Mycro 3

Mycro 3 is an orally active, potent and selective inhibitor of Myc-associated factor X (MAX) dimerization. Mycro 3 also inhibit DNA binding of c-Myc^[1]. Mycro 3 could be used for the research of pancreatic cancer^[2]. IC50 & Target:Myc-MAX dimerization^[1] In Vitro:Mycro 3 is a potent and selective c-Myc inhibitor in whole cell assays, with weak inhibitory activity against Activator protein 1 (AP-1). Mycro 3 has a superior specificity profile to its predecessors. Mycro 3 inhibits the interaction between c-Myc and Max. Mycro 3 has high selectivity and inhibits c-Myc/Max dimerization and conjugation with DNA^[1]. Mycro 3 exhibits an excellent specificity with IC₅₀s of 0.25 and 9.0 µM for cells with intact Myc alleles and Myc-null cells, respectively^[2]. In Vivo:Mycro 3 (100 mg/kg; oral administration; daily for two months) induces marked shrinkage of pancreatic ductal adenocarcinoma (PDA), increases cancer cell apoptosis, and reduces cell proliferation. Tumor growth is also drastically attenuated in Mycro 3-treated NOD/SCID mice carrying orthotopic or heterotopic xenografts of human pancreatic cancer cells^[2].