| 产品描述: | TZ9 is a selective Rad6 inhibitor. TZ9 inhibits Rad6B-induced histone H2A ubiquitination, downregulates intracellular β-catenin, induces G2-M arrest and apoptosis, and inhibits the proliferation and migration of metastatic human breast cancer cells |
| 靶点: |
E1/E2/E3 Enzyme;Apoptosis;Apoptosis; E1/E2/E3Enzyme |
| 体外研究: |
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. |
| 参考文献: |
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. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.73 ml |
13.649 ml |
27.298 ml |
| 5 mM |
0.546 ml |
2.73 ml |
5.46 ml |
| 10 mM |
0.273 ml |
1.365 ml |
2.73 ml |
| 50 mM |
0.055 ml |
0.273 ml |
0.546 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |