NI-42

NI-42 is an inhibitor of the bromodomain and PHD finger-containing 1 (BRPF1) bromodomain (IC50 = 7.9 nM). It is selective for BRPF1 over BRPF2/BRD1, BRPF3, BRD9, and BRD4/BD1 (IC50s = 48, 260, 310, and 4,500 nM, respectively). NI-42 inhibits the growth of OCI-AML2, Nomo-1, THP-1, KG-1, and MV-4-11 acute myeloid leukemia (AML) cells (GI50s = 1.3, 4.6, 5.7, 7, and 9.9 µM, respectively) and a variety of non-AML cells (GI50s = 1-10 µM). It also inhibits the growth of DMS114 lung, HRA-19 colon, and RERF-LC-Sq1 lung cancer cells (GI50s = 16.6, 15.6, and 17.1 µM, respectively) but not NCI H1703 lung cancer cells (GI50 = >30 µM).Formal Name: 4-cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)-benzenesulfonamide. CAS Number: 1884640-99-6. Molecular Formula: C18H15N3O3S. Formula Weight: 353.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 239, 273, 335 nm. SMILES: O=S(C1=CC=C(C#N)C=C1)(NC2=CC(C=C(C)C(N3C)=O)=C3C=C2)=O. InChi Code: InChI=1S/C18H15N3O3S/c1-12-9-14-10-15(5-8-17(14)21(2)18(12)22)20-25(23,24)16-6-3-13(11-19)4-7-16/h3-10,20H,1-2H3. InChi Key: BMVCSXFOQPYKKC-UHFFFAOYSA-N.