TZ9

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TZ9 是一种选择性的?Rad6?抑制剂。TZ9 能抑制?Rad6B?诱导的组蛋白?H2A?泛素化，下调细胞内?β-catenin，诱导 G2-M 停滞和凋亡，并抑制转移性人类乳腺癌细胞的增殖和迁移。

A novel selective inhibitor of Rad6 ubiquitin conjugating enzyme; inhibits Rad6B-ubiquitin thioester formation and subsequent ubiquitin transfer to histone H2A, with no activity for UbcH5; potently inhibits proliferation, colony formation, and migration and induces MDA-MB-231 breast cancer cell G2-M arrest and apoptosis.

TZ9 (Rad6B SMI #9) (0.5-100 μM; 72 h) inhibits MDA-MB-231 cell proliferation and migration.TZ9 (0.1-5 μM; 24-72 h) delays cell-cycle progression in MDA-MB-231 cells.TZ9 (5 μM; 8-48 h) induces apoptosis in MDA-MB-231 cells.TZ9 (0.5, 1, 2.5, 5 μM; 24 h) inhibits H2A ubiquitination and downregulates levels of PCNA and β-catenin protein in MDA-MB-231 cells. Cell Proliferation Assay Cell Line:MDA-MB-231 cells Concentration: 0.5-100 μM Incubation Time:72 h Result:Inhibited MDA-MB-231 cell proliferation with IC50 ~6μM.Apoptosis Analysis Cell Line:MDA-MB-231 cells Concentration:5 μM Incubation Time:8-48 h Result:Induced cells apoptosis.Cell Cycle Analysis Cell Line:MDA-MB-231 cells Concentration:0.1-5 μM Incubation Time:24-72 h Result:Increased the proportion of G2-M-arrested cells by 2-fold and was accompanied by a proportional decrease in S-phase cells when at 24 h.Significantly increased the percentage of cells with cytoplasmic/nuclear cyclin B1 staining.Western Blot Analysis Cell Line:MDA-MB-231 cells Concentration:0.5, 1, 2.5, 5 μM Incubation Time:24 h Result:Inhibited H2A ubiquitination, decreased PCNA and β-catenin protein levels.

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TZ-9 | Rad6-SMI-9

Proteasome/Ubiquitin

E2

E2

Cancer

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1002789-86-7

366.3309

C17H14N6O4

>98% (HPLC)

DMSO: ≥ 40 mg/mL

O=C(OCC1=NC(N)=NC(NC2=CC=CC=C2)=N1)C3=CC=C([N+]([O-])=O)C=C3

1,3,5-Triazine-2-methanol, 4-amino-6-(phenylamino)-, 2-(4-nitrobenzoate)

(-20℃)

With Ice Pack

≥ 2 years