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GSK 461364
- GSK 461364A
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C27H28F3N5O2S
- MW: 543.6
Description
GSK 461364 is a potent and selective Polo-like kinase 1 (PLK1) inhibitor with a Ki value of 2.2 nM and selectivity over PLK2 and PLK3.
PLK1 controls mitotic entry, spindle formation and chromosome segregation. GSK 461364 is used to study mitotic kinase dependence, cell-cycle arrest and anticancer mechanisms involving PLK1 inhibition.
Key Features
- Potent PLK1 inhibitor
- Ki: 2.2 nM
- Selective over PLK2 and PLK3
- Induces mitotic pathway disruption in proliferating cells
Applications
- PLK1 kinase assay development
- Mitotic checkpoint and cell-cycle studies
- Cancer cell proliferation models
- Antimitotic drug mechanism research
More Information
| Parent CAS No. | 929095-18-1 |
|---|---|
| Chemical Name | (R)-5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide |
| SMILES | C1C(C(F)(F)F)=C([C@@H](C)OC2=C(C(=O)N)SC(N3C=NC4C=CC(CN5CCN(C)CC5)=CC3=4)=C2)C=CC=1 |&1:7,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C27H28F3N5O2S/c1-17(19-5-3-4-6-20(19)27(28,29)30)37-23-14-24(38-25(23)26(31)36)35-16-32-21-8-7-18(13-22(21)35)15-34-11-9-33(2)10-12-34/h3-8,13-14,16-17H,9-12,15H2,1-2H3,(H2,31,36)/t17-/m1/s1 |
| InChiKey | ZHJGWYRLJUCMRT-QGZVFWFLSA-N |
| CID | 15983966 |
| Short Description | PLK1 inhibitor |
References
- TR Rheault et al. Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophene carboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties. Bioorg. Med. Chem. Lett. 2010, 20(15), 4587-92.
- KA Emmitte et al. Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. Bioorg. Med. Chem. Lett. 2009, 19(6), 1694-7.
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