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GW 843682X
- Soluble in DMSO
- MF: C22H18F3N3O4S
- MW: 477.46
Description
GW 843682X is a potent and selective polo-like kinase (PLK) inhibitor with reported IC50 values of 2 nM for PLK1 and 9 nM for PLK3 and >100-fold selectivity against roughly 30 other kinases (including cdk1 and cdk2). It is used to study mitotic kinase signaling and cell-cycle control.
PLK1 is a key regulator of mitotic entry, spindle formation, chromosome segregation and cytokinesis. GW 843682X is valuable for probing PLK-dependent cell-cycle progression and for profiling anti-proliferative kinase inhibitor effects.
Key Features
- Potent and selective PLK inhibitor
- IC50: 2 nM for PLK1 and 9 nM for PLK3
- Targets mitotic kinase signaling
- Useful for cell-cycle and anti-proliferative studies
Applications
- PLK1 and PLK3 inhibition assays
- Mitosis and cell-cycle research
- Cancer cell proliferation studies
- Kinase inhibitor profiling
More Information
| Parent CAS No. | 660868-91-7 |
|---|---|
| Chemical Name | 5-(5,6-Dimethoxy-benzoimidazol-1-yl-3-(2-trifluoromethyl-benzyloxy)-thiophene-2-carboxylic acid amide |
| SMILES | C1(OC)C=C2N=CN(C3SC(C(=O)N)=C(OCC4C=CC=CC=4C(F)(F)F)C=3)C2=CC=1OC |
| MFCD | MFCD09971143 |
| InChi | InChI=1S/C22H18F3N3O4S/c1-30-16-7-14-15(8-17(16)31-2)28(11-27-14)19-9-18(20(33-19)21(26)29)32-10-12-5-3-4-6-13(12)22(23,24)25/h3-9,11H,10H2,1-2H3,(H2,26,29) |
| InChiKey | JSKUWFIZUALZLX-UHFFFAOYSA-N |
| CID | 9826308 |
| Short Description | PLK1/3 inhibitor |
References
- EF Johnson et al. Pharmacological and Functional Comparison of the Polo-like Kinase Family: Insight into Inhibitor and Substrate Specificity. Biochemistry 2007, 46(33), 9558.
- T Lansing et al. In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1. Mol. Cancer Ther. 2007, 6, 450-459.
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