PRT 4165

Name: PRT 4165
Brand: Tocris Bioscience
SKU: 5047

Tocris Bioscience, part of Bio-Techne | Catalog # 5047

Citations (21)

COA / SDS

Inhibitor of Bmi1/Ring1A; blocks histone H2A ubiquitination

Key Product Details

Description:	Inhibitor of Bmi1/Ring1A; blocks histone H2A ubiquitination
Chemical Name:	2-(3-Pyridinylmethylene)-1H-Indene-1,3(2H)-dione
Purity:	≥98% (HPLC)
Molecular Weight:	235.24

View Full Technical Details for PRT 4165

Technical Data
Citations

Biological Activity for PRT 4165

PRT 4165 is an inhibitor of Bmi1/Ring1A, subunits of the polycomb repressive complex 1 (PRC1); PRT 4165 inhibits self-ubiquitination (IC₅₀ = 3.9 μM) but does not increase cellular levels of either subunit. PRT 4165 prevents Bmi1/Ring1A-mediated ubiquitination and drug-induced degradation of topoisomerase 2α (Top2α). PRT 4165 inhibits the in vitro E3 ubiquitin ligase activity of RNF2 and a Bmi1/RNF2 complex, inhibiting H2A/H2AX ubiquitination. PRT 4165 blocks polycomb repressor complex (PRC) 1-mediated histone H2A ubiquitination in vitro.

Compound Libraries for PRT 4165

PRT 4165 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for PRT 4165

M. Wt	235.24
Formula	C₁₅H₉NO₂
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	31083-55-3
PubChem ID	207893
InChi Key	OMHZFEWYVFWVLI-UHFFFAOYSA-N
Smiles	O=C(C2=CC=CC=C2C3=O)/C3=C\C1=CC=CN=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PRT 4165

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	23.52	100
	1eq. HCl	1.18	5 with gentle warming

Preparing Stock Solutions for PRT 4165

The following data is based on the product molecular weight 235.24.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	4.25 mL	21.25 mL	42.51 mL
5 mM	0.85 mL	4.25 mL	8.50 mL
10 mM	0.43 mL	2.13 mL	4.25 mL
50 mM	0.09 mL	0.43 mL	0.85 mL

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References for PRT 4165

References are publications that support the biological activity of the product.

Ismail A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks. J.Biol.Chem. 2013 PMID: 23902761
Alchanati The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2α cleavage complex - a potentially new drug target. PLoS One 2009 PMID: 19956605