Biological Activity:

TZ9 is a selective and cell permeable inhibitor of human E2 ubiquitin-conjugating enzyme Rad6B. It binds to the Rad6B catalytic site, inhibits Rad6B-induced histone H2A ubiquitination, downregulates intracellular β-catenin. It can induce G2/M arrest and apoptosis, and inhibit proliferation and migration of metastatic human breast cancer cells (IC50 ~6 µM).

How to Use:

In vitro: TZ9 was used at 10-50 µM final concentration in vitro and in cellular assays.
In vivo: n/a


Reference:

• 1. Sanders MA, et al. Novel inhibitors of Rad6 ubiquitin conjugating enzyme: design, synthesis, identification, and functional characterization. (2013) Mol Cancer Ther. 12(4):373-83.