| Identification | Back Directory | [Name]
(5Z)-2-hydroxy-4-methyl-6-oxo-5-[(5-phenylfuran-2-yl)methylidene]-5,6-dihydropyridine-3-carbonitrile | [CAS]
591239-68-8 | [Synonyms]
ZINC05007751
NEK6 inibitor 8
NEK6 inhibitor 8
3-Pyridinecarbonitrile, 1,2,5,6-tetrahydro-4-methyl-2,6-dioxo-5-[(5-phenyl-2-furanyl)methylene]-
(5Z)-2-hydroxy-4-methyl-6-oxo-5-[(5-phenylfuran-2-yl)methylidene]-5,6-dihydropyridine-3-carbonitrile | [Molecular Formula]
C18H12N2O3 | [MOL File]
591239-68-8.mol | [Molecular Weight]
304.3 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 8.33 mg/mL (27.37 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [color ]
Brown to black |
| Hazard Information | Back Directory | [Uses]
ZINC05007751 is a potent NIMA-related kinase NEK6 inhibitor with an IC50 of 3.4 μM. ZINC05007751 shows antiproliferative activity against a panel of human cancer cell lines, and displays a synergistic effect with Cisplatin and Paclitaxel in a BRCA2 mutated ovarian cancer cell line. ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity was observed against NEK2, NEK7, and NEK9[1]. | [Biological Activity]
ZINC05007751 is a potent NIMA-related kinase NEK6 inhibitor with an IC50 of 3.4 μM. ZINC05007751 shows antiproliferative activity against a panel of human cancer cell lines, and displays a synergistic effect with Cisplatin and Paclitaxel in a BRCA2 mutated ovarian cancer cell line. ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity was observed against NEK2, NEK7, and NEK9[1].
ZINC05007751 (6 μM-190 μM; 24 hours) inhibits the growth of MDA-MB-231, PEO1, NCI-H1299 and HCT-15 with IC50 below 100 μM[1].ZINC05007751 induces perturbation of PEO1 cell cycle[1].ZINC05007751 (ovarian cancer cells PEO1) shows synergism with Cisplatin, resulting in a significant reduction of Cisplatin IC50 from 7.9 to 0.1 μM, with combination ZINC05007751 (44 μM) + Cisplatin (10 μM) exhibiting the greatest synergistic effect[1]. | [IC 50]
NEK6: 3.4 μM (IC50) | [References]
[1]. De Donato M, et al. Identification and antitumor activity of a novel inhibitor of the NIMA-related kinase NEK6. Sci Rep. 2018;8(1):16047. Published 2018 Oct 30. |
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| Company Name: |
DC Chemicals
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021-8447131 13564518121 |
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www.chemicalbook.com/showsupplierproductslist927327/0.htm |
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