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    Z-IETD-FMK
    Z-IETD-FMK

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0030
    CAS #: 210344-98-2Purity ≥98%

    Description: Z-IETD-FMK (also known as Z-IE(OMe)TD(OMe)-FMK) is a novel, specific, selective, irreversible and cell permeable Caspase-8/9 inhibitor. 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. 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.

    References: Toxicol Appl Pharmacol. 2012 Nov 15;265(1):103-12; Cancer Res. 2000 Nov 15;60(22):6259-65.


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    Molecular Weight (MW)654.68
    FormulaC30H43FN4O11
    CAS No.210344-98-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 91 mg/mL (138.99 mM)
    Water:<1 mg/mL (slightly soluble or insoluble)
    Ethanol: <1 mg/mL
    Other info

    Synonym: Z-IE(OMe)TD(OMe)-FMK; Granzyme B Inhibitor III; Z-IETD-FMK; Z-Ile-Glu(OMe)-Thr-Asp(OMe)-CH₂F.

    Chemical Name: (5S,8S,11S,14S)-5-((S)-sec-butyl)-8-(2-carboxyethyl)-14-(2-fluoroacetyl)-11-((R)-1-hydroxyethyl)-3,6,9,12-tetraoxo-1-phenyl-2-oxa-4,7,10,13-tetraazahexadecan-16-oic acid

    InChi Key: CTXDBLYOEUERAT-VUVYEONESA-N

    InChi Code: InChI=1S/C28H39FN4O11/c1-4-15(2)23(33-28(43)44-14-17-8-6-5-7-9-17)26(41)30-18(10-11-21(36)37)25(40)32-24(16(3)34)27(42)31-19(12-22(38)39)20(35)13-29/h5-9,15-16,18-19,23-24,34H,4,10-14H2,1-3H3,(H,30,41)(H,31,42)(H,32,40)(H,33,43)(H,36,37)(H,38,39)/t15-,16+,18-,19-,23-,24-/m0/s1

    SMILES Code: O=C(O)C[C@@H](C(CF)=O)NC([C@H]([C@H](O)C)NC([C@H](CCC(O)=O)NC([C@H]([C@@H](C)CC)NC(OCC1=CC=CC=C1)=O)=O)=O)=O

    Chemical NameL-Threoninamide, N-[(phenylmethoxy)carbonyl]-L-isoleucyl-L-α-glutamyl-N-[(1S)-3-fluoro-1-(2-methoxy-2-oxoethyl)-2-oxopropyl]-, methyl ester


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    In VitroZ-IETD-FMK, which inhibits the cleavage of caspase-8 and partially inhibits the cleavage of caspase-3 and PARP, prevents the execution of apoptosis in retinal cells exposed to different apoptotic stimuli. Z-IETD-FMK (50 μM) reduces ceramide-induced cardiomyocyte death and significantly inhibits the activation of caspase 3.
    In VivoIn vivo, inhibition of caspase-8 by Z-IETD-FMK reduces memory/activated CD4 and CD8 T cells, and increases susceptibility to T. cruzi infection. Z-IETD-FMK promotes neuronal survival and regeneration of injured retinal ganglion cells after CNS injuries.
    Animal modelT. cruzi-infected mice
    Formulation & Dosage DMSO/PBS (15%); 0.4 mg/3 days
    References[1] Silva EM, et al. J Immunol. 2005, 174(10), 6314-6321.  [2] Monnier PP, et al. J Neurosci. 2011, 31(29), 10494-10505.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    Z-IETD-FMK

     

    Z-IETD-FMK

     

    Z-IETD-FMK

    Caspase-8 and caspase-3 processing in newly activated T cells without apoptotic phenotype. Toxicol Appl Pharmacol. 2012 Nov 15;265(1):103-12. 



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