For research use only. Not for therapeutic Use.
GSK6853（Cat No.:I002449）is a selective inhibitor of the protein kinase MPS1 (monopolar spindle 1), which is essential for proper mitotic progression and chromosome alignment during cell division. By targeting MPS1, GSK6853 disrupts the spindle assembly checkpoint, leading to mitotic defects and apoptosis in cancer cells. This compound has demonstrated significant anti-tumor activity in preclinical models, particularly in cancers with high proliferation rates. GSK6853’s ability to enhance the efficacy of conventional therapies positions it as a promising candidate for further investigation in the development of targeted cancer treatments that exploit mitotic vulnerabilities.
| Catalog Number | I002449 |
| CAS Number | 1910124-24-1 |
| Synonyms | N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxy-benzamide |
| Molecular Formula | C22H27N5O3 |
| Purity | ≥95% |
| Target | Epigenetic Reader Domain |
| Solubility | DMSO ≥ 31 mg/mL |
| Storage | Store at -20°C |
| IUPAC Name | N-[1,3-dimethyl-6-[(2R)-2-methylpiperazin-1-yl]-2-oxobenzimidazol-5-yl]-2-methoxybenzamide |
| InChI | InChI=1S/C22H27N5O3/c1-14-13-23-9-10-27(14)17-12-19-18(25(2)22(29)26(19)3)11-16(17)24-21(28)15-7-5-6-8-20(15)30-4/h5-8,11-12,14,23H,9-10,13H2,1-4H3,(H,24,28)/t14-/m1/s1 |
| InChIKey | FQWDVNSBYDXPIO-CQSZACIVSA-N |
| SMILES | C[C@@H]1CNCCN1C2=CC3=C(C=C2NC(=O)C4=CC=CC=C4OC)N(C(=O)N3C)C |
| Reference | 1:ACS Med Chem Lett. 2016 May 9;7(6):552-7. doi: 10.1021/acsmedchemlett.6b00092. eCollection 2016 Jun 9. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.Bamborough P,Barnett HA,Becher I,Bird MJ,Chung CW,Craggs PD,Demont EH,Diallo H,Fallon DJ,Gordon LJ,Grandi P,Hobbs CI,Hooper-Greenhill E,Jones EJ,Law RP,Le Gall A,Lugo D,Michon AM,Mitchell DJ,Prinjha RK,Sheppard RJ,Watson AJ,Watson RJ, PMID: 27326325 PMCID: PMC4904261 [Available on 2017-06-09] DOI: 10.1021/acsmedchemlett.6b00092 </br><span>Abstract:</span> The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engagement assay was recently described. Herein, we report the optimization of this series leading to the identification of a superior BRPF1 inhibitor suitable for in vivo studies. |
