CA-074

CA-074 is a selective epoxysuccinyl peptide inhibitor of the cysteine protease cathepsin B (Kis = 0.0087, 75, and 233 µM for rat cathepsin B, H, and L, respectively). It inhibits degradation of DQ-collagen IV and DQ-collagen I in 4T1.2 breast cancer cells in a concentration-dependent manner and reduces the number of lung and bone metastases in a 4T1.2 murine mammary cancer model, without affecting primary tumor growth, when administered at a dose of 50 mg/kg. CA-074 (0.1 and 0.2 mg/animal per day) reduces mercury-induced increases in expression of TNF-alpha, IL-1beta, and the inflammasome component NRLP3 and decreases the severity of mercury-induced skin induration in mice. CA-074 also reduces ischemia-induced hippocampal neuron cell death in monkeys.Formal Name: N-[[3S-[(propylamino)carbonyl]-2S-oxiranyl]carbonyl]-L-isoleucyl-L-proline. CAS Number: 134448-10-5. Molecular Formula: C18H29N3O6. Formula Weight: 383.4. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Methanol: 1 mg/ml. SMILES: OC([C@@H]1CCCN1C([C@@]([C@@H](C)CC)([H])NC([C@@H]2[C@@H](C(NCCC)=O)O2)=O)=O)=O. InChi Code: InChI=1S/C18H29N3O6/c1-4-8-19-15(22)13-14(27-13)16(23)20-12(10(3)5-2)17(24)21-9-6-7-11(21)18(25)26/h10-14H,4-9H2,1-3H3,(H,19,22)(H,20,23)(H,25,26)/t10-,11-,12-,13-,14-/m0/s1. InChi Key: ZEZGJKSEBRELAS-PEDHHIEDSA-N.