iCRT14

iCRT14 is a potent inhibitor of beta-catenin-responsive transcription (CRT) that inhibits Wnt signaling in a reporter assay in vitro (IC50 = 40.3 nM). It inhibits the interaction between beta-catenin and T cell factor 4 (Tcf4) in quantitative reporter assays of beta-catenin/Tcf4 binding (Ki = 53.51 µM). It inhibits Notch, hedgehog (Hh), and JAK/STAT signaling in reporter assays with IC50 values of 69.2, 194, and 70 nM, respectively. iCRT14 (50 mg/kg, i.p.) reduces the number of proliferating cells and leads to a decrease of approximately 50% in the initial tumor growth rate in mouse xenograft models of colon carcinoma. iCRT14 also inhibits proliferation of leukemia cell lines and suppresses ATP-driven migration of the MCF-7 and MDA-MB-231 breast cancer cell lines.Formal Name: 5-[[2,5-dimethyl-1-(3-pyridinyl)-1H-pyrrol-3-yl]methylene]-3-phenyl-2,4-thiazolidinedione. CAS Number: 677331-12-3. Molecular Formula: C21H17N3O2S. Formula Weight: 375.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 2 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 371 nm. SMILES: O=C(S/C1=C\C2=C(C)N(C3=CN=CC=C3)C(C)=C2)N(C4=CC=CC=C4)C1=O. InChi Code: InChI=1S/C21H17N3O2S/c1-14-11-16(15(2)23(14)18-9-6-10-22-13-18)12-19-20(25)24(21(26)27-19)17-7-4-3-5-8-17/h3-13H,1-2H3/b19-12-. InChi Key: NCSHZXNGQYSKLR-UNOMPAQXSA-N.