NI-57 |
| Catalog No.GC16763 |
bromodomains of BRPF proteins inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1883548-89-7
Sample solution is provided at 25 µL, 10mM.
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NI-57 is a potent inhibitor of the bromodomain of the BRPFs that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively [1].
The bromodomain and PHD finger-containing protein 1, 2, 3 (BRPF1/2/3) are scaffolding subunit of the MOZ/MORF histone acetyltransferase complexes that links together KAT6A/B, ING5 and hEAF6 in the tetrameric assembly. BRPF1 (BR140 or Peregrin) is important in the maintenance of expression levels of Hox genes and the development of axial skeleton, multiple tissues and the hematopoietic system [2][3].
NI-57 is a potent inhibitor of the bromodomain of the BRPFs and acts as a chemical probe for the bromodomains of the BRPF family of proteins (BRPF1/2/3). As determined by isothermal titration calorimetry, NI-57 binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively. As measured by both biophysical and biochemical methods, NI-57 exhibited selective against other non-Class IV bromodomains, including the BETs. In the BRPF2 FRAP assay, NI-57 at 1 μM prevented binding of full-length BRPF2 to chromatin [1].
References:
[1]. http://www.thesgc.org/chemical-probes/NI-57
[2]. Klein BJ, Lalonde ME, Cté J, et al. Crosstalk between epigenetic readers regulates the MOZ/MORF HAT complexes. Epigenetics. 2014 Feb;9(2):186-93.
[3]. Ullah M, Pelletier N, Xiao L, et al. Molecular architecture of quartet MOZ/MORF histone acetyltransferase complexes. Mol Cell Biol. 2008 Nov;28(22):6828-43.
Kinase experiment: | All reagents are diluted in the recommended buffer (50 mMHEPES, 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 normalised against corresponding DMSO controls prior to IC50 determination, which are given as the final concentration of compound in the 20 µL reaction volume[1]. |
References: [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. | |
| Cas No. | 1883548-89-7 | SDF | |
| Chemical Name | 4-cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)-2-methoxy-benzenesulfonamide | ||
| Canonical SMILES | COC1=CC(C#N)=CC=C1S(NC2=CC=C(N(C)C(C(C)=C3)=O)C3=C2)(=O)=O | ||
| Formula | C19H17N3O4S | M.Wt | 383.4 |
| Solubility | ≤25mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6082 mL | 13.0412 mL | 26.0824 mL |
| 5 mM | 0.5216 mL | 2.6082 mL | 5.2165 mL |
| 10 mM | 0.2608 mL | 1.3041 mL | 2.6082 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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