ML-264

ML-264 is a selective inhibitor of Krüppel-like factor 5 (KLF5), a zinc finger-containing transcription factor that is highly expressed in rapidly dividing intestinal epithelial cells. It displays an IC50 value of 29 nM in a cell-based assay for proliferation of KLF5-expressing DLD-1 cells and an IC50 value of 81 nM in a cell-based luciferase assay but does not inhibit kinases associated with the KLF5 pathway, as determined using a panel of 47 selected kinases. ML-264 induces death in most colon cancer cell lines (HCT116, IC50 = 560 nM, HT-29, IC50 = 130 nM, SW620, IC50 = 430 nM), with cytotoxicity toward an established xenograft mouse model of colon cancer as well.Formal Name: (2E)-3-(3-chlorophenyl)-N-[2-[methyl(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)amino]-2-oxoethyl]-2-propenamide. CAS Number: 1550008-55-3. Molecular Formula: C17H21ClN2O4S. Formula Weight: 384.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 10 mg/ml. lambdamax: 219, 268 nm. SMILES: ClC1=CC=CC(/C=C/C(NCC(N(C)C2CCS(CC2)(=O)=O)=O)=O)=C1. InChi Code: InChI=1S/C17H21ClN2O4S/c1-20(15-7-9-25(23,24)10-8-15)17(22)12-19-16(21)6-5-13-3-2-4-14(18)11-13/h2-6,11,15H,7-10,12H2,1H3,(H,19,21)/b6-5+. InChi Key: AJCDZIDKYKCOMZ-AATRIKPKSA-N.