PRT-4165, E3 Ubiquitin ligase inhibitor (TBI1478)

Description

Product Details

Formal Name: 2-(3-Pyridinylmethylene)-1H-indene-1,3(2H)-dione

Molecular Formula: C₁₅H₉NO₂

Formula Weight: 235.24

CAS Number: 31083-55-3

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 6 mg/ml with warming).

Storage: Room temperature

Stability: ≥ 1 year.

Applications

E3 Ubiquitin ligase inhibitor

Functions

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. 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.

Application Procedures

First dissolved in DMSO (up to 25 mg/ml) or in Ethanol (up to 6 mg/ml with warming), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.