CASPASE-8 INHIBITOR II

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

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.