TZ9 |
| رقم الكتالوجGC18561 |
TZ9 هو مثبط انتقائي Rad6يثبط TZ9 انتشار الهيستون H2A الناجم عن Rad6B ، ويقلل من تنظيم β-catenin داخل الخلايا ، ويحفز توقيف G2-M وموت الخلايا المبرمج ، ويمنع انتشار وانتقال خلايا سرطان الثدي البشرية النقيلية
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Cas No.: 1002789-86-7
Sample solution is provided at 25 µL, 10mM.
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TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.IC50 value: 6 uM [1]Target: Rad6 inhibitorThe bulk of MDA-MB-231 cells treated with 10 μmol/L or more SMI #9 displayed a round morphology compared with controls and less than 5 μmol/L doses of SMI #9. Simultaneous comparison of SMIs #8 and 9 confirmed SMI #9 inhibits Matrigel-induced migration of MDA-MB-231 cells in a dose-dependent manner compared with SMI #8. 5 μmol/L SMI #9 treatment triggered morphologic changes consistent with apoptosis in a time-dependent manner. 5 μmol/L SMI #9 treatment of MDA-MB-231 cells for 24 hours increased the proportion of G2–M-arrested cells by 2-fold and was accompanied by a proportional decrease in S-phase cells. SMIs #8 or 9 treatments dramatically reduced β-catenin staining as visualized by reduced merged Rad6/β-catenin yellow fluorescence.
References:
[1]. Sanders MA, et al. Novel inhibitors of Rad6 ubiquitin conjugating enzyme: design, synthesis, identification, and functional characterization. Mol Cancer Ther. 2013 Apr;12(4):373-83.
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