An inhibitor of the BRPF1 bromodomain (IC50 = 7.9 nM); selective for BRPF1 over BRPF2/BRD1

NI-42 – 10 mg

Brand:
Cayman
CAS:
1884640-99-6
Storage:
-20
UN-No:
Non-Hazardous - /

NI-42 is an inhibitor of the bromodomain and PHD finger-containing 1 (BRPF1) bromodomain (IC50 = 7.9 nM).{48550} It is selective for BRPF1 over BRPF2/BRD1, BRPF3, BRD9, and BRD4/BD1 (IC50s = 48, 260, 310, and 4,500 nM, respectively).{48551} 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).{48550} 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).{48551}  

 

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SKU: 28293 - 10 mg Category:

Description

An inhibitor of the BRPF1 bromodomain (IC50 = 7.9 nM); selective for BRPF1 over BRPF2/BRD1, BRPF3, BRD9, and BRD4/BD1 (IC50s = 48, 260, 310, and 4,500 nM, respectively); inhibits the growth of OCI-AML2, Nomo-1, THP-1, KG-1, and MV-4-11 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); 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)

Formal name: 4-cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)-benzenesulfonamide

Synonyms: 

Molecular weight: 353.4

CAS: 1884640-99-6

Purity: ≥98%

Formulation: A crystalline solid

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