4-Cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)benzenesulfonamide , 99% HPLC , 1884640-99-6
CAS NO.：1884640-99-6
Empirical Formula: C18H15N3O3S
Molecular Weight: 353.39
MDL number: MFCD30290161
PRODUCT Properties
| Boiling point: | 554.6±60.0 °C(Predicted) |
| Density | 1.43±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml |
| form | A crystalline solid |
| pka | 8.05±0.20(Predicted) |
Description and Uses
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).
NI-42 is a new chemical probe for the BRPFs (bromodomain and PHD finger-containing) suitable for cellular and invivo studies to explore the fundamental biology of these proteins.