(5Z)-2-hydroxy-4-methyl-6-oxo-5-[(5-phenylfuran-2-yl)methylidene]-5,6-dihydropyridine-3-carbonitrile
(5Z)-2-hydroxy-4-methyl-6-oxo-5-[(5-phenylfuran-2-yl)methylidene]-5,6-dihydropyridine-3-carbonitrile Basic information
- Product Name:
- (5Z)-2-hydroxy-4-methyl-6-oxo-5-[(5-phenylfuran-2-yl)methylidene]-5,6-dihydropyridine-3-carbonitrile
- Synonyms:
-
- (5Z)-2-hydroxy-4-methyl-6-oxo-5-[(5-phenylfuran-2-yl)methylidene]-5,6-dihydropyridine-3-carbonitrile
- NEK6 inibitor 8
- ZINC05007751
- 3-Pyridinecarbonitrile, 1,2,5,6-tetrahydro-4-methyl-2,6-dioxo-5-[(5-phenyl-2-furanyl)methylene]-
- NEK6 inhibitor 8
- HCT-15,NCI-H1299,PEO1,ovarian,Inhibitor,ZINC 05007751,inhibit,cells,ZINC05007751,NEK6,antiproliferative,ZINC-05007751
- 4-Methyl-2,6-dioxo-5-((5-phenylfuran-2-yl)methylene)-1,2,5,6-tetrahydropyridine-3-carbonitrile
- CAS:
- 591239-68-8
- MF:
- C18H12N2O3
- MW:
- 304.3
- Mol File:
- 591239-68-8.mol
(5Z)-2-hydroxy-4-methyl-6-oxo-5-[(5-phenylfuran-2-yl)methylidene]-5,6-dihydropyridine-3-carbonitrile Chemical Properties
- 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
(5Z)-2-hydroxy-4-methyl-6-oxo-5-[(5-phenylfuran-2-yl)methylidene]-5,6-dihydropyridine-3-carbonitrile Usage And Synthesis
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].
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.
(5Z)-2-hydroxy-4-methyl-6-oxo-5-[(5-phenylfuran-2-yl)methylidene]-5,6-dihydropyridine-3-carbonitrileSupplier
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(5Z)-2-hydroxy-4-methyl-6-oxo-5-[(5-phenylfuran-2-yl)methylidene]-5,6-dihydropyridine-3-carbonitrile(591239-68-8)Related Product Information
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