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GSK 461364 analogue II
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C27H27F3N4O3S
- MW: 544.59
Description
GSK 461364 analogue II is a potent Polo-like kinase inhibitor with preferential activity at PLK1 and reported IC50 value of 2 nM for PLK1.
PLK1 is essential for mitotic progression and cytokinesis, making it a pharmacologically important target in proliferating tumor cells. GSK 461364 analogue II is useful for studying PLK1-driven cell-cycle control and mitotic arrest.
Key Features
- Potent PLK1-focused inhibitor
- Reported IC50: 2 nM for PLK1 and 270 nM for PLK3
- Blocks mitotic progression through Polo-like kinase inhibition
- Useful analog for PLK inhibitor mechanism studies
Applications
- Polo-like kinase assays
- Mitotic arrest and checkpoint research
- Cancer cell proliferation studies
- PLK1 inhibitor profiling
More Information
| Parent CAS No. | 929095-22-7 |
|---|---|
| Chemical Name | (R)-5-(6-(1-methylpiperidin-4-yloxy)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide |
| SMILES | [C@@H](OC1C=C(N2C3C=C(OC4CCC(N)CC4)C=CC=3N=C2)SC=1C(N)=O)(C)C1=C(C(F)(F)F)C=CC=C1 |&1:0,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C27H27F3N4O3S/c1-16(19-5-3-4-6-20(19)27(28,29)30)36-23-14-24(38-25(23)26(31)35)34-15-32-21-8-7-18(13-22(21)34)37-17-9-11-33(2)12-10-17/h3-8,13-17H,9-12H2,1-2H3,(H2,31,35)/t16-/m1/s1 |
| InChiKey | SWIVJTVGOIXUKC-MRXNPFEDSA-N |
| CID | 16050925 |
| 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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