kgp94

Description: KGP94 is a novel, potent, reversible, time-dependent and competitive inhibitor of human cysteine protease Cathepsin L inhibitor(CTSL). It inhibits the activity of cathepsin L toward human type I collagen. KGP94significantly impedes both migration and invasion of MDA-MB-231 humanbreast cancer cells. Molecular modeling places the thiocarbonyl of KGP94 in proximity to the active site Cys25. Significant growth retardation of C3H mouse mammary carcinomas is achieved with KGP94 treatment 1, 2. KGP94 treatment led to marked attenuation of tumor cell invasion andmigration under both normal and aberrant microenvironmental conditionssuggesting that it may have significant utility as an anti-metastaticagent. 3

References:

1. European Journal of Medicinal Chemistry Volume 58, December 2012, Pages 568-572

2. Synthesis and biological evaluation of a water-soluble phosphate prodrug salt and structural analogues of KGP94, a lead inhibitor of cathepsin L. Bioorg Med Chem Lett. 2017 Mar 1; 27(5):1304-1310. doi: 10.1016/j.bmcl.2016.12.039. PubMed PMID: 28117205.

3. Clin Exp Metastasis . 2013 Oct; 30(7):891-902. doi: 10.1007/s10585-013-9590-9