Molecular structure of Polo-like Kinase Inhibitor III, CAS Number: 660868-91-7
Polo-like Kinase Inhibitor III (CAS 660868-91-7)
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Alternate Names:
5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-((2-(trifluoromethyl)-benzyl)oxy)thiophene-2-carboxamide; Plk Inhibitor III
Application:
Polo-like Kinase Inhibitor III is a cell-permeable thiophene-benzimidazole compound and reversible PLK inhibitor
CAS Number:
660868-91-7
Purity:
>97%
Molecular Weight:
477.46
Molecular Formula:
C22H18F3N3O4S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Polo-like Kinase Inhibitor III is a cell-permeable thiophene-benzimidazole compound that acts as a potent and reversible inhibitor against polo-like kinases (Ki against Plk1/2/3/4 = 4.8, 3.8, 8.0, and 163 nM , respectively), while exhibiting little or much reduced activity against 39 other commonly studied kinases. Polo-like Kinase Inhibitor III preferentially inhibits the proliferation of a panel of 11 tumor cell lines (IC50 ≤0.7 µM) over normal human diploid fibroblasts (IC50 = 6.14 µM) in culture and is equally potent against the mdr-1-expressing MES-SA/DX5 and its parent non-drug resistant MES-SA uterine sarcoma cell line.
Polo-like Kinase Inhibitor III (CAS 660868-91-7) References
- In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1. | Lansing, TJ., et al. 2007. Mol Cancer Ther. 6: 450-9. PMID: 17267659
- A novel treatment strategy targeting polo-like kinase 1 in hematological malignancies. | Ikezoe, T., et al. 2009. Leukemia. 23: 1564-76. PMID: 19421227
- Polo-like kinase 1 (Plk1) is expressed by cutaneous T-cell lymphomas (CTCLs), and its downregulation promotes cell cycle arrest and apoptosis. | Nihal, M., et al. 2011. Cell Cycle. 10: 1303-11. PMID: 21436619
- Polo-like kinase 1 regulates activation of AMP-activated protein kinase (AMPK) at the mitotic apparatus. | Vazquez-Martin, A., et al. 2011. Cell Cycle. 10: 1295-302. PMID: 21474997
- Targeting Plk1 in cutaneous T-cell lymphomas (CTCLs). | Liu, XS. and Liu, X. 2011. Cell Cycle. 10: 1523. PMID: 21478668
- Polo-like kinase 1 inhibition causes decreased proliferation by cell cycle arrest, leading to cell death in glioblastoma. | Pezuk, JA., et al. 2013. Cancer Gene Ther. 20: 499-506. PMID: 23887645
- Polo-like kinase 1 (PLK1) is involved in toll-like receptor (TLR)-mediated TNF-α production in monocytic THP-1 cells. | Hu, J., et al. 2013. PLoS One. 8: e78832. PMID: 24205328
- The cytotoxic effect of GW843682X on nasopharyngeal carcinoma. | Hu, Q., et al. 2016. Anticancer Agents Med Chem. 16: 1640-1645. PMID: 27198987
- Construction of m6A-Related lncRNA Prognostic Signature Model and Immunomodulatory Effect in Glioblastoma Multiforme. | Xie, P., et al. 2022. Front Oncol. 12: 920926. PMID: 35719945
- Proteasome activation is critical for cell death induced by inhibitors of polo-like kinase 1 (PLK1) in multiple cancers. | Wang, Y., et al. 2024. Eur J Pharmacol. 972: 176558. PMID: 38614382
Inhibitor of:
BMP-4, Cdc5, Cdt1, cyclin B1, EG244495, EG624855, EG633057, fzr, Hemoglobin δ, Myt 1, OIP5, Olfr551, ORMDL3, PCTAIRE-3, Plk, and ZMAT4.Activator of:
ASPM, E2F-3, FGF-19, IL-15, and RANKL.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Polo-like Kinase Inhibitor III, 500 µg | sc-203202 | 500 µg | $107.00 |