KLK5 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.

DKFZ-251 is a kininogenase-related peptidase KLK6 inhibitor (IC₅₀=0.47 μM), and also exhibits certain inhibitory activity against KLK5 and KLK7 (IC₅₀ values are 1.1 nM and 73 nM, respectively). DKFZ-251 transiently acylates the catalytic serine of KLK6 to form a long-lived acyl-enzyme complex that inhibits enzyme function. DKFZ-251 is a phenotypic modulator that alters cell proliferation capacity and regulates epithelial-mesenchymal transition (EMT). DKFZ-251 can be used in research related to head and neck cancer.

KLK5-IN-1 is a selective kallikrein 5 (KLK5) inhibitor with an IC₅₀ of 14 nM and a K_i of 11 nM. KLK5-IN-1 reduces KLK5-mediated PAR2-dependent calcium mobilization. KLK5-IN-1 improves epithelial barrier integrity. KLK5-IN-1 can be used in research related to atopic dermatitis and 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.