PI-1840

PI-1840 is an inhibitor of chymotrypsin-like (CTL) proteasome activity (IC50 = 27 nM). It is selective for the CTL activity over the trypsin-like (TL) and peptidylglutamyl peptide hydrolyzing (PGPH) activities (IC50s = >100 µM for both), as well as for the 20S constitutive proteasome over the immunoproteasome (IC50s = 18 and 2,170 nM, respectively). PI-1840 decreases the viability of a panel of cancer cell lines (IC50s = 2.2-45.2 µM). It induces cell cycle arrest at the G2/M phase, apoptosis, and autophagy, as well as inhibits migration and invasion, in U2OS and MG-63 osteosarcoma cells when used at concentrations of 40 and 60 µM, respectively. PI-1840 (150 mg/kg) decreases tumor volume in an MDA-MB-231 breast cancer mouse xenograft model.Formal Name: N-(1-methylethyl)-2-(4-propylphenoxy)-N-[[3-(3-pyridinyl)-1,2,4-oxadiazol-5-yl]methyl]-acetamide. CAS Number: 1401223-22-0. Molecular Formula: C22H26N4O3. Formula Weight: 394.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 5 mg/ml, DMSO: 5 mg/ml, Ethanol: 5 mg/ml. lambdamax: 224 nm. SMILES: O=C(COC1=CC=C(CCC)C=C1)N(C(C)C)CC2=NC(C3=CN=CC=C3)=NO2. InChi Code: InChI=1S/C22H26N4O3/c1-4-6-17-8-10-19(11-9-17)28-15-21(27)26(16(2)3)14-20-24-22(25-29-20)18-7-5-12-23-13-18/h5,7-13,16H,4,6,14-15H2,1-3H3. InChi Key: ZVVXAODXPVWGMF-UHFFFAOYSA-N.