Molibresib besylate is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4, and BRDT. It competitively occupies acetylated lysine binding sites, disrupting the interaction between BET proteins and chromatin. This action inhibits MYC expression and target gene transcription, demonstrating broad antiproliferative activity by inhibiting cancer cell growth and inducing growth arrest.
- Inhibits cancer cell proliferation and induces cell cycle arrest.
- Downregulates mitosis-related genes and upregulates p-ERK1/2.
- Shows synergistic anti-proliferative effects with MEK inhibitors.
- Reduces tumor burden and prolongs survival in mouse models of leukemia.
- Applicable to research in acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, and other advanced solid tumors.