| Identification | Back Directory | [Name]
CASPASE-8 INHIBITOR II | [CAS]
210344-98-2 | [Synonyms]
Z-IETD-FMK
Z-IETD-FMK?, >98%
Z-IE(OME)TD(OME)-FMK
CASPASE-8 INHIBITOR II
GRANZYME B INHIBITOR III
Z-ILE-GLU(OME)-THR-ASP(OME)-FMK
Z-IE(OME)TD(OME)-FLUOROMETHYLKETONE
CASPASE-8 INHIBITOR;Z-IE(OME)TD(OME)-FMK
Z-ILE-GLU(OME)-THR-ASP(OME)-FLUOROMETHYLKETONE
Z-ILE-GLU(OME)-THR-DL-ASP(OME)-FLUOROMETHYLKETONE
CASPASE-3 PROCESSING ENZYME INHIBITOR (FLUOROMETHYLKETONE)
BENZYLOXYCARBONYL-ILE-GLU(OME)-THR-ASP(OME)-FLUOROMETHYLKETONE
L-Threoninamide, N-[(phenylmethoxy)carbonyl]-L-isoleucyl-L-α-glutamyl-N-[(1S)-3-fluoro-1-(2-methoxy-2-oxoethyl)-2-oxopropyl]-, methyl ester | [Molecular Formula]
C30H43FN4O11 | [MDL Number]
MFCD03490491 | [MOL File]
210344-98-2.mol | [Molecular Weight]
654.68 |
| Chemical Properties | Back Directory | [Boiling point ]
925.7±65.0 °C(Predicted) | [density ]
1.247±0.06 g/cm3(Predicted) | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
Soluble in DMSO | [form ]
Powder | [pka]
11.12±0.46(Predicted) | [color ]
White to light yellow | [Sequence]
Z-Ile-Glu-Thr-Asp-FMK |
| Hazard Information | Back Directory | [Uses]
A potent, cell-permeable, and irreversible inhibitor of caspase-8 and granzyme B. Effectively inhibits influenza virus-induced apoptosis in HeLa cells. Also inhibits granzyme B. | [Biological Activity]
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]. | [in vivo]
Pharmacological inhibition of caspase-8 by z-IETD-FMK robustly reduces tumor growth and this is closely associated with a reduction in the release of pro-inflammatory cytokines, IL-6, TNF-α, IL-18, IL-1α, IL-33, but not IL-1β. Furthermore, inhibition of caspase-8 reduces the recruitment of innate suppressive cells, such as myeloid-derived suppressor cells, but not of regulatory T cells to lungs of tumor-bearing mice[4]. | [target]
caspase 8 | [IC 50]
Caspase-8 | [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 ?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. |
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