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product name Z-IETD-FMK


Description: Z-IETD-FMK is a specific Caspase-8 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.

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



Molecular Weight (MW)

654.68
Formula

C30H43FN4O11
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
Solubility (In vivo)

 
Chemical Name

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

other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404898

Z-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 Vivo In 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 model T. cruzi-infected mice
Formulation & Dosage  DMSO/PBS (15%); 0.4 mg/3 days
Reference [1] Silva EM, et al. J Immunol. 2005, 174(10), 6314-6321.  [2] Monnier PP, et al. J Neurosci. 2011, 31(29), 10494-10505.

Amcasertib