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Z-VAD-FMK

Cell-permeable, irreversible pan-caspase inhibitor

Z-VAD-FMK

Catalog No. A1902
Size Price Stock Qty
Evaluation Sample $28.00  All Inclusive In stock
1mg $55.00 In stock
5mg $150.00 In stock
10mg $250.00 In stock
25mg $400.00 In stock

All inclusive: Shipping and all other fees included

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Sample solution is provided at 25 µL, 10mM.

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Related Biological Data

Z-VAD-FMK

Related Biological Data

Z-VAD-FMK

Related Biological Data

Z-VAD-FMK
Apoptosis was induced by Paclitaxel and the cells were then treated with Z-VAD-FMK and Q-VD-OPH at 0,10,20, and 50um. Caspase activities were measured by Promega Caspase-Glo assay were compared with vehicle control.

Biological Activity

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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Chemical Properties

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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Research Update

1. 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. doi: 10.1016/j.taap.2012.09.002. Epub 2012 Sep 12.
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.
2. [Inhibition of elicitation of allergic contact dermatitis by topical use of Z-VAD-FMK, a broad caspase inhibitor: experiment in mice]. Zhonghua Yi Xue Za Zhi. 2012 Jul 24;92(28):1992-6.
Abstract
The effects of Z-VAD-FMK, a caspase inhibitor, on T lymphocytes and the elicitation of murine ACD were investigated.
3. Radiation-induced cytochrome c release and the neuroprotective effects of the pan-caspase inhibitor z-VAD-fmk in the hypoglossal nucleus. Exp Ther Med. 2014 Feb;7(2):383-388. Epub 2013 Nov 20.
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.
5. Intracochlear perfusion of leupeptin and z-VAD-FMK: influence of antiapoptotic agents on gunshot-induced hearing loss. Eur Arch Otorhinolaryngol. 2011 Jul;268(7):987-93. doi: 10.1007/s00405-011-1487-0. Epub 2011 Jan 19.
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.

Background

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