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Submit ReviewGSK 6853
Description: Potent and selective BRPF1 inhibitor
Chemical Name: N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxybenzamide
Purity: ≥98% (HPLC)
Biological Activity for GSK 6853
GSK 6853 is a potent and selective BRPF1 inhibitor. Exhibits >1600-fold selectivity for BRPF1 over other bromodomains (pIC50 values by TR-FRET are 8.1, 5.1/4.8 and 4.7/<4.3 for BRPF1, BRPF2/3 and BRD4 BD1/2, respectively).
Negative Control also available.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the GSK 6853 probe summary on the SGC website.
Compound Libraries for GSK 6853
GSK 6853 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for GSK 6853
| M. Wt | 409.48 |
| Formula | C22H27N5O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1910124-24-1 |
| PubChem ID | 121232405 |
| InChI Key | FQWDVNSBYDXPIO-CQSZACIVSA-N |
| Smiles | COC1=C(C(NC2=C(N3CCNC[C@H]3C)C=C4N(C(N(C4=C2)C)=O)C)=O)C=CC=C1 |
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 6853
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.95 | 100 | |
| 1eq. HCl | 40.95 | 100 |
Preparing Stock Solutions for GSK 6853
The following data is based on the product molecular weight 409.48. 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 | 2.44 mL | 12.21 mL | 24.42 mL |
| 5 mM | 0.49 mL | 2.44 mL | 4.88 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.44 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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Product Datasheets for GSK 6853
References for GSK 6853
References are publications that support the biological activity of the product.
Bamborough et al (2016) GSK6853, a chemical probe for inhibition of the BRPF1 bromodomain. ACS Med.Chem.Lett. 7 552 PMID: 27326325
If you know of a relevant reference for GSK 6853, please let us know.
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Keywords: GSK 6853, GSK 6853 supplier, GSK6853, bromodomains, BRPF1, inhibitors, inhibits, potent, selective, Bromodomains, 6198, Tocris Bioscience
Citations for GSK 6853
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