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.
In Vitro
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: MDA-MB-231 cells Concentration: 0.5-100 µM Incubation Time: 72 h Result: Inhibited MDA-MB-231 cell proliferation with IC 50 ~6µM. Apoptosis AnalysisCell Line: MDA-MB-231 cells Concentration: 5 µM Incubation Time: 8-48 h Result: Induced cells apoptosis. Cell Cycle AnalysisCell 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 AnalysisCell 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.
Form:Solid
Associated Targets(Human)
UBE2BTchemUbiquitin-conjugating enzyme E2 B (1 Activities)
