PTX80

PTX80 is an antagonist of p62 (IC50 = 31.18 nM for the human receptor). It decreases the soluble fraction of p62 in MM.1S multiple myeloma cells when used at a concentration of 1.5 µM. PTX80 (200 nM) increases the levels of polyubiquitinated proteins in MM.1S cells. It induces apoptosis in MM.1S cells when used at a concentration of 100 nM. PTX80 (50-400 nM) decreases the survival of CD138+ cells, but not CD138- cells, in primary plasma cells derived from patients with multiple myeloma. It reduces the viability of tumor tissue samples isolated from ten patient-derived xenograft (PDX) mouse models of colorectal cancer (IC50s = 113-1,220 nM). In vivo, PTX80 (8 or 12 mg/kg twice per week) reduces tumor volume in an HCT116 colorectal cancer mouse xenograft model.Formal Name: 4,4'-((1E,1'E)-(1-((3-(dimethylamino)propyl)sulfonyl)-4-oxopiperidine-3,5-diylidene)bis(methaneylylidene))dibenzonitrile. CAS Number: 2376297-69-5. Molecular Formula: C26H26N4O3S. Formula Weight: 474.6. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly soluble: 0.1-1 mg/ml, DMSO: Sparingly soluble: 1-10 mg/ml. SMILES: O=C(/C(CN(C/1)S(CCCN(C)C)(=O)=O)=C/C2=CC=C(C=C2)C#N)C1=C\C3=CC=C(C=C3)C#N. InChi Code: InChI=1S/C26H26N4O3S/c1-29(2)12-3-13-34(32,33)30-18-24(14-20-4-8-22(16-27)9-5-20)26(31)25(19-30)15-21-6-10-23(17-28)11-7-21/h4-11,14-15H,3,12-13,18-19H2,1-2H3/b24-14+,25-15+. InChi Key: ACOAFAKBTXAOQG-KOJZRSEWSA-N.