PRT4165, E3 Ubiquitin-ligase Bmi1/Ring1A Inhibitor

Catalog No. size PriceQuantity
M60245-2S 2 mg solid $79
M60245-10S 10mg solid $324


Product Information
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:


  • 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. 


Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed