-Inducing Agent for Tumor-Targeted Theranostics[J]. ACS nano. 2018 Dec 26;12(12):12380-12392.

Citations

1. Bi G, Liang J, Shan G, et al.Retinol saturase mediates retinoid metabolism to impair a ferroptosis defense system in cancer cells.Cancer Research.2023: CAN-22-3977. 2. Li Y, Yang W, Zheng Y, et al.Targeting fatty acid synthase modulates sensitivity of hepatocellular carcinoma to sorafenib via ferroptosis.Journal of Experimental & Clinical Cancer Research.2023, 42(1): 1-19. 3. Quan D, Hou R, Shao H, et al.Structure-Based Design of Novel Alkynyl Thio-Benzoxazepinone Receptor-Interacting Protein Kinase-1 Inhibitors: Extending the Chemical Space from the Allosteric to ATP Binding Pockets.Journal of Medicinal Chemistry.2023 4. Zhang X, Han Q, Hou R, et al.Targeting Receptor-Interacting Protein Kinase 1 by Novel Benzothiazole Derivatives: Treatment of Acute Lung Injury through the Necroptosis Pathway.Journal of Medicinal Chemistry.2023 5. Yang W, Sun X, Liu S, et al.TLR8 agonist Motolimod-induced inflammatory death for treatment of acute myeloid leukemia.Biomedicine & Pharmacotherapy.2023, 163: 114759. 6. Cui N, Li S, Zhang Y, et al.Discovery of Sibiriline derivatives as novel receptor-interacting protein kinase 1 inhibitors.European Journal of Medicinal Chemistry.2023: 115190. 7. Urade R, Chang W T, Ko C C, et al.A fluorene derivative inhibits human hepatocellular carcinoma cells by ROS-mediated apoptosis, anoikis and autophagy.Life Sciences.2023: 121835. 8. Xu Y, Liang C, Zhang W, et al.Profiling of the chemical space on the phenyl group of substituted benzothiazole RIPK3 inhibitors.Bioorganic Chemistry.2022: 106339. 9. Tang J, Wu Y, Zhao W, et al.Scaffold hopping derived novel benzoxazepinone RIPK1 inhibitors as anti-necroptosis agents.Bioorganic & Medicinal Chemistry.2023: 117385. 10. Yang D L, Zhang Y, He L, et al. Demethylzeylasteral (T-96) Initiates Extrinsic Apoptosis Against Prostate Cancer cells by Inducing ROS-Mediated ER Stress and Suppressing Autophagic Flux. Biological Research. 2021, 54(1): 1-14.

