Z-VAD-FMK
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Cat.code:
tlrl-vad
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ABOUT
Caspase-1 inhibitor
Z-VAD-FMK is a cell-permeable pan-caspase inhibitor [1, 2]. It potently inhibits human caspase-1 to -10 with the exception of caspase-2 [3]. It also inhibits murine caspases, notably caspase-1, caspase-3, and caspase-11, the ortholog of human caspase-4 and -5 [4, 5]. Caspases are a family of cysteine proteases that are centrally involved in cell death and inflammation responses [6, 7].
Mode of action:
Z-VAD-FMK inhibits caspases by irreversibly binding to their catalytic site [1]. By inhibiting the activity of multiple caspases, Z-VAD-FMK can block many different biological processes including inflammasome activation and the induction of apoptosis leading to increased cell survival in many different cell types [2-5]. Interestingly, It has been shown that Z-VAD‑FMK administration can significantly reduce inflammation and lethality in an experimental model of endotoxic shock [5]. To conclude, this broad-spectrum inhibitor is a useful tool for studying the role of caspases in inflammation and cell death.
Key features:
- Broad-spectrum caspase inhibitor
- Potent inhibitor of caspase-dependent inflammasomes
- Blocks the induction of apoptosis
- InvitroFit™ grade: each lot is highly pure (≥95%) and functionally tested
Download our Practical guide on Inflammasomes
References:
1. Slee EA. et al., 1996. Benzyloxycarbonyl-Val-Ala-Asp (OMe) fluoromethylketone (Z-VAD.FMK) inhibits apoptosis by blocking the processing of CPP32. Biochem J. 315 ( Pt 1):21-4.
2. Li X. et al., 2019. The caspase inhibitor Z-VAD-FMK alleviates endotoxic shock via inducing macrophages necroptosis and promoting MDSCs-mediated inhibition of macrophages activation. Front Immunol. 10:1824.
3. Chauvier D. et al., 2007. Broad-spectrum caspase inhibitors: from myth to reality? Cell Death Differ. 14:387-91.
4. Guey B. et al., 2014. Caspase-1 autoproteolysis is differentially required for NLRP1b and NLRP3 inflammasome function. PNAS 11(48):17254-9.
5. Py B.F. et al., 2014. Caspase-11 controls interleukin-1β release through degradation of TRPC1. Cell Rep. 6: 1122–8.
6. Van Opdenbosch N. & Lamkanfi M. et al., 2019. Caspases in Cell Death, Inflammation, and Disease. Immunity. 50(6):1352-1364.
7. Tsuchiya K. et al., 2019. Caspase-1 initiates apoptosis in the absence of gasdermin D. Nat Commun. 10(1):2091.
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 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
C22H30FN3O7
10 mg/ml (20 mM) in DMSO
10 μg/ml (20 μM) 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:Z-VAD-FMK
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Cat code:tlrl-vad
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Quantity:1 mg
Z-VAD-FMK is provided as a translucent film.
Shipping & Storage
- Shipping method: Room temperature
- -20°C
- Avoid repeated freeze-thaw cycles
Storage:
Caution:
Details
Caspases in inflammation & cell death:
The caspase enzymes are a family of cytosolic proteases involved in the regulation of inflammation and cell death [1, 2]. They can be divided into inflammatory caspases (such as caspases-1, -4, -5, and -12 in humans and caspases-1, -11, and -12 in mice) and apoptotic caspases (such as caspases-2, -3, -6, -7, -8, -9, and -10) [3].
Notably, caspase-1 plays a crucial role in the control of inflammation. Its activity is regulated by a multi-protein complex known as the inflammasome, inflammasome activation drives oligomerization and self-activation of caspase-1. Upon activation, caspase-1 processes the inflammatory cytokines, interleukin-1β (IL-1β) and IL-18, and Gasdermin-D, promoting inflammation and pyroptosis, a form of cell death.
1. Van Opdenbosch N. & Lamkanfi M. et al., 2019. Caspases in Cell Death, Inflammation, and Disease. Immunity. 50(6):1352-1364.
2. Tsuchiya K.et al., 2019. Caspase-1 initiates apoptosis in the absence of gasdermin D. Nat Commun. 10(1):2091.
3. Shalini M. et al., 2015. Old, new and emerging functions of caspases. Cell Death Differ. 22:526-39.
Chemical structure of Z-VAD-FMK:
DOCUMENTS
Documents
Technical Data Sheet
Validation Data Sheet
Safety Data Sheet
Certificate of analysis
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