Name: Z-IETD-FMK
Price: 866.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Z-IETD-FMK is an inhibitor of caspase 8 [1].
    Z-IETD-FMK inhibits T cell proliferation induced by PHA or anti-CD3 plus anti-CD28 without toxicity of resting T cells. The mechanism of this inhibition of Z-IETD-FMK has been proved not through the effect on IL-2 secretion or IFN-γ production but the decrease of CD25 expression. Experiments show that Z-IETD-FMK has no effect on normal cell growth when there is no activation signal. Z-IETD-FMK has also been found to significantly inhibit NF-κB activation when the concentration is 100μM [1].
    Apart from the ability of inhibiting cell proliferation, Z-IETD-FMK is reported to inhibit TRAIL-mediated killing in cells. It protects the procaspases 9, 2, and 3, and protects PARP to a similar extent in both HCT116 and SW480 cells [2].
    
    [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 Özören, 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.
- Properties
  - Alternative Name
    
    Benzyloxycarbonyl-Ile-Glu(OMe)-Thr-Asp(OMe)-fluoromethylketone, Z-Ile-Glu(OMe)-Thr-Asp(OMe)-FMK; 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
    
    CAS Number
    
    210344-98-2
    
    Molecular Formula
    
    C30H43FN4O11
    
    Molecular Weight
    
    654.68
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥32.73 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. 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
    2. 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
    3. 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
    4. 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
    5. 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
    6. 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
    7. 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
    8. 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
    9. 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
    10. Yazhong Ge, Qing Gao, et al . "Su Yang Decoction induces human colon carcinoma cell apoptosis by activating caspases." Oncology letters.October 26, 2018.
    11. 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
    12. 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
    13.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
    14. 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
    15. 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
    16. 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
    17. Dikchha Rijal. "Cell death signaling complexes during macrophage differentiation." University of Ottawa, 2017.
    18. Ardeshir Ariana,Faculty of Medicine, et al, "Dissection of TLR4-induced necroptosis using specific inhibitors of endocytosis and p38 MAPK." University of Ottawa, 2017.
    19. 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
    20. 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

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