PRT 4165

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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% (HPLC