cathepsin k (human)

Odanacatib is an inhibitor of cathepsin K with potential anti-osteoporotic activity.

ONO-5334 is a selective, orally active and potent histone K inhibitor with anti-SAR-COV-2 and anti-bone resorption activity for the study of osteoporosis.

Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V, exhibiting high affinity with Ki values of 41 pM, 68 pM, and 53 pM, respectively. It effectively inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. In vitro studies confirm its inhibitory effect on bone resorption in human tissue, and in vivo studies on cynomolgus monkeys validate its efficacy in reducing bone resorption.

Cathepsin K inhibitor4 is a potent carboxyhydrazide inhibitor of cathepsin K, exhibiting IC50 values of 13 nM for human, 269 nM for rat, and 296 nM for mouse cathepsin K.