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Caspase-8 Inhibitor Z-IETD-FMK
Novel and selective caspase-8 inhibitor

Catalog No.B4096
Size Price Stock Qty
100 µl (2 mM)
$125.00
In stock
20 µl (10 mM)
$125.00
In stock

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Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Caspase-8 Inhibitor Z-IETD-FMK

Biological Activity

Description Z-IETD-FMK is a specific inhibitor of caspase 8
Targets caspase 8          
IC50            

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Chemical Properties

Cas No. N/A SDF Download SDF
Chemical Name (Z)-2-((Z)-(2-((E)-((benzyloxy)(hydroxy)methylene)amino)-1-hydroxy-3-methylpentylidene)amino)-N-((Z)-1-((5-fluoro-1-methoxy-1,4-dioxopentan-3-yl)imino)-1,3-dihydroxybutan-2-yl)-5-methoxy-5-oxopentanimidic acid
Canonical SMILES CCC(C(/N=C(OCC1=CC=CC=C1)\O)/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(C(CF)=O)CC(OC)=O)C(O)C)CCC(OC)=O)C
Formula C30H43FN4O11 M.Wt 654.68
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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].

References:
[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.