To enhance service speed and avoid tariff delays, we've opened a US warehouse. All US orders ship directly from our US facility.
| 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 |
|