HP537

HP537 is a potent and selective small-molecule inhibitor of the p300/CBP bromodomain (BRD), developed by Hinova Pharma for the treatment of hematologic malignancies. It functions by competitively inhibiting the binding of acetylated peptide substrates to the bromodomains of p300 and CREB-binding protein (CBP), which are key epigenetic co-activators. This inhibition leads to a significant reduction in the expression of oncogenic drivers, including c-Myc and IRF4, and decreases the levels of acetylated histone H3 lysine 27 (H3K27ac). HP537 has demonstrated broad anti-proliferative activity in cell lines derived from multiple myeloma, leukemia, and lymphoma. It is currently undergoing Phase 1/2 clinical evaluation in both China and the United States for indications such as Acute Myeloid Leukemia (AML), Multiple Myeloma (MM), and Myelodysplastic Syndromes (MDS).