Z-VAD-FMK |
Cell-permeable, irreversible pan-caspase inhibitor |
Sample solution is provided at 25 µL, 10mM.
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Related Biological Data
Related Biological Data
Related Biological Data
| Cell-permeable, irreversible pan-caspase inhibitor. Inhibits caspase processing and apoptosis induction in tumor cells in vitro (IC50 = 0.0015 - 5.8 mM). Active in vivo. | ||||||
| Targets | Caspase | |||||
| IC50 | 0.0015 - 5.8 mM | |||||
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| Cas No. | 187389-52-2 | SDF | Download SDF |
| Synonyms | Benzyloxycarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone | ||
| 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 | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition: | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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Abstract
The caspase inhibitor Z-VAD-FMK exhibits immunosuppressive and anti-proliferative activities in T cell without inhibiting the activity of caspases 8 and 3, where it inhibits NF-KB, the expression of CD25 and FasL-induced apoptosis.
Abstract
The effects of Z-VAD-FMK, a caspase inhibitor, on T lymphocytes and the elicitation of murine ACD were investigated.
Abstract
Intracerebroventricular administration of Z-VAD-FMK, a caspase inhibitor restricted by blood-brain barrier, to post-radiation rats resulted in reduced numbers of TUNEL-positive cells in the hypoglossal nucleus, suppressed expression and activation of caspases 3/8/9 and decrease appearance of cytochrome c in the cytosolic fraction.
Abstract
Z-VAD-FMK is a caspase inhibitor that inhibits mitochondria-related apoptotic effects induced by CIN.
Abstract
Early direct infusion of Z-VAD-FMK, a caspase inhibitor, into cochlear leads to accelerated hearing recovery and reduced hair cell loss in pigs suffering gunshot noise-induced trauma.
Z-VAD-FMK, an inhibitor of ICE-like proteases, inhibits apoptosis in THP.1 cells induced by diverse stimuli1 and Fas antigen-induced apoptosis in Jurkat T-cells2. It inhibits apoptosis by blocking the activation of proCPP32 into its active form, rather than by preventing the proteolytic action of CPP32 directly.
Z- VAD-FMK inhibits the formation of large kilobasepair fragments of DNA induced by diverse stimuli. Z-VAD-FMK had little or no effect on STS-induced necrotic cell death suggesting that the ICE-like protease activity was not involved in necrosis3.
Z-VAD-FMK almost completely inhibited the formation of large kilobasepair induced by all four stimuli. Similarly Z-VAD-FMK almost completely inhibited the enhanced formation of large kilobasepair fragments induced by thapsigargin or cycloheximide in the presence of TLCK, in good agreement with its ability to inhibit apoptosis induced by these treatments. These stimuli also induced internucleosomal cleavage of DNA, which was inhibited by Z-VAD-FMK. These results suggested that an ICE-like protease(s) acts at a stage prior to the formation of large kilobasepair fragments of DNA3.
References:
1. Darmon, A.J., Ehrman, N., Caputo, A., Fujinaga, J. and Bleackley, R.C. (1994) J. Biol. Chem. 269, 32043-32046.
2. Chow, S. C., Weis M., Kass, G. E. N., Holmstrom, T. H., Eriksson, J. E. and Orrenius S. (1995) FEBS Lett. 364, 134±138
3. H. Zhu et al./FEBS Letters 374 (1995) 303-308
