CPI-0610 is a potent, selective, and cell-active BET bromodomain inhibitor CPI-0610 inhibits BRD4-BD1 with IC50 of 39 nM in time-resolved fluorescence energy transfer (TR-FRET ) binding assay.

10074-A4 is a c-Myc binding compound that associates with c-Myc370–409 and behaves like a “ligand cloud” around a “protein cloud”, with distinct features from that of a non-binding ligand.

MYCi975 is an orally active inhibitor of MYC.MYCi975 inhibits P493-6, MV411,SK-N-B2 cells viability in an MYC-dependent manner(IC50s of 3.7, 3.9, 6.4 μM, respectively).The initial lead, MYC inhibitor 361 (MYCi361), suppressed in vivo tumor growth in mice, increased tumor immune cell infiltration, upregulated PD-L1 on tumors, and sensitized tumors to anti-PD1 immunotherapy. However, 361 demonstrated a narrow therapeutic index.