OXF BD 02

OXF BD 02 is an inhibitor of bromodomain 1 (BD1) in bromodomain-containing protein 4 (BRD4, IC50 = 382 nM). It is selective for BRD4 BD1 over a panel of 60 bromodomain-containing proteins but does inhibit CREB-binding protein (CBP) at 25 µM. OXF BD 02 is cytotoxic to MV4-11 acute myeloid leukemia (AML) cells (IC50 = 0. nM) but not A549 or H1975 lung cancer cells (IC50s = >10 µM for both) or U2OS osteosarcoma or HeLa cervical cancer cells (IC50s = >100 µM for both). OXF BD 02 also binds to recombinant S. mansoni BRD3 (SmBRD3) that contains BD1 and BD2 (Kd = 683 nM) but not recombinant BD2 of SmBRD3. InChI: InChI=1S/C18H17NO3/c1-11-17(12(2)22-19-11)14-8-15(10-16(20)9-14)18(21)13-6-4-3-5-7-13/h3-10,18,20-21H,1-2H3 InChIKey: FEQUIPXIENTMJN-UHFFFAOYSA-N SMILES: OC(C1=CC(O)=CC(C2=C(C)ON=C2C)=C1)C3=CC=CC=C3