Chemical Structure : NI-42
CAS No.: 1884640-99-6
货号: PC-61007Not For Human Use, Lab Use Only.
BRPF1 inhibitor NI-42 (NI-42) is a potent, selective and orally active BRPF1 bromodomain inhibitor with IC50 of 7.9 nM, with excellent selectivity over nonclass IV BRDs.
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BRPF1 inhibitor NI-42 (NI-42) is a potent, selective and orally active BRPF1 bromodomain inhibitor with IC50 of 7.9 nM, with excellent selectivity over nonclass IV BRDs.
NI-42 weakly inhibits BRPF2 (BRD1), BRPF3, BRD9 and BRD4 (BD1) with IC50 of 48, 260, 310 and 4500 nM respectively, and no activity for ATAD2A/2B (IC50>100 uM).
NI-42 shows a modest (GI50=1-10 uM) and selective inhibition of proliferation of certain cancer lines, particularly those lines exhibiting monocytic lineage differentiation.
NI-42 is a novel, structurally orthogonal chemical probe for the BRPFs suitable for cellular and in vivo studies.
分子量 | 353.396 | |
分子式 | C18H15N3O3S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
4-Cyano-N-(1,3-dimethyl-2-oxo-1,2-dihydroquinolin-6-yl)-benzenesulfonamide |
1. Igoe N, et al. J Med Chem. 2017 Jan 26;60(2):668-680.
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