11. Zhu Q, Ding L, Zi Z, et al. Viral-Mediated AURKB Cleavage Promotes Cell Segregation and Tumorigenesis. Cell Reports. 2019 Mar 26;26(13):3657-3671.e5 12. Wang S, Li F, Qiao R, et al. Arginine-Rich Manganese Silicate Nanobubbles as a Ferroptosis-Inducing Agent for Tumor-Targeted Theranostics. ACS nano. 2018 Dec 26;12(12):12380-12392. 13. Xia Z, Zhang X, Liu P, et al. GNA13 regulates BCL2 expression and the sensitivity of GCB-DLBCL cells to BCL2 inhibitors in a palmitoylation-dependent manner. Cell Death & Disease. 2021, 12(1): 1-11. 14. Liao X, Fan Y, Hou J, et al. Identification of Chaetocin as a Potent non-ROS-mediated Anticancer Drug Candidate for Gastric Cancer. Journal of Cancer. 2019, 10(16): 3678-3690. 15. Ouyang S, Li H, Lou L, et al. Inhibition of STAT3-ferroptosis negative regulatory axis suppresses tumor growth and alleviates chemoresistance in gastric cancer. Redox Biology. 2022: 102317 16. Wu X, Lu Y, Qin X. Combination of Compound Kushen Injection and cisplatin shows synergistic antitumor activity in p53-R273H/P309S mutant colorectal cancer cells through inducing apoptosis. Journal of Ethnopharmacology. 2021: 114690. 17. Wu Q, Zhang M, Wen Y, et al. Identifying chronic alcoholism drug disulfiram as a potent DJ-1 inhibitor for cancer therapeutics. European Journal of Pharmacology. 2022: 175035 18. Shao C S, Zhou X H, Zheng X X, et al. Ganoderic acid D induces synergistic autophagic cell death except for apoptosis in ESCC cells. Journal of Ethnopharmacology. 2020, 262: 113213. 19. Hussain M, Lu Y, Tariq M, et al. A small-molecule Skp1 inhibitor elicits cell death by p53-dependent mechanism. Iscience. 2022, 25(7): 104591. 20. Wen L, Guo R, You L, et al. Major triterpenoids in Chinese hawthorn “Crataegus pinnatifida” and their effects on cell proliferation and apoptosis induction in MDA-MB-231 cancer cells. Food and chemical toxicology. 2017 Feb;100:149-160. 21. Zhu L, Han Z, He Y, et al. Caspase-1-Dependent Pyroptosis Mediates Adjuvant Activity of Platycodin D as an Adjuvant for Intramuscular Vaccines. Cells. 2022, 11(1): 134. 22. Lu Z, Zhang G, Zhang Y, et al. Isoalantolactone induces apoptosis through reactive oxygen species-dependent upregulation of death receptor 5 in human esophageal cancer cells. Toxicology and applied pharmacology. 2018, 352: 46-58. 23. Zhang P, Zhang J, Quan H, et al. Effects of butein on human osteosarcoma cell proliferation, apoptosis, and autophagy through oxidative stress. Human & Experimental Toxicology. 2022, 41: 09603271221074346. 24. Shan G, Bi G, Zhao G, et al.Inhibition of PKA/CREB1 pathway confers sensitivity to ferroptosis in non-small cell lung cancer.Respiratory Research.2023, 24(1): 1-15. 25. Wang Y, Zhang B, Liu S, et al.The traditional herb Sargentodoxa cuneata alleviates DSS-induced colitis by attenuating epithelial barrier damage via blocking necroptotic signaling.Journal of Ethnopharmacology.2023: 117373. 26. Heber N, Kuhn B J, Strobel T D, et al.The impact of cycling hypoxia on the phenotype of HPV‐positive cervical cancer cells.Journal of Medical Virology.2023, 95(12): e29280. 27. Xin Y F, Dai P, Shao H, et al.Discovery of novel biaryl benzoxazepinones as dual-mode receptor-interacting protein kinase-1 (RIPK1) inhibitors.Bioorganic & Medicinal Chemistry.2024: 117611. 28. Tang Y, Zhuang C.Design, synthesis and anti-necroptosis activity of fused heterocyclic MLKL inhibitors.Bioorganic & Medicinal Chemistry.2024: 117659. 29. Xu L, Wen B, Wu Q, et al.Long non-coding RNA KB-1460A1. 5 promotes ferroptosis by inhibiting mTOR/SREBP-1/SCD1-mediated polyunsaturated fatty acid desaturation in glioma.Carcinogenesis.2024: bgae016. 30. Jiang R, Xu B, Zhi S, et al.Scaffold hopping derived novel benzoxazepinone receptor-interacting protein kinase 1 (RIP1) inhibitors as anti-necroptosis agents: Anti-inflammatory effect in systemic inflammatory response syndrome (SIRS) and epilepsy.European Journal of Medicinal Chemistry.2024: 116304. 31. Bi G, Liang J, Bian Y, et al.Polyamine-mediated ferroptosis amplification acts as a targetable vulnerability in cancer.Nature Communications.2024, 15(1): 2461.

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This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library Peptide Compound Library Bioactive Compounds Library Max Covalent Inhibitor Library Anti-Cancer Compound Library NO PAINS Compound Library Bioactive Compound Library Protease Inhibitor Library Pyroptosis Compound Library

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Keywords

Z-VAD(OMe)-FMK 187389-52-2 Apoptosis Proteases/Proteasome Caspase Inhibitor Z-VAD-FMK ZVAD(OMe)FMK inhibit Z-Val-Ala-Asp(OMe)-FMK Z VAD(OMe) FMK inhibitor

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