E-7386 is a first-in-class orally active specific inhibitor of CBP/β-catenin complex, and a modulator of Wnt signaling pathway. It disrupts the interaction and inhibits canonical Wnt signaling pathway /TCF reporter gene activity in LiCl-stimulated HEK-293 and MDA-MB-231 in a dose-dependent manner, with IC50 of 55 and 73 nM, respectively; exhibits anti-tumor activity in vitro tumor proliferation panel against 28 human tumor cell lines; modulates the expression of Wnt signaling pathway related genes including AXIN2 and other genes. Oral administration of E7386 significantly suppressed the number of polyposis in a dose dependent manner at the dose range from 8.5 to 50 mg/kg. It also significantly changed the expressions of Wnt related genes in whisker follicle of ApcMin/+mice model.

KEYWORDS: E-7386 | Supplier | CBP/beta-catenin modulator | E7386 | E 7386 | CT-E7386 | CAS [1799824-08-0] | ECM-adhesion | β-Catenin | Wnt | Modulator | Proteins