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PRT4165 | E3 ubiquitin ligase inhibitor

PRT-4165 (31083-55-3) is an inhibitor of Bmi1/Ring1A, subunits of the polycomb repressive complex 1 (PRC1). Inhibits self-ubiquitination (IC50 = 3.9 μM) but does not increase cellular levels of either subunit. Blocks Bmi1/Ring1A-mediated ubiquitination and drug-induced degradation of topoisomerase 2α.1 PRT-4165 inhibits H2A/H2AX ubiquitination via blocking the E3 ubiquitin ligase activity of RNF2 and a Bmi1/RNF2 complex. Blocks polycomb repressor complex (PRC) 1-mediated histone H2A ubiquitination in vitro and in vivo and as such represents a new tool for studying chromatin remodeling.2

References/Citations

1) Alchanati et al. (2009), The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2alpha cleavage complex – a potentially new drug target; PLoS One, 4 e8104
2) Ismail et al. (2013), A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks; J. Biol. Chem., 288 26944

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Focus Biomolecules cell signaling supplier, chemical structure of PRT4165 | E3 ubiquitin ligase inhibitor | CAS 31083-55-3

Catalog#  10-1478-0010

$65.00
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CAS:
31083-55-3
Catalog Number:
10-1478
Activity:
E3 ubiquitin ligase inhibitor
Chemical Name:
2-(3-Pyridinylmethylene)-1H-indene-1,3(2H)-dione
Molecular Weight:
235.24
Molecular Formula:
C15H9NO2
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 6 mg/ml with warming).
Physical Properties:
Yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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