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Z-VAD-FMK

Z-VAD-FMK

Catalog No.

A1902

pan-caspase inhibitor

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Grouped product items
Size	Price	Stock
10mM (in 1mL DMSO)	$171.00	In stock
1mg	$61.00	In stock
5mg	$165.00	In stock
10mg	$275.00	In stock
25mg	$440.00	In stock

For scientific research use only and should not be used for diagnostic or medical purposes.

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Background
Product Citation
Chemical Properties
Protocol
Biological Activity
Quality Control

Background

Z-VAD-FMK (CAS 187389-52-2) is a cell-permeable inhibitor targeting ICE-like proteases (caspases), enzymes that mediate apoptosis. It selectively prevents apoptosis triggered by diverse stimuli, as demonstrated in THP.1 cells, and inhibits Fas-mediated apoptosis in Jurkat T cells. Mechanistically, Z-VAD-FMK suppresses apoptosis by blocking activation of pro-caspase CPP32 rather than directly inhibiting the proteolytic activity of activated CPP32 enzyme, thereby preventing the caspase-dependent formation of large DNA fragments. Due to its specificity, Z-VAD-FMK serves as an essential tool in apoptosis-related signal transduction research.

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

Product Citation

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Chemical Properties

Storage	Store at -20°C
M.Wt	467.49
Cas No.	187389-52-2
Formula	C₂₂H₃₀FN₃O₇
Synonyms	Benzyloxycarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone,Z-Val-Ala-Asp(OMe)-FMK
Solubility	≥23.37 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Chemical Name	methyl (3S)-5-fluoro-3-[[(2S)-2-[[(2S)-3-methyl-2-(phenylmethoxycarbonylamino)butanoyl]amino]propanoyl]amino]-4-oxopentanoate
SDF	Download SDF
Canonical SMILES	CC(C)C(C(=O)NC(C)C(=O)NC(CC(=O)OC)C(=O)CF)NC(=O)OCC1=CC=CC=C1
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Kinase experiment [1]:
Preventing the processing of CPP32 to its active form	Z-VAD-FMK inhibits apoptosis by inhibiting the activation of CPP32, which presumably blocked the process by interfering directly with the processing of CPP32.
Cell experiment [2]:
Cell lines	Human CD4+ (~ 97%) and CD8+ T (~ 98%) cells
Preparation method	The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.
Reaction Conditions	24 h
Applications	Z-VAD-FMK dose-dependently inhibited T cell proliferation mediated through the co-stimulation with anti-CD3 and anti-CD28. Z-IETD-FMK was less effective at 25 and 50 μM, but inhibited T cell proliferation at the 100 μM concentration.
Animal experiment [3]:
Animal models	C57BL mice
Dosage form	1.25 mM, ear provocation
Applications	The right ear swelling degree, weight differences and thickness between two ears in the 1.25 mM Z-VAD-FMK group were significantly lower than those of the negative control (NC). The levels of INF-γ and IL-2 in the ear skin lesions, the mean intensity of BrdU in T lymphocytes, and the percent of activation markers-positive T lymphocytes were all lower than those of NC.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: [1]. Slee EA1, Zhu H, Chow SC 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):21-4. [2]. Lawrence CP1, 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. [3]. Li YY, Yan CL. 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.

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