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NI-42

  Cat. No.:  DC23371   Featured
Chemical Structure
1884640-99-6
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More than 5000 active chemicals with high quality for research!
Field of application
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; 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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1884640-99-6
Chemical Name: 4-Cyano-N-(1,3-dimethyl-2-oxo-1,2-dihydroquinolin-6-yl)-benzenesulfonamide
Synonyms: NI42;NI 42;BRPF1 inhibitor NI-42
SMILES: C(C1C=CC(S(NC2C=C3C(=CC=2)N(C)C(=O)C(C)=C3)(=O)=O)=CC=1)#N
Formula: C18H15N3O3S
M.Wt: 353.396
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Igoe N, et al. Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies. J Med Chem. 2017 Jan 26;60(2):668-680.
Description: 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; 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.
Target: BRPF1:7.9 nM (IC50) BRPF2:48 nM (IC50) BRPF3:260 nM (IC50) BRPF1:40 nM (Kd) BRPF2:210 nM (Kd) BRPF3:940 nM (Kd) BRD4 (BD1):4500 nM (IC50) BRD7:82 nM (IC50) BRD9:310 nM (IC50) BRD9:1130 nM (Kd)
In Vitro: 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[1].
Animal Administration: [1]. Igoe N, et al. Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies. J Med Chem. 2017 Jan 26;60(2):668-680.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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