NI-42

Research use only, not for human use.

A potent, selective and orally active BRPF1 bromodomain inhibitor with IC50 of 7.9 nM.

A potent, selective and orally active BRPF1 bromodomain inhibitor with IC50 of 7.9 nM, with excellent selectivity over nonclass IV BRDs; 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); shows a modest (GI50=1-10 uM) and selective inhibition of proliferation of certain cancer lines, particularly those lines exhibiting monocytic lineage differentiation; a novel, structurally orthogonal chemical probe for the BRPFs suitable for cellular and in vivo studies.

NI-42 shows IC50s of 82, 310, and 4500 nM for BRD7, BRD9, and BRD4 (BD1), respectively, and has a Kd of 1130 nM for BRD9.

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NI42 | NI 42 | BRPF1 inhibitor NI-42

Chromatin/Epigenetic

Bromodomain

Bromodomain

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1884640-99-6

353.396

C18H15N3O3S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (282.97 mM)

O=S(C1=CC=C(C#N)C=C1)(NC2=CC(C=C(C)C(N3C)=O)=C3C=C2)=O

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

(-20℃)

With Ice Pack

≥ 2 years