Z-YVAD-FMK
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 μmol/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.
- 1. Xueping Li, Jiarui Zhou, et al. "Nucleoside-diphosphate kinase of uropathogenic Escherichia coli inhibits caspase-1-dependent pyroptosis facilitating urinary tract infection." Cell Rep. 2024 Apr 23;43(4):114051. PMID: 38564334
- 2. Madhusoodhanan Suresh Kumar Meena Kumari, Pengyu Liu, et al. "NLRP3 and AIM2 inflammasomes exacerbate the pathogenic Th17 cell response to eggs of the helminth Schistosoma mansoni." bioRxiv. 2024 Mar 13:2024.03.11.584371. PMID: 38559160
- 3. Jiaxin He, Jialin Cui, et al. "Astragaloside IV Attenuates High-Glucose-Induced Impairment in Diabetic Nephropathy by Increasing Klotho Expression via the NF-κB/NLRP3 Axis." J Diabetes Res. 2023 May 22:2023:7423661. PMID: 37261217
- 4. Kempen CG, Deragon MA, et al. "Necroptosis of Lung Epithelial Cells Triggered by Ricin Toxin and Bystander Inflammation." Cell Physiol Biochem 2023 Jan 25;57(1) PMID: 36695077
- 5. Qian Dai, Xiaolin Liu, et al. "Excipient of paclitaxel induces metabolic dysregulation and unfolded protein response." iScience. 2021 Sep 25;24(10):103170. PMID: 34646996
- 6. Shouwen Chen, Peng Jin, et al. "Dual function of a turbot inflammatory caspase in mediating both canonical and non-canonical inflammasome activation." Dev Comp Immunol. 2021 Aug;121:104078. PMID: 33794278
- 7. Peng Zhang, Boyao Lu, et al. "Hyperglycemia accelerates inflammaging in the gingival epithelium through inflammasomes activation." J Periodontal Res. 2021 Aug;56(4):667-678. PMID: 33650689
- 8. Kai J, Yang X, et al. "Oroxylin a promotes PGC-1α/Mfn2 signaling to attenuate hepatocyte pyroptosis via blocking mitochondrial ROS in alcoholic liver disease." Free Radic Biol Med. 2020;153:89-102. PMID: 32289481
- 9. Ding H, Li Y, et al. "Treatment with 7% and 10% CO2 enhanced expression of IL-1β, TNF-α, and IL-6 in hypoxic cultures of human whole blood." J Int Med Res. 2020;48(4):300060520912105. PMID: 32264730
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- 11. Hodges AL, Kempen CG, et al. "TNF Family Cytokines Induce Distinct Cell Death Modalities in the A549 Human Lung Epithelial Cell Line when Administered in Combination with Ricin Toxin." Toxins (Basel). 2019 Aug 1;11(8). pii: E450. PMID: 31374990
- 12. Dong X, Zheng Z, et al. "ACPAs promote IL-1βproduction in rheumatoid arthritis by activating the NLRP3 inflammasome." Cell Mol Immunol. 2019 Mar 25. PMID: 30911117
- 13. Chou X, Ding F, et al. "Sirtuin-1 ameliorates cadmium-induced endoplasmic reticulum stress and pyroptosis through XBP-1s deacetylation in human renal tubular epithelial cells. Arch Toxicol." 2019 Feb 22. PMID: 30796460
- 14. Hua S, Ma M, et al. "Glycyrrhizin attenuates hepatic ischemia-reperfusion injury by suppressing HMGB1-dependent GSDMD-mediated kupffer cells pyroptosis." Int Immunopharmacol. 2019 Mar;68:145-155. PMID: 30634142
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| Storage | Store at -20°C |
| M.Wt | 630.66 |
| Cas No. | 210344-97-1 |
| Formula | C31H39FN4O9 |
| Solubility | ≥31.55 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| 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 |
| SDF | Download SDF |
| Canonical SMILES | COC(C[C@H](NC([C@H](C)NC([C@@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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Caco-2 (ATCC Number HTB-37) |
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Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. |
|
Reaction Conditions |
48 h |
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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]: | |
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Animal models |
Albino Wistar rats |
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Dosage form |
Rats were injected intravenously (2 μL) with caspase inhibitor Z-VAD-FMK (1.06 mM in 2% DMSO) |
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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. |
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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. |
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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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