Z-WEHD-FMK

Names

[ Name ]:
Z-WEHD-FMK

[Synonym ]:
Z-WE(OMe)HD(OMe)-FMK
Z-Trp-Glu(OMe)-His-Asp(OMe)-FMK
Z-Trp-Glu(OMe)-His-Asp(OMe)-Fluoromethylketone
Z-WEHD-FMK

Biological Activity

[Description]:

Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis[1][2][4].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> Caspase

Signaling Pathways >> Metabolic Enzyme/Protease >> Cathepsin

[Target]

Caspase-1

[In Vitro]

Z-WEHD-FMK (80 μM; 9 hours) elicits a near-complete blockage of C. trachomatis-induced cleavage of golgin-84 and increases GM130 expression in cells[1]. Z-WEHD-FMK (30 min before being exposed to E. piscicida) effectively inhibits 0909I E. piscicida induced ZF4 cells cytotoxicity and pyroptotic morphology. And in addition, it also inhibits the cytotoxicity induced by cytosolic LPS delivery[2]. Z-WEHD-FMK (20 μM;18-24 hours following Cr3+,Ni2+, and Co2+) significantly induces a decrease of 76% to 86% in IL-1β release with 200 to 400 ppm Cr3+, it also induces a decrease of 35% to 45% with 48 ppm Ni2+ or higher, Finally, this caspase-1 inhibitor induced a decrease with 6 ppm Co2+, down to a level below the detection threshold, and a decrease of 40% to 48% with 12 to 24 ppm Co2+ in bone marrow-derived macrophages (BMDM)[3]. Western Blot Analysis[1] Cell Line: C. trachomatis- or mock-infected HeLa cells Concentration: 80 μM Incubation Time: 9 hours Result: Increased golgin-84 and GM130 expression. Cell Viability Assay[2] Cell Line: Mycoplasma free-ZF4 cells Concentration: Incubation Time: 30 min before being exposed to E. piscicida Result: Inhibited ZF4 cells cytotoxicity and pyroptotic morphology.

[References]

[1]. Kamada S, et al. Caspase-4 and caspase-5, members of the ICE/CED-3 family of cysteine proteases, are CrmA-inhibitable proteases.Cell Death Differ. 1997 Aug;4(6):473-8.

[2]. Yang D, et al. Sensing of cytosolic LPS through caspy2 pyrin domain mediates noncanonical inflammasome activation in zebrafish.Nat Commun. 2018 Aug 3;9(1):3052.

[3]. Ferko MA, et al. Effects of metal ions on caspase-1 activation and interleukin-1β release in murine bone marrow-derived macrophages.PLoS One. 2018 Aug 23;13(8):e0199936.

[4]. Newman ZL, et al. CA-074Me protection against anthrax lethal toxin.Infect Immun. 2009 Oct;77(10):4327-36.