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Description: Potent and selective BRPF bromodomain inhibitor
Chemical Name: 4-Cyano-N-(1,3-dimethyl-2-oxo-1,2-dihydroquinolin-6-yl)-2-methoxybenzene-1-sulfonamide
Purity: ≥98% (HPLC)
Biological Activity for NI 57
NI 57 is a potent and selective BRPF bromodomain inhibitor (Kd values are 31, 108 and 408 nM, for BRPF1B, 2 and 3, respectively, which exhibits >32-fold selectivity for BRPFs over BRD9 and other non-Class IV bromodomains. NI 57 inhibits RANKL-induced differentiation of primary murine bone marrow cells and human primary monocytes into osteoclasts.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the NI 57 probe summary on the SGC website.
External Portal Information for NI 57
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of NI 57 is reviewed on the chemical probes website.
Compound Libraries for NI 57
NI 57 is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for NI 57
| M. Wt | 383.42 |
| Formula | C19H17N3O4S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1883548-89-7 |
| PubChem ID | 91827373 |
| InChI Key | UEMQPCYDWCSVCU-UHFFFAOYSA-N |
| Smiles | O=S(NC1=CC=C(N(C)C(C(C)=C2)=O)C2=C1)(C3=C(OC)C=C(C#N)C=C3)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for NI 57
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.34 | 100 |
Preparing Stock Solutions for NI 57
The following data is based on the product molecular weight 383.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.61 mL | 13.04 mL | 26.08 mL |
| 5 mM | 0.52 mL | 2.61 mL | 5.22 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.61 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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Product Datasheets for NI 57
References for NI 57
References are publications that support the biological activity of the product.
Igoe et al (2017) Design of a chemical probe for the bromodomain and plant homeodomain finger-containing (BRPF) family of proteins. J.Med.Chem. 60 6998 PMID: 28714688
Meier et al (2017) Selective targeting of bromodomains of the bromodomain-PHD fingers family impairs osteoclast differentiation. ACS Chem.Biol. 12 2619 PMID: 28849908
If you know of a relevant reference for NI 57, please let us know.
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Keywords: NI 57, NI 57 supplier, NI57, potent, and, selective, bromodomain, inhibitors, inhibits, BRPF, sgc, structural, genomics, consortium, Bromodomains, 5546, Tocris Bioscience
Citations for NI 57
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