Z-IETD-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-IETD-FMK是一种caspase 8抑制剂[1]。
Z-IETD-FMK抑制由PHA或anti-CD3/anti-CD28诱导的T细胞增值,而对静息T细胞没有细胞毒性效应。Z-IETD-FMK通过减少CD25的表达,而非影响IL-2的分泌或IFN-γ的产生,从而发挥其抑制效应。已有实验表明,Z-IETD-FMK对正常细胞的生长没有影响。当浓度达到100 μM时,Z-IETD-FMK也可以显著抑制NF-κB的激活[1]。
据报道,除了抑制细胞增殖,Z-IETD-FMK可以抑制TRAIL介导的细胞凋亡。在HCT116和SW480细胞中,Z-IETD-FMK可以保护procaspases 9、2和3以及PARP[2]。
参考文献:
[1] C. P. Lawrence, S.C. Chow. Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties. Toxicology and Applied Pharmacology. 2012, 265: 103-112.
[2] Nesrin ?z?ren, Kunhong Kim, Timothy F. Burns, et al. The caspase 9 inhibitor Z-LEHD-FMK protects human liver cells while permitting death of cancer cells exposed to tumor necrosis factor-related apoptosis-inducing ligand. Cancer Research. 2000, 60: 6259-6265.
- 1. Yuhang Miao, Tao Ding, et al. "The Yeast and Hypha Phases of Candida kruseiInduce the Apoptosis of Bovine Mammary Epithelial Cells via Distinct Signaling Pathways." Animals (Basel). 2023 Oct 15;13(20):3222. PMID: 37893947
- 2. Xin Ming, Huan Chen, et al. "Porcine Enteric Coronavirus PEDV Induces the ROS-ATM and Caspase7-CAD-γH2AX Signaling Pathways to Foster Its Replication." Viruses. 2022 Aug 15;14(8):1782. PMID: 36016404
- 3. Jingying Wu, Siming Lin, et al. "TNF-α contributes to sarcopenia through caspase-8/caspase-3/GSDME-mediated pyroptosis." Research Square. September 23rd, 2022.
- 4. Xin Ming, Huan Chen, et al. "Porcine Enteric Coronavirus PEDV Induces the ROS-ATM and Caspase7-CAD-γH2AX Signaling Pathways to Foster Its Replication." Viruses. 2022 Aug 15;14(8):1782. PMID: 36016404
- 5. Jiamin Yi, Jiangling Peng, et al. "Degradation of Host Proteins and Apoptosis Induced by Foot-and-Mouth Disease Virus 3C Protease." Pathogens. 2021 Nov 30;10(12):1566. PMID: 34959521
- 6. Jesse R Poganik, Kuan-Ting Huang, et al. "Wdr1 and cofilin are necessary mediators of immune-cell-specific apoptosis triggered by Tecfidera." Nat Commun. 2021 Sep 30;12(1):5736. PMID: 34593792
- 7. Jiangqi Zhao, Xuyan Huang, et al. "Toll-like receptor 3 is an endogenous sensor of cell death and a potential target for induction of long-term cardiac transplant survival." Am J Transplant. 2021 Oct;21(10):3268-3279. PMID: 33784431
- 8. Melissa S Phuong, Rafael E Hernandez, et al. "Impairment in inflammasome signaling by the chronic Pseudomonas aeruginosa isolates from cystic fibrosis patients results in an increase in inflammatory response." Cell Death Dis. 2021 Mar 4;12(3):241. PMID: 33664232
- 9. Yang Pan, Yu-miao Pan, et al. "MicroRNA-98 ameliorates doxorubicin-induced cardiotoxicity via regulating caspase-8 dependent Fas/RIP3 pathway." Environ Toxicol Pharmacol. 2021 Jul;85:103624. PMID: 33617954
- 10. Claire Reynolds-Peterson, Dylan J Ehrbar, et al. "Sensitization of Airway Epithelial Cells to Toxin-Induced Death by TNF Superfamily Cytokines." Methods Mol Biol. 2021;2248:19-42. PMID: 33185865
- 11. Nan Jiang, Zhidong Li, et al. "Laquinimod exerts anti-inflammatory and antiapoptotic effects in retinal ischemia/reperfusion injury." Int Immunopharmacol. 2020 Nov;88:106989. PMID: 33182069
- 12. HAIDONG SUN, HUAJIE ZONG, et al. " 2‑Hydroxypropyl‑β‑cyclodextrin blocks autophagy flux and triggers caspase‑8‑mediated apoptotic cascades in HepG2 cells." Mol Med Rep. 2020 Sep;22(3):1901-1909. PMID: 32705246
- 13. Chen Z, Xu G, et al. "Lobaplatin induces pyroptosis through regulating cIAP1/2, Ripoptosome and ROS in nasopharyngeal carcinoma." Biochem Pharmacol. 2020;177:114023. PMID: 32413426
- 14. Zhao M, Duan X, et al. "A Novel Role for PX, a Structural Protein of Fowl Adenovirus Serotype 4 (FAdV4), as an Apoptosis-Inducer in Leghorn Male Hepatocellular Cell." Cell. Viruses. 2020;12(2):E228. PMID: 32085479
- 15. Jiao C, Chen W, et al. "Ganoderma lucidum spore oil induces apoptosis of breast cancer cells in vitro and in vivo by activating caspase-3 and caspase-9." J Ethnopharmacol. 2019 Oct 3:112256. PMID: 31586690
- 16. 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
- 17. Luo Q, Yang D, et al. "Role of the Death Receptor and Endoplasmic Reticulum Stress Signaling Pathways in Polyphyllin I-Regulated Apoptosis of Human Hepatocellular Carcinoma HepG2 Cells." Biomed Res Int. 2018 Dec 25;2018:5241941. PMID: 30671458
- 18. Yazhong Ge, Qing Gao, et al . "Su Yang Decoction induces human colon carcinoma cell apoptosis by activating caspases." Oncology letters.October 26, 2018.
