PRT 4165

Pricing Availability Delivery Time Qty
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
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
1eq. HCl 1.18 5mM with gentle warming
DMSO 23.52 100
ethanol 2.35 10mM 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.

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


If you know of a relevant reference for PRT 4165, please let us know.

View Related Products by Product Action

View all Ubiquitin E3 Ligase Inhibitors

Keywords: 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, E3, Ligases, Tocris Bioscience

Citations for PRT 4165

Citations are publications that use Tocris products.

Currently there are no citations for PRT 4165. Do you know of a great paper that uses PRT 4165 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Programmed Cell Death

Programmed Cell Death Poster

There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.

Pathways for PRT 4165

Protocols

TODO: Add Protocols