KGP94 is a reversible, time-dependent and competitive inhibitor of human cathepsin L. ► KGP94 inhibits the activity of cathepsin L toward human type I collagen. ► KGP94 significantly impedes both migration and invasion of MDA-MB-231 human breast 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.
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