CASPASE-8 INHIBITOR II

Product NameCASPASE-8 INHIBITOR II
CAS210344-98-2
MFC30H43FN4O11
MW654.68
EINECS
MOL FileMol File

Chemical Properties

Boiling point	925.7±65.0 °C(Predicted)
Density	1.247±0.06 g/cm3(Predicted)
storage temp.	under inert gas (nitrogen or Argon) at 2-8°C
solubility	Soluble in DMSO
pka	11.12±0.46(Predicted)
form	Powder
color	White to light yellow
Sequence	Z-Ile-Glu-Thr-Asp-FMK
InChIKey	PHLCQASLWHYEMX-DEKIMQJDSA-N
SMILES	[C@@H]([C@@H](C)CC)(NC(=O)OCC1C=CC=CC=1)C(=O)N[C@@H](CCC(=O)OC)C(=O)N[C@@H]([C@H](O)C)C(=O)N[C@H](C(=O)CF)CC(=O)OC

Usage And Synthesis

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 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.

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