KLK14 Inhibitor

Kallikrein 5-IN-2 TFA is the TFA salt form of Kallikrein 5-IN-2 (HY-148949). Kallikrein 5-IN-2 TFA is a selective inhibitor for kallikrein 5 (KLK5) with pIC₅₀ of 7.1. Kallikrein 5-IN-2 TFA is non-phototoxic (100 μg/mL) and non-irritant. Kallikrein 5-IN-2 is stable at pH 4-pH 8 under non-oxidative condition. Kallikrein 5-IN-2 is potent in ameliorating the Netherton syndrome.

GSK951 is a highly potent, selective, and reversibly covalent KLK5 inhibitor, with an IC₅₀ of approximately 250 pM and a pIC₅₀ of 9.6 against hKLK5. It exhibits over 100-fold selectivity over KLK7, KLK14, matriptase, and elastase. GSK951 binds to the catalytic site of KLK5 via covalent interaction with the catalytic serine, with a slow dissociation rate. GSK951 improves skin barrier function, reduces transepidermal water loss, decreases the expression of proinflammatory cytokines, and inhibits the elevated KLK5 protease activity in the stratum corneum. GSK951 can be used in studies related to skin barrier dysfunction.

KLK5/14-IN-1 is a selective human skin kallikrein inhibitor with IC₅₀ values of 0.048 μM, 0.2 μM, and 0.1 μM for KLK7, KLK5, and KLK14, respectively. KLK5/14-IN-1 shows no or only low inhibitory activity against Cathepsin G, Chymotrypsin, Trypsin, and Thrombin. KLK5/14-IN-1 can be used in research related to Netherton syndrome.