Cathepsins (the term standing for “lysosomal proteolytic enzyme”) are a class of globular proteases that catalyze the hydrolysis of intracellular peptides and also exhibit extracellular functions. So far, a total of sixteen members of human cathepsin family have been identified, which are divided into three subfamilies, including cysteine protease family (cathepsin B, C, F, H, L, K, O, S, V, W, X and Z), serine carboxypeptidase family (cathepsin A and G) and aspartic protease family (cathepsin D and E). Cathepsins are highly expressed in various human cancers with each member playing different roles in distinct tumorigenic processes, including proliferation, angiogenesis, metastasis and invasion.
- 2-cyano-PyrimidineCatalog No. :C5038cathepsin K inhibitor
- Cathepsin Inhibitor 1Catalog No. :B2084Cathepsin inhibitorCathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.
- Odanacatib (MK-0822)Catalog No. :A2487Cathepsin K,potent and selectiveOdanacatib (MK-0822) is a potent, orally active and selective inhibitor of Cathepsin K with IC50 value of 0.20 nM ,
- CA-074 MeCatalog No. :A8239Cathepsin B inhibitor
CA-074 Me is a membrane-permeable and selective inhibitor of cathepsin B with IC50 value of 36.3 nM [1, 2].
- SID 26681509Catalog No. :A4424Human cathepsin L inhibitor,potent and reversiblePotent and reversible human cathepsin L inhibitor (IC50 = 56 nM). Displays no inhibitory activity at cathepsin G. Antimalarial; inhibits leishmaniasis.
- MDL 28170Catalog No. :A4412Calpain and cathepsin B inhibitor, selective
MDL 28170 is a selective inhibitor, which inhibites calpain with Ki values of 10nM and cathepsin B with Ki values of 25 nM while does not inhibit trypsin-like serine proteases.
- L 006235Catalog No. :A4422Cathepsin K inhibitorPotent, reversible cathepsin K inhibitor (IC50 = 0.25 nM) that displays > 4000-fold selectivity over cathepsins B, L and S. Displays reduced selectivity in cell-based assays possibly due to lysosomal accumulation. Reduces collagen breakdown and promotes bone deposition in vivo. Orally active and has intrinsic fluorescence.
- Cathepsin S inhibitorCatalog No. :A3284Blocks MHCII antigen presentationA slow, tight-binding reversible inhibitor of recombinant cathepsin S (Ki = 185 pM). Exhibits about 410-fold greater selectivity for cathepsin S compared to cathepsin B (Ki = 76 nM).
- E-64-cCatalog No. :A8162Inhibitor of cysteine proteinases
E-64-c, which is also known as Ep-475, is an analog of E-64 and inhibitor of cysteine proteinases.
- CA 074Catalog No. :A1926Cathepsin B inhibitorInhibitor of cathepsin B (Ki = 2-5 nM). Displays selectivity over cathepsins H and L (Ki = 40-200 μM). Shown to reduce bone metastasis in a 4T1.2 breast cancer model.