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Submit ReviewGSK 5959
Description: Potent and selective BRPF1 inhibitor
Chemical Name: N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-piperidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide
Purity: ≥99% (HPLC)
Biological Activity for GSK 5959
GSK 5959 is a potent and selective BRPF1 bromodomain inhibitor (IC50 = 80 nM). Exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. Inhibits BRPF1 interaction with histone H3.3. Cell permeable.
External Portal Information for GSK 5959
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GSK 5959 is reviewed on the chemical probes website.
Technical Data for GSK 5959
| M. Wt | 394.47 |
| Formula | C22H26N4O3 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 901245-65-6 |
| PubChem ID | 15990224 |
| InChI Key | LTUGYAOMCKNTGG-UHFFFAOYSA-N |
| Smiles | CN(C1=CC(NC(C4=C(OC)C=CC=C4)=O)=C(N3CCCCC3)C=C1N2C)C2=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 GSK 5959
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.94 | 10 with sonication |
Preparing Stock Solutions for GSK 5959
The following data is based on the product molecular weight 394.47. 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 |
|---|---|---|---|
| 0.1 mM | 25.35 mL | 126.75 mL | 253.5 mL |
| 0.5 mM | 5.07 mL | 25.35 mL | 50.7 mL |
| 1 mM | 2.54 mL | 12.68 mL | 25.35 mL |
| 5 mM | 0.51 mL | 2.54 mL | 5.07 mL |
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Product Datasheets for GSK 5959
References for GSK 5959
References are publications that support the biological activity of the product.
Demont et al (2014) 1,3-dimethyl benzimidazolones are potent, selective inhibitors of the BRPF1 bromodomain. ACS Med.Chem.Lett. 5 1190 PMID: 25408830
If you know of a relevant reference for GSK 5959, please let us know.
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Keywords: GSK 5959, GSK 5959 supplier, GSK5959, potent, selective, BRPF1, bromodomains, inhibitors, inhibits, cell, permeable, Bromodomains, 5385, Tocris Bioscience
Citations for GSK 5959
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