PRT 4165

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Cat.No. 5047 - PRT 4165 | C15H9NO2 | CAS No. 31083-55-3
Description: Inhibitor of Bmi1/Ring1A; blocks histone H2A ubiquitination
Chemical Name: 2-(3-Pyridinylmethylene)-1H-Indene-1,3(2H)-dione
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

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.

Compound Libraries

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

Technical Data

M. Wt 235.24
Formula C15H9NO2
Storage Store at +4°C
Purity ≥99% (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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 235.24. Batch specific molecular weights may vary from batch to batch due to solvent 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 8.5 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

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

Alchanati et al (2009) The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2α cleavage complex - a potentially new drug target. PLoS One 4 e8104 PMID: 19956605

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 PMID: 23902761


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View all Ubiquitin E3 Ligase Inhibitors

Keywords: PRT 4165, PRT 4165 supplier, PRT4165, E3, ubiquitin, ligase, inhibitors, inhibits, Bmi1, Ring1A, ubiquitination, ubiquitylation, topoisomerase, 2a, Top2a, Top2alpha, Top2α, polycomb, repressive, complex, 1, PRC1, RNF2, Bmi1/RNF2, Ubiquitin, Ligases, 5047, Tocris Bioscience

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