iCRT3

iCRT3 is an inhibitor of beta-catenin-responsive transcription (CRT). It inhibits Wnt signaling in a reporter assay using HEK293 cells (IC50 = 8.2 nM). It is selective for inhibition of the protein-protein interaction between beta-catenin and T cell factor (Tcf) over the interaction between beta-catenin and epithelial cadherin (E-cadherin) or alpha-catenin. iCRT3 (50 µM) inhibits neurotensin- or Wnt3a-induced increases in the proliferation of A172 and U87 glioblastoma cells. It also reduces tumor growth in an A172 mouse xenograft model when administered at a dose of 5 mg/kg. iCRT3 (5 and 10 mg/kg) reduces plasma levels of IL-6, TNF-alpha, and IL-1beta, as well as the general organ damage marker aspartate aminotransferase (AST) and the liver damage marker alanine transaminase (ALT) in a mouse model of cecal ligation and puncture-induced sepsis. It also reduces lung cell apoptosis and the severity of sepsis-induced lung injury in the same model when administered at a dose of 10 mg/kg.Formal Name: 2-[[[2-(4-ethylphenyl)-5-methyl-4-oxazolyl]methyl]thio]-N-(2-phenylethyl)-acetamide. CAS Number: 901751-47-1. Molecular Formula: C23H26N2O2S. Formula Weight: 394.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Soluble: >10 mg/ml. SMILES: O=C(CSCC1=C(C)OC(C2=CC=C(CC)C=C2)=N1)NCCC3=CC=CC=C3. InChi Code: InChI=1S/C23H26N2O2S/c1-3-18-9-11-20(12-10-18)23-25-21(17(2)27-23)15-28-16-22(26)24-14-13-19-7-5-4-6-8-19/h4-12H,3,13-16H2,1-2H3,(H,24,26). InChi Key: QTDYVSIBWGVBKU-UHFFFAOYSA-N.