Description
InformationMYCi975 MYCi975 is an orally active inhibitor of MYC that disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 exhibits potent anti-tumor activities.TargetsMYCIn vitroMYCi975 localizes to the same region of the MYC protei. Treatment of cells with MYCi975 enhances MYC degradation and phosphorylation on T58. MYCi975 also directly increases GSK3b-mediated MYC pT58 in the in vitro kinase assay.In vivoMYCi975 suppresses in vivo tumor growth in mice, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy with good tolerability.Cell Research(from reference)Cell lines：MycCaP, PC3, LNCaP, PC12, MV411, SK-N-BE (2), 293T, P493-6 B cells, LLC1 cells, TGR-1, HO15.19 Rat-1 cells Concentrations：3-25 µM, 8 µM, 6 µM Incubation Time：24 h