Ac-YVAD-cmk
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Cat.code:
inh-yvad
- Documents
ABOUT
Caspase-1 inhibitor
Ac-YVAD-cmk is a potent and irreversible inhibitor of the inflammatory enzyme caspase-1 [1]. Caspase-1, also known as IL-1 converting enzyme (ICE), is a cysteine protease that cleaves the precursors of the pro-inflammatory cytokines interleukin-1β (IL-1β) and IL-18, as well as the gasdermin D (GSDMD) pore-forming protein [2].
Mode of action:
Ac‑YVAD‑cmk is a tetrapeptide sequence based on the target sequence of caspase-1 in pro‑IL‑1β (YVHD) [1, 3]. This drug was described as blocking inflammatory cell death in experimental models [4]. Additional reports showed that Ac‑YVAD‑cmk effectively blocks inflammasome activation and that it displays anti-inflammatory, anti-apoptotic, and anti-pyroptotic effects [5, 6].
Key features:
- Potent and irreversible inhibitor of caspase-1
- Weak inhibitor of caspase-4 and caspase-5 (human paralogs of caspase-1)
- InvitroFit™ grade: each lot is highly pure (≥97%) and functionally tested
Download our Practical guide on Inflammasomes
References
1. Garcia-Calvo M. et al., 1998. Inhibition of human caspases by peptide-based and macromolecular inhibitors. J Biol Chem. 273(49):32608-13.
2. Man S.M. & Kanneganti T.D., 2016.Converging roles of caspases in inflammasome activation, cell death and innate immunity. Nat. Rev. Immunol. 16(1):7-21.
3. Talanian, R.V., et al., 1997. Substrate specificities of caspase family proteases. J Biol Chem. 272(15):9677‑82.
4. Schierle GS. et al., 1999. Caspase inhibition reduces apoptosis and increases survival of nigral transplants. Nat Med. 5(1):97-100.
5. Van Opdenbosch N. et al., 2014. Activation of the NLRP1b inflammasome independently of ASC-mediated caspase-1 autoproteolysis and speck formation. Nat Commun. 5:3209.
6. Zhang Y. et al, 2014. Involvement of inflammasome activation in lipopolysaccharide-induced mice depressive-like behaviors. CNS Neurosci Ther. 20(2):119-24.
All products are for research use only, and not for human or veterinary use.
InvitroFit™
InvitroFit™ is a high-quality standard specifically adapted for in vitro studies of inhibitors. InvitroFit™ products are highly pure (≥95%) and guaranteed free of bacterial contamination, as confirmed using HEK Blue™ TLR2 and HEK Blue™ TLR4 cellular assays. Each lot is rigorously tested for functional activity using validated (or proprietary) cellular models. This grade ensures reliability and reproducibility for your research applications.
SPECIFICATIONS
Specifications
C24H33ClN4O8
50 mg/ml (92.4 mM) in DMSO
0.1–30 μg/ml for cell culture assays
Negative (tested using EndotoxDetect™ assay)
In vitro Inflammasome cellular assays
Each lot is functionally tested and validated using cellular assays.
CONTENTS
Contents
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Product:Ac-YVAD-cmk
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Cat code:inh-yvad
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Quantity:5 mg
Ac-YVAD-cmk is provided as a translucent film.
Shipping & Storage
- Shipping method: Room temperature
- -20°C
Storage:
Details
Caspase-1 in inflammasome responses:
Rapid responses to infections and tissue damages are largely mediated by the inflammasomes. The formation of these cytosolic signaling platforms occurs according to a consensual two-step model. The priming step (step 1) induces the transcription of pro-IL-1β. The activation step (step 2) triggers the multimerization of the activated inflammasome sensor with the ASC adaptor and pro-caspase-1. This assembly permits caspase-1 self-activation, which in turn induces the maturation of IL-1β and IL-18 cytokines. Activated caspase-1 also cleaves the N-terminal fragment of GSDMD, which accumulates to form pores at the cell membrane. These pores allow the unconventional secretion of IL-1β and IL-18, and in the absence of membrane repair, their accumulation leads to pyroptosis [1].
1. Man S.M. & Kanneganti T.D., 2016.Converging roles of caspases in inflammasome activation, cell death and innate immunity. Nat. Rev. Immunol. 16(1):7-21.
Chemical structure of Ac-YVAD-cmk:
DOCUMENTS
Documents
Technical Data Sheet
Safety Data Sheet
Validation Data Sheet
Certificate of analysis
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