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Z-YVAD(OMe)-FMK

ALX-260-074

7 citations

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Inhibitor of caspase-1 and -4

Irreversible, cell permeable inhibitor of caspase-1. Inhibits also caspase-4.

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Product Details

Alternative Name	Caspase-1 inhibitor (fluoromethylketone)
Appearance	White to off-white powder.
Formula	C₃₁H₃₉FN₄O₉
MW	630.7
Purity	≥98% (TLC)
Sequence	Z-Tyr-Val-Ala-Asp(OMe)-fluoromethylketone
Solubility	Soluble in DMSO.
Technical Info / Product Notes	The carboxyl groups are OMe ester forms to enhance cell permeability. If purified enzyme is used, esterase should be added for the hydrolysis of the ester groups.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stock solutions should be divided into aliquots and stored at -20°C.
Handling	Packaged under inert gas.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

The colonic pathogen Entamoeba histolytica activates caspase-4/1 that cleaves the pore-forming protein gasdermin D to regulate IL-1β secretion: S. Wang, et al.; PLoS Pathog. 18, e1010415 (2022), Abstract
Interruption of Helicobacter pylori-Induced NLRP3 Inflammasome Activation by Chalcone Derivatives: H.R. Choi, et al.; Biomol. Ther. (Seoul) 29, 410 (2021), Application(s): THP-1 cells treatment, Abstract
A calpain inhibitor protects against fractalkine production in lipopolysaccharide-treated endothelial cells: J. Jang, et al.; Kidney Res. Clin. Pract. 36, 224 (2017), Abstract — Full Text
Increased expression of the NLRP3 inflammasome components in patients with Behçet’s disease: E.H. Kim, et al.; J. Inflamm. (Lond) 12, 41 (2015), Application(s): Cell Culture, qRT-PCR, Abstract — Full Text
Protective effect of a caspase inhibitor in models for cerebral ischemia in vitro and in vivo: C. Wiessner, et al.; Cell Mol. Biol. (Noisy-Le-Grand) 46, 53 (2000), Abstract
Inhibition of ubiquitin-proteasome pathway activates a caspase-3-like protease and induces Bcl-2 cleavage in human M-07e leukaemic cells: X.M. Zhang, et al.; Biochem. J. 340, 127 (1999), Abstract — Full Text
The role of CED-3-related cysteine proteases in apoptosis of cerebellar granule cells: B.A. Eldadah, et al.; J. Neurosci. 17, 6105 (1997), Abstract — Full Text

Datasheet, Manuals, SDS & CofA

Manuals And Inserts

Datasheet

Specific Protocol

Prepare a 10mM stock solution of the caspase inhibitor in high quality DMSO. Add 2µl of this stock solution to 1 ml of culture medium containing cells to give 20µM final concentration. Effective final concentrations are estimated to be 5-20µM. If a particular caspase inhibitor is applied at higher concentrations specificity for an individual caspase or even for the caspase family (>100µM) might be compromised. DMSO concentration above 0.2% may cause cellular toxicity thus masking the effect of the caspase inhibitor. For in vivo experiments extending for 12 to 48 hours, fresh inhibitor may have to be added (injected) due to inactivation by reaction with cysteine protease.

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