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GSK579289A
- GSK461364 analogue I
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C26H27ClN4O3S
- MW: 511.04
Description
GSK579289A is a potent and selective Polo-like kinase 1 (PLK1) inhibitor with reported IC50 value of 2 nM for PLK1 and 630 nM for PLK3.
PLK1 regulates mitotic entry, spindle assembly, chromosome segregation and cytokinesis. GSK579289A is useful for studying PLK1-dependent mitotic failure and the role of Polo-like kinase signaling in proliferating cancer cells.
Key Features
- Potent inhibitor of PLK1
- Reported IC50: 2 nM for PLK1 versus 630 nM for PLK3
- Selectivity over PLK3 supports PLK1-focused studies
- Disrupts mitotic progression and cytokinesis pathways
Applications
- PLK1 kinase assays
- Mitosis and cell-cycle research
- Cancer cell proliferation models
- Polo-like kinase selectivity profiling
More Information
| Parent CAS No. | 929095-23-8 |
|---|---|
| Chemical Name | (R)-3-(1-(2-chlorophenyl)ethoxy)-5-(6-(1-methylpiperidin-4-yloxy)-1H-benzo[d]imidazol-1-yl)thiophene-2-carboxamide |
| SMILES | C1(=CC(=C(C(N)=O)S1)O[C@H](C)C1C=CC=CC=1Cl)N1C2C=C(C=CC=2N=C1)OC1CCN(CC1)C |&1:9,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C26H27ClN4O3S/c1-16(19-5-3-4-6-20(19)27)33-23-14-24(35-25(23)26(28)32)31-15-29-21-8-7-18(13-22(21)31)34-17-9-11-30(2)12-10-17/h3-8,13-17H,9-12H2,1-2H3,(H2,28,32)/t16-/m1/s1 |
| InChiKey | GILNGUYOGYOZMP-MRXNPFEDSA-N |
| CID | 16051023 |
| 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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