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TZ9

Catalog No.GC18561

TZ9 est un inhibiteur sélectif de Rad6. TZ9 inhibe l'ubiquitination de l'histone H2A induite par Rad6B, régule négativement la β-caténine intracellulaire, induit l'arrêt et l'apoptose de G2-M, et inhibe la prolifération et la migration des cellules métastatiques du cancer du sein humain.

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TZ9 Chemical Structure

Cas No.: 1002789-86-7

Taille Prix Stock Qté
1mg Please Inquire Please Inquire
5mg
90,00 $US
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10mg
144,00 $US
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25mg Please Inquire Please Inquire

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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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