Irreversible, cell permeable inhibitor of caspase-1. Inhibits also caspase-4.
Product Details
| Alternative Name: | Caspase-1 inhibitor (fluoromethylketone) |
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| Sequence: | Z-Tyr-Val-Ala-Asp(OMe)-fluoromethylketone |
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| Formula: | C31H39FN4O9 |
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| MW: | 630.7 |
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| Purity: | ≥98% (TLC) |
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| Appearance: | White to off-white powder. |
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| Solubility: | Soluble in DMSO. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stock solutions should be divided into aliquots and stored at -20°C. |
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| Handling: | Packaged under inert gas. |
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| 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. |
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| 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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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
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
