产品描述:
GNE-781 is an inhibitor of CREB-binding protein (CBP) and histone acetyltransferase p300 (IC50s = 0.94 and 1.2 nM, respectively).{40313} It is selective for CBP and p300 over bromodomain-containing protein 4 (BRD4) bromodomain 1, BRD4 bromodomain 2, and bromodomain and PHD finger-containing 1 (BRPF1; IC50s = 5.1, 12, and 4.6 µM, respectively), as well as nine other bromodomain-containing proteins (IC50s = >18 µM for all). GNE-781 inhibits the expression of Myc in MV4-11 leukemia cells (EC50 = 6.6 nM). It reduces the differentiation of isolated human naïve CD4+ T cells into FOXP3+ inducible regulatory T cells (Tregs) in a concentration-dependent manner without affecting cell viability. Oral administration of GNE-781 (3-30 mg/kg) decreases tumor volume in a MOLM-16 acute myeloid leukemia (AML) mouse xenograft model.