PRT 4165

Catalog # Availability Size / Price Qty
5047/10
5047/50
Cat.No. 5047 - PRT 4165 | C15H9NO2 | CAS No. 31083-55-3
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Description: Inhibitor of Bmi1/Ring1A; blocks histone H2A ubiquitination

Chemical Name: 2-(3-Pyridinylmethylene)-1H-Indene-1,3(2H)-dione

Purity: ≥99%

Product Details
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Biological Activity

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. Prevents Bmi1/Ring1A-mediated ubiquitination and drug-induced degradation of topoisomerase 2α (Top2α). Also shown to inhibit the in vitro E3 ubiquitin ligase activity of RNF2 and a Bmi1/RNF2 complex, inhibiting H2A/H2AX ubiquitination. Blocks polycomb repressor complex (PRC) 1-mediated histone H2A ubiquitination in vitro and in vivo.

Technical Data

M.Wt:
235.24
Formula:
C15H9NO2
Solubility:
Soluble to 100 mM in DMSO and to 5 mM in 1eq. HCl with gentle warming
Purity:
≥99%
Storage:
Store at +4°C
CAS No:
31083-55-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.

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