| Molecular Weight: | 235.24 |
| Formula: | C15H9NO2 |
| Purity: | ≥98% |
| CAS#: | 31083-55-3 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | 2-(pyridin-3-ylmethylene)-1H-indene-1,3(2H)-dione |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
PRT4165 is a potent and selective E3 Ubiquitin-ligase Bmi1/Ring1A Inhibitor, inhibits self-ubiquitination (IC50 ~3.9 μM) but does not increase cellular levels of either subunit. Bmi1/Ring1A are subunits of the polycomb repressive complex 1 (PRC1) and play an important role in aberrant gene silencing in human cancers. PRT4165 could prevent Bmi1/Ring1A-mediated ubiquitination and drug-induced degradation of topoisomerase 2α (Top2α). It also inhibits the in vitro E3 ubiquitin ligase activity of RNF2 and a Bmi1/RNF2 complex, inhibiting H2A/H2AX ubiquitination. It can block polycomb repressor complex (PRC) 1-mediated histone H2A ubiquitination in vitro. PRT4165 is a novel chromatin-remodeling compound and provides a new tool for the inhibition of ubiquitylation signaling at DNA double-strand breaks.
How to Use:
In vitro: PRT4165 was used at 10-50 µM final concentration in various in vitro assays.
In vivo: n/a
Reference:
- 1. Alchanati I, et al. The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2alpha cleavage complex - a potentially new drug target. (2009) PLoS One. 4(12):e8104.
- 2. Ismail IH, et al. A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks. (2013) J Biol Chem. 288(37):26944-54.
Products are for research use only. Not for human use.
