ZINC05007751 |
Catalog No.GC63626 |
Le ZINC05007751 est un puissant inhibiteur de la kinase NEK6 liée À NIMA avec une IC50 de 3,4 μM. ZINC05007751 montre une activité antiproliférative contre un panel de lignées cellulaires cancéreuses humaines et affiche un effet synergique avec le cisplatine et le paclitaxel dans une lignée cellulaire de cancer de l'ovaire mutée BRCA2. Le ZINC05007751 est très sélectif contre NEK1 et NEK6, aucune activité significative n'a été observée contre NEK2, NEK7 et NEK9.
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Cas No.: 591239-68-8
Sample solution is provided at 25 µL, 10mM.
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].
[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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