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NI-42

Chemical Structure : NI-42

CAS No.: 1884640-99-6

NI-42 (NI42;NI 42;BRPF1 inhibitor NI-42)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 353.396
Formula C18H15N3O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-Cyano-N-(1,3-dimethyl-2-oxo-1,2-dihydroquinolin-6-yl)-benzenesulfonamide

References

1. Igoe N, et al. J Med Chem. 2017 Jan 26;60(2):668-680.

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