- 19. Gan I, Jiang J, et al. "Mitochondrial permeability regulates cardiac endothelial cell necroptosis and cardiac allograft rejection." Am J Transplant. 2018 Sep 11. PMID: 30203531
- 20. Rijal D, Ariana A, et al. "Differentiated Macrophages Acquire a Pro-Inflammatory and Cell Death-Resistant Phenotype Due to Increasing XIAP and P38-mediated inhibition of RipK1." J Biol Chem. 2018 Jun 13. pii:jbc.RA118.003614. PMID: 29899110
- 21. Song F, Yu X, et al. "Caspase-3 Inhibition Attenuates the Cytopathic Effects of EV71 Infection. Front Microbiol." 2018 Apr 26;9:817. PMID: 29755438
- 22. Wang JN, Zhang ZR, et al. "Acetyl-macrocalin B, an ent-kaurane diterpenoid, initiates apoptosis through the ROS-p38-caspase 9-dependent pathway and induces G2/M phase arrest via the Chk1/2-Cdc25C-Cdc2/cyclin B axis in non-small cell lung cancer." Cancer Biol Ther. 2018 Jul 3;19(7):609-621. PMID: 29565730
- 23. Tabtieng T, Degterev A, et al. "Caspase-dependent suppression of type I interferon signaling promotes KSHV lytic replication." J Virol. 2018 Mar 7. pii:JVI.00078-18. PMID: 29514903
- 24. Wang J, Zhang Z, et al. "Rabdocoestin B exhibits antitumor activity by inducing G2/M phase arrest and apoptosis in esophageal squamous cell carcinoma." Cancer Chemother Pharmacol. 2018 Mar;81(3):469-481. PMID: 29308536
- 25. Dikchha Rijal. "Cell death signaling complexes during macrophage differentiation." University of Ottawa, 2017.
- 26. Ardeshir Ariana,Faculty of Medicine, et al, "Dissection of TLR4-induced necroptosis using specific inhibitors of endocytosis and p38 MAPK." University of Ottawa, 2017.
- 27. Chen Y, Sun M, et al, "SM-1,a novel PAC-1 derivative, activates procaspase-3 and causes cancer cell apoptosis." Cancer Chemother Pharmacol. 2016 Sep;78(3):643-54. PMID: 27488460
- 28. Tian, Chongchong, et al. "A novel dual EGFR/HER2 inhibitor KU004 induces cell cycle arrest and apoptosis in HER2-overexpressing cancer cells." Apoptosis 20.12 (2015): 1599-1612. PMID: 26437915
Storage | Store at -20°C |
M.Wt | 654.68 |
Cas No. | 210344-98-2 |
Formula | C30H43FN4O11 |
Synonyms | Benzyloxycarbonyl-Ile-Glu(OMe)-Thr-Asp(OMe)-fluoromethylketone, Z-Ile-Glu(OMe)-Thr-Asp(OMe)-FMK |
Solubility | ≥32.73 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | methyl 5-[[1-[(5-fluoro-1-methoxy-1,4-dioxopentan-3-yl)amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-[[3-methyl-2-(phenylmethoxycarbonylamino)pentanoyl]amino]-5-oxopentanoate |
SDF | Download SDF |
Canonical SMILES | CCC(C)C(C(=O)NC(CCC(=O)OC)C(=O)NC(C(C)O)C(=O)NC(CC(=O)OC)C(=O)CF)NC(=O)OCC1=CC=CC=C1 |
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 |
纯化的CD4+和CD8+ T细胞 |
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℃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℃可放置数月。 |
反应条件 |
24 h |
实验结果 |
使用[3H]-胸苷掺入测定T细胞增殖。z-IETD-FMK(100 μM)抑制T细胞增殖。在100 μM的z-IETD-FMK存在下,活化后约9%的对照活化T细胞摄取PI,细胞死亡增加至23%。此外,100 μM z-IETD-FMK降低活化T细胞中p65的核易位。 |
动物实验: [2] | |
动物模型 |
SHIP1-/- (CD45.1)小鼠 |
给药剂量 |
5 mg/kg,每周三次,持续3周 |
实验结果 |
与载体对照相比,Z-IETD-FMK处理的小鼠的小肠和肺中的解剖病理学显著减少。在Z-IETD-FMK处理的SHIP1-/-宿主的小肠和肺中CD3+T细胞数目显著恢复,而载体处理的SHIP1-/-宿主的T细胞缺乏。 |
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. Lawrence CP, Chow SC. Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties. Toxicol Appl Pharmacol. 2012 Nov 15;265(1):103-12. 2. Park MY, Srivastava N, Sudan R et al. Impaired T-cell survival promotes mucosal inflammatory disease in SHIP1-deficient mice. Mucosal Immunol. 2014 Nov;7(6):1429-39. |
描述 | Z-IETD-FMK是一种特异性的caspase 8抑制剂。 | |||||
靶点 | caspase 8 | |||||
IC50 |
质量控制和MSDS
- 批次: