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NI-57

Catalog No. TQ0083 CAS 1883548-89-7

NI-57 is an inhibitor of proteins of bromodomain and plant homeodomain finger-containing (BRPF) family, with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively.

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NI-57, CAS 1883548-89-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
5 mg	In stock	$ 76.00
10 mg	In stock	$ 129.00
25 mg	In stock	$ 288.00
50 mg	In stock	$ 452.00
1 mL * 10 mM (in DMSO)	In stock	$ 89.00

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Purity: 100%

Biological Description

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Description	NI-57 is an inhibitor of proteins of bromodomain and plant homeodomain finger-containing (BRPF) family, with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively.
Targets&IC50	BRPF3:140 nM, BRPF1:3.1 nM, BRPF2 BRD1:46 nM
In vitro	NI-57 binds the BRD of BRPF1 with a Kd of 31 nM, BRD1 with a Kd of 110 nM, and BRPF3 with a Kd of 410 nM, whereas binding to BRD9 is weaker (Kd 1000 nM) measured by isothermal titration calorimetry. NI-57 shows less active effect on BRD9 (IC50, 520 nM) and BRD4 (BD1) (IC50, 3700 nM), TRIM24 (IC50, 1600 nM). NI-57 also inhibits BRPF BRDs in the nucleus but shows little effect on the proliferation of many cancer cell lines with GI50s of 10.4 μM (NCI-H1703 cells), 14.7 μM (DMS114), 15.6 μM (HRA-19), and 16.6 μM (RERF-LC-Sq1). Furthermore, Inhibition on BRPF1 of NI-57 (10 μM) reduces the gene expression of CCL-22 by 27.7%.
Kinase Assay	All reagents are diluted in the recommended buffer (50 mM HEPES, 100 mM NaCl, 0.1% BSA; pH = 7.4) supplemented with 0.05% CHAPS and allowed to equilibrate to room temperature prior to addition to plates. 4 mL of HIS-tagged protein is added to low-volume 384-well plates, followed by 4 mL of either buffer, non-biotinylated peptide, solvent or compounds (NI-57, etc.). Plates are sealed and incubated at room temperature for 30 minutes, before the addition of 4 mL biotinylated peptide, resealing and incubation for a further 30 minutes. 4 mL of streptavidin-coated donor beads (25 μg/mL) and 4 μL of nickel chelate acceptor beads (25 μg/mL) are then added under low light conditions. Plates are foil-sealed to protect from light, incubated at room temperature for 60 minutes and read on a PHERAstar FS plate reader using an AlphaScreenTM 680 excitation/570 emission filter set. IC50s are calculated in GraphPad Prism 5. Results for compounds (NI-57, etc.) dissolved in DMSO are normalized against corresponding DMSO controls prior to IC50 determination, which is given as the final concentration of the compound in the 20 μL reaction volume.

Molecular Weight	383.42
Formula	C19H17N3O4S
CAS No.	1883548-89-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (208.65 mM)

References and Literature

1. Igoe N, et al. Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins. J Med Chem. 2017 Aug 24;60(16):6998-7011.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library Bioactive Compound Library PPI Inhibitor Library Epigenetics Compound Library Reprogramming Compound Library Histone Modification Compound Library NO PAINS Compound Library

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Keywords

NI-57 1883548-89-7 Chromatin/Epigenetic Epigenetic Reader Domain Inhibitor NI57 inhibit NI 57 inhibitor

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