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1884640-99-6

1884640-99-6 Structure

1884640-99-6 Structure
IdentificationBack Directory
[Name]

4-Cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)benzenesulfonamide
[CAS]

1884640-99-6
[Synonyms]

NI-42 >=98% (HPLC)
BRPF1 inhibitor NI-42
NI-42,Inhibitor,inhibit,NI 42,Epigenetic Reader Domain,NI42
4-Cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)benzenesulfonamide
[Molecular Formula]

C18H15N3O3S
[MDL Number]

MFCD30290161
[MOL File]

1884640-99-6.mol
[Molecular Weight]

353.39
Chemical PropertiesBack Directory
[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
Hazard InformationBack Directory
[Description]

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).
[Uses]

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.
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