Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

Primary TargetLTA4

General description

A cell-permeable benzylphenyl-thiazolamine compound that selectively inhibits against the leukotriene (LT) A₄ epoxide hydrolase activity of LTA4H by occupying the same hydrophobic tunnel (K_i = 2.3 µM) targeted by LTA₄ Ω-end, displaying much reduced potency against LTA4H aminopeptidase activity (% inhibition/[ARM1] = 0/100 µM & 35/1 mM; Substrate = 800 µM Pro-Gly-Pro) coordinated by E296 and the catalytic site Zn²⁺ at the adjacent hydrophilic peptide substrate-binding cavity. Shown to inhibit A23187- (Cat. Nos. 100105 & 100106) induced LTB₄ production in primary human polymorphonuclear neutrophil (PMN) cultures (IC₅₀ = 0.5 µM; ARM1 added 10 min prior to 5 min stimulation by 2.5 µM A23187). Another LTA4H inhibitor SC 57461A (CAS 423169-68-0), in comparison, inhibits both the LTA₄-to-LTB₄ conversion as well as the chemotactic tripeptide Pro-Gly-Pro degradation activity of LTA4H.

A cell-permeable benzylphenyl-thiazolamine compound that acts as a selective inhibitor against the epoxide hydrolase activity of leukotriene A4 hydrolase (LTA4H; K_i = 2.3 µM) and inhibits A23187- (Cat. Nos. 100105 & 100106) induced leukotriene B4 (LTB₄) synthesis in primary human polymorphonuclear neutrophil (PMN) cultures (IC₅₀ = 0.5 µM). Does not affect LTA4H aminopeptidase activity toward the cleavage of Pro-Gly-pro even at a high concentratin of 100 µM. Binds to the hydrophobic pocket that accommodates LTA₄ Ω-end, which is distant from the aminopeptidase active site.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Stsiapanava, A., et al. 2014. Proc. Natl. Acad. Sci. USA111, 4227.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Use only fresh DMSO for reconstitution.

Warning

Toxicity: Standard Handling (A)