Z-YVAD-FMK
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Z-YVAD-FMK是一种细胞通透性的、不可逆的caspase-1抑制剂。
在Caco-2细胞中，Z-YVAD-FMK显著降低丁酸对细胞生长的抑制作用。当浓度达到100 μmol/L时，Z-YVAD-FMK完全消除了丁酸的作用。这些结果表明，caspase-1的抑制剂显著改变了caspase级联反应，减弱了丁酸诱导的细胞凋亡效应 [1]。在MyD88缺陷的骨髓树突状细胞中，明矾（Alum）处理诱导caspase-1的激活和IL-1的释放，而Z-YVAD-FMK可以抑制这种效应 [2]。
参考文献：
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. 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
- 2. 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
- 3. 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
- 4. 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
- 5. 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
- 6. Wang X, Li H, et al. "The role of Caspase-1/GSDMD-mediated pyroptosis in Taxol-induced cell death and a Taxol-resistant phenotype in nasopharyngeal carcinoma regulated by autophagy." Cell Biol Toxicol. 2020;10.1007/s10565-020-09514-8. PMID: 31993881
- 7. 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
- 8. 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
- 9. 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
- 10. 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
- 11. Yang D, Zheng X, et al. "Sensing of cytosolic LPS through caspy2 pyrin domain mediates noncanonical inflammasome activation in zebrafish." Nat Commun. 2018 Aug 3;9(1):3052. PMID: 30076291
- 12. Fanfan Xu, Xinghua Qiu, et al. "Effects on IL-1b signaling activation induced by water and organic extracts of fine particulate matter (PM2.5) in vitro" Environmental Pollution 237 (2018) 592e600. PMID: 29525626
- 13. Kalantari P, Morales Y, Met al. "CD209a Synergizes with Dectin-2 and Mincle to Drive Severe Th17 Cell-Mediated Schistosome Egg-Induced Immunopathology." Cell Rep. 2018 Jan 30;22(5):1288-1300. PMID: 29386115
- 14. Ding HG, Deng YY, et al. "Hypercapnia induces IL-1β overproduction via activation of NLRP3 inflammasome: implication in cognitive impairment in hypoxemic adult rats. "J Neuroinflammation. 2018 Jan 5;15(1):4. PMID: 29304864
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验: [1] | |
|
细胞系 |
Caco-2 (ATCC Number HTB-37) |
|
制备方法 |
溶解度有限，若配制更高浓度的溶液，一般步骤如下：请将试管置于37°C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20°C可放置数月。 |
|
反应条件 |
48 h |
|
实验结果 |
Z-YVAD-FMK显著下调Caco-2细胞中丁酸盐诱导的生长抑制。浓度为100 μmol/L的抑制剂完全废除了丁酸盐效应，表明caspase-1抑制剂显著改变caspase级联反应，减少丁酸盐诱导的凋亡效应。 |
| 动物实验: [2] | |
|
动物模型 |
Albino Wistar大鼠 |
|
给药剂量 |
静脉注射caspase抑制剂Z-VAD-FMK的大鼠；1.06 mM，溶于2％DMSO，2 μL |
|
实验结果 |
在暴露于损伤光之前，YVAD将caspase 1的活性降低至51％ ± 34％，但对caspase 3的活性（98％ ± 5％）没有影响。暴露于YVAD的视网膜显示caspase-1活性为66％ ± 33％。这些值的显著性（P <0.02和P <0.004）低于DMSO组。 |
|
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
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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质量控制和MSDS
- 批次：
化学结构
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