Formulation: A solid
Formal Name: 3-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-1,4,6,7-tetrahydro-N-methyl-1-(tetrahydro-2H-pyran-4-yl)-5H-pyrazolo[4,3-c ]pyridine-5-carboxamide
Purity: ≥98%
Formula Markup: C27H33F2N7O2
CAS Number: 1936422-33-1
Notes: 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.
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