PRT4165, E3 Ubiquitin-ligase Bmi1/Ring1A Inhibitor

PRT4165 is a small molecule inhibitor of polycomb repressive complex 1, which inhibits ubiquitin signaling at DNA double-strand breaks. PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation in vivo and in vitro. The drug also inhibits the accumulation of all detectable ubiquitin at sites of DNA double-strand breaks (DSBs), the retention of several DNA damage response proteins in foci that form around DSBs, and the repair of the DSBs.

Product information

CAS Number: 31083-55-3

Molecular Weight: 235.24

Formula: C15H9NO2

Chemical Name: 2-(pyridin-3-ylmethylene)-1H-indene-1,3(2H)-dione

Smiles: O=C1C(=CC2=CN=CC=C2)C(=O)C2=CC=CC=C12

InChiKey: OMHZFEWYVFWVLI-UHFFFAOYSA-N

InChi: InChI=1S/C15H9NO2/c17-14-11-5-1-2-6-12(11)15(18)13(14)8-10-4-3-7-16-9-10/h1-9H

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

PRT4165 was used at 10-50 µM final concentration in various in vitro assays.

References:

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.