NI-57 NEW
| Price | $46 | $77 | $173 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: NI-57 | CAS No.: 1883548-89-7 |
| Purity: 98% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | NI-57 |
| Description | NI-57 is an inhibitor of the bromodomain and plant homeodomain finger-containing (BRPF) family proteins, with IC50 values of 3.1 nM for BRPF1, 46 nM for BRPF2 (BRD1), and 140 nM for BRPF3. |
| 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. |
| 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%. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 80 mg/mL (208.65 mM) |
| Keywords | Inhibitor | NI57 | inhibit | NI-57 | NI 57 | Epigenetic Reader Domain |
| Inhibitors Related | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Anacardic Acid | Curcumin | dBET6 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin | GSK1379725A |
| Related Compound Libraries | Histone Modification Compound Library | Reprogramming Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Inhibitor Library | NO PAINS Compound Library | PPI Inhibitor Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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