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Z-YVAD-FMK Caspase-1 inhibitor

Catalog No.A8955
Size Price Stock Qty
10mM (in 1mL DMSO)
$910.00
In stock
1mg
$160.00
In stock
5mg
$400.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Yang D, Zheng X, et al. "Sensing of cytosolic LPS through caspy2 pyrin domain mediates noncanonical inflammasome activation in zebrafish." Nat Commun. 2018 Aug 3;9(1):3052. PMID:30076291
2.Fanfan Xu, Xinghua Qiu, et al. "Effects on IL-1b signaling activation induced by water and organic extracts of fine particulate matter (PM2.5) in vitro*" Environmental Pollution 237 (2018) 592e600.
3. Kalantari P, Morales Y, Met al. "CD209a Synergizes with Dectin-2 and Mincle to Drive Severe Th17 Cell-Mediated Schistosome Egg-Induced Immunopathology." Cell Rep. 2018 Jan 30;22(5):1288-1300. PMID:29386115
4. Ding HG, Deng YY, et al. "Hypercapnia induces IL-1β overproduction via activation of NLRP3 inflammasome: implication in cognitive impairment in hypoxemic adult rats. "J Neuroinflammation. 2018 Jan 5;15(1):4. PMID:29304864

Quality Control

Chemical structure

Z-YVAD-FMK

Related Biological Data

Z-YVAD-FMK

Related Biological Data

Z-YVAD-FMK

Protocol

Cell experiment [1]:

Cell lines

Caco-2 (ATCC Number HTB-37)

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

48 h

Applications

Z-YVAD-FMK significantly downregulates the growth inhibition induced by butyrate in Caco-2 Cells. Complete abrogation of butyrate’s effect occurs at an inhibitor concentration of 100 μmol/L, indicating that caspase-1 inhibitor significantly alters the caspase cascade, diminishing the butyrate-induced apoptotic effect.

Animal experiment [2]:

Animal models

Albino Wistar rats

Dosage form

Rats were injected intravenously (2 μL) with caspase inhibitor Z-VAD-FMK (1.06 mM in 2% DMSO)

Applications

Immediately before exposure to damaging light, YVAD significantly reduces caspase-1 activity to 51% ± 34% but has no effect on caspase-3 activity (98% ± 5%). Exposed-YVAD retinas showed caspase-1 activities of 66% ± 33%, respectively. These values were significantly (P < 0.02 and P < 0.004, respectively) lower than in the Exposed-DMSO group.

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. Avivi-Green C, Polak-Charcon S, Madar Z, Schwartz B. Different molecular events account for butyrate-induced apoptosis in two human colon cancer cell lines. J Nutr. 2002 Jul;132(7):1812-8.

2. Perche O, Doly M, Ranchon-Cole I. Caspase-dependent apoptosis in light-induced retinal degeneration. Invest Ophthalmol Vis Sci. 2007 Jun;48(6):2753-9.

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Chemical Properties

Cas No. N/A SDF Download SDF
Synonyms N/A
Chemical Name (8S,11S,14S)-methyl 14-(2-fluoroacetyl)-5-(4-hydroxybenzyl)-8-isopropyl-11-methyl-3,6,9,12-tetraoxo-1-phenyl-2-oxa-4,7,10,13-tetraazahexadecan-16-oate
Canonical SMILES COC(C[[email protected]](NC([[email protected]](C)NC([[email protected]@H](NC(C(CC1=CC=C(O)C=C1)NC(OCC2=CC=CC=C2)=O)=O)C(C)C)=O)=O)C(CF)=O)=O
Formula C31H39FN4O9 M.Wt 630.66
Solubility >31.6mg/mL 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Z-YVAD-FMK is a potent cell-permeable and irreversible inhibitor of caspase-1.
In Caco-2 cells, Z-YVAD-FMK significantly decreased the growth inhibition induced by butyrate. Complete abrogation of butyrate’s effect occurred at an inhibitor concentration of 100 mol/L. It is indicated that caspase-1 inhibitor significantly alters the caspase cascade, diminishing the butyrate-induced apoptotic effect [1]. After treated with Alum reflected caspase-1 activation, IL-1-release in cells was blocked by Z-YVAD-FMK. This effect was observed even in MyD88-deficient bone marrow DC [2].
References:
1.Avivi-Green C, Polak-Charcon S, Madar Z, et al. Different molecular events account for butyrate-induced apoptosis in two human colon cancer cell lines. J Nutr. 2002 Jul;132(7):1812-8.
2.Li H, Nookala S, Re F. Aluminum hydroxide adjuvants activate caspase-1 and induce IL-1beta and IL-18 release. J Immunol. 2007 Apr 15;178(8):5271-6.