CAY10698

Platelet-type 12-lipoxygenase (12-LO; Item No. 10341) catalyzes the formation of 12-HpETE (Item No. 44570) from arachidonic acid (Item No. 90010).¹ It has been found to be expressed in various tumor cells as well as pancreatic islets and can be activated by inflammatory cytokines.² It has also been implicated in the modulation of hemostasis and thrombosis through its role in regulating platelet function.² CAY10698 is an inhibitor of 12-LO with an IC₅₀ value of 5.1 µM. It demonstrates greatly reduced potency for 15-LO-1, 15-LO-2, and 5-LO (IC₅₀s = >50, >40, and >200 µM.² The scaffold of this compound has been subjected to medicinal chemistry optimization and biological characterization for development of potential 12-LO inhibitors.²

WARNING This product is not for human or veterinary use.

1. Chen, X.-S., Kurre, U., Jenkins, N.A., et al. cDNA cloning, expression, mutagenesis of C-terminal isoleucine, genomic structure, and chromosomal localizations of murine 12-lipoxygenases. The Journal of Biological Chemisty 269(19), 13979-13987 (1994).

2. Luci, D.K., Jameson, J.B., II, Yasgar, A., et al. Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase. J. Med. Chem. 57(2), 495-506 (2014).