Z-VAD-FMK (Synonyms: Benzyloxycarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone,Z-Val-Ala-Asp(OMe)-FMK) |
| Catalog No.GC12861 |
Z-VAD-FMK (Benzyloxycarbonyl-Val-Ala-Asp (OMe) fluoromethylketone), an ICE-like protease inhibitor, inhibits apoptosis by preventing the processing of CPP32 to its active form. [3]
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Cas No.: 187389-52-2
Sample solution is provided at 25 µL, 10mM.
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Z-VAD-FMK (Benzyloxycarbonyl-Val-Ala-Asp (OMe) fluoromethylketone), an ICE-like protease inhibitor, inhibits apoptosis by preventing the processing of CPP32 to its active form. [3]
Z-VAD-FMK is immunosuppressive in vitro and inhibit T cell proliferation without blocking the processing of caspase-8 and caspase-3. Z-VAD-FMK is capable of inhibiting T cell proliferation induced by anti-CD3 plus anti-CD28 or PHA. Besides, z-VAD-FMK inhibits caspase processing during apoptosis but not during T cell activation. Z-VAD-FMK Inhibits caspase processing and apoptosis induction in tumor cells in vitro (IC50 = 0.0015 - 5.8 mM). [1]
Z-VAD-FMK, can be used to induce necroptosis under certain stimuli. Treatment of mice with Z-VAD-FMK could significantly reduce mortality and alleviate disease after lipopolysaccharide (LPS) challenge. Notably, in LPS-challenged mice, treatment with Z-VAD-FMK could also reduce the percentage of peritoneal macrophages by promoting necroptosis and inhibiting pro-inflammatory responses in macrophages. What’s more, pretreatment with Z-VAD-FMK promoted LPS-induced nitric oxide-mediated necroptosis of bone marrow-derived macrophages (BMDMs), leading to reduced pro-inflammatory cytokine secretion. Interestingly, Z-VAD-FMK treatment promoted the accumulation of myeloid-derived suppressor cells (MDSCs) in a mouse model of endotoxin shock, and this process inhibited LPS-induced pro-inflammatory responses in macrophages. Treatment with Z-VAD-FMK alleviates LPS-induced endotoxic shock by inducing macrophage necroptosis and promoting MDSC-mediated inhibition of macrophage activation. For in vivo experienment, the mice were pretreated or post-treated with Z-VAD-FMK (5, 10, and 20 μg/g of body weight) or vehicle (saline) for 2 h and endotoxic shock was induced by an intraperitoneal injection of LPS (10 μg/g of body weight) and saline was used as control. [2]
References:
[1]. Lawrence CP, Chow SC. Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties. Toxicol Appl Pharmacol. 2012 Nov 15;265(1):103-12.
[2]. Li X, Yao X, Zhu Y, 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.
[3]. Slee EA, Zhu H, et al. Benzyloxycarbonyl-Val-Ala-Asp (OMe) fluoromethylketone (Z-VAD.FMK) inhibits apoptosis by blocking the processing of CPP32. Biochem J. 1996 Apr 1;315 (Pt 1) (Pt 1):21-4.
| Cell experiment [1]: | |
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Cell lines |
CD4+ and CD8+ T cells |
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Preparation Method |
Soluble in DMSO to 20 mM |
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Reaction Conditions |
100 μM, 24 h |
|
Applications |
Z-VAD-FMK is immunosuppressive in vitro and inhibit T cell proliferation without blocking the processing of caspase-8 and caspase-3. |
| Animal experiment [2]: | |
|
Animal models |
C57BL/6 Mice (Treatment with LPS) |
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Preparation Method |
Soluble in DMSO to 20 mM |
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Dosage form |
20 μg/g, i.p. |
|
Applications |
Z-VAD-FMK treatment alleviates LPS-induced endotoxic shock by inducing macrophage necroptosis and promoting MDSC-mediated inhibition of macrophage activation. |
|
References: [1]. Lawrence CP, Chow SC. Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties. Toxicol Appl Pharmacol. 2012 Nov 15;265(1):103-12. [2]. Li X, Yao X, Zhu Y, 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. |
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| Cas No. | 187389-52-2 | SDF | |
| Synonyms | Benzyloxycarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone,Z-Val-Ala-Asp(OMe)-FMK | ||
| Chemical Name | methyl (3S)-5-fluoro-3-[[(2S)-2-[[(2S)-3-methyl-2-(phenylmethoxycarbonylamino)butanoyl]amino]propanoyl]amino]-4-oxopentanoate | ||
| Canonical SMILES | CC(C)C(C(=O)NC(C)C(=O)NC(CC(=O)OC)C(=O)CF)NC(=O)OCC1=CC=CC=C1 | ||
| Formula | C22H30FN3O7 | M.Wt | 467.49 |
| Solubility | ≥ 23.37mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1391 mL | 10.6954 mL | 21.3908 mL |
| 5 mM | 0.4278 mL | 2.1391 mL | 4.2782 mL |
| 10 mM | 0.2139 mL | 1.0695 mL | 2.1391 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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After pretreatment with the pancaspase inhibitor zVAD-FMK for 2 h, U251 and U87MG cells were incubated with AT7519 for an additional 48 h.
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HBO1 knockdown provokes apoptosis of B-ALL cells.A. E, F B-ALL cells with or without HBO1 knockdown were treated with Z-DEVD-FMK (30 μM), Z-VAD-FMK (30 μM), or vehicle (0.1% of DMSO) and cultured for 96 h,followed by the cell viability (E) and death (F) examination by CCK8 and trypan blue staining.
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Cetuximab treatment enhances RSL3-induced ferroptosis in KRAS mutant CRC cells.E HCT116 and DLD-1 cells were treated with cetuximab (100 μg/ml) or RSL3 (1 μM) in combination with Z-VAD-FMK (10 μM), necrostatin-1 (10 μM) or 3-MA (60 μM) for 24 h,and cell viability was assessed by the CCK-8 assay.
HCT116 and DLD-1 cells were treated with Z-VAD-FMK (10 μM),and cell viability was assessed by the CCK-8 assay.
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Resv inhibits the proliferation of breast cancer cells by autophagy. (c) After the 4T1 cells were pretreated with Resv (25 μM), the 3-MA (1 mM), Z-VAD-FMK (40 μM), or necrosulfonamide (NSA, 2.5 μM) was added respectively to the cells for 24 hr, and the cell viability was detected by the CCK-8 assay.
The Z-VAD-FMK (40 μM) added to the 4T1 cells for 24 hr, and the cell viability was detected by the CCK-8 assay.
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Cysteine depletion induces ferroptosis in K562/G01 but not K562 cells.(a) K562/G01 cells were treated with Fer-1 (2 μM), Nec-1s(10 μM), Z-VAD-FMK (10 μM), or chloroquine (25 μM) cultured in normal or cysteine depletion condition for 24 h. Cell viability was measured using the MTS kit.
K562 cells were treated with Fer-1 (2μM), necrostatin-1s (10 μM), Z-VAD-FMK (10 μM), or chloroquine (25 μM) cultured in normal or cysteine depletion condition for 24 h.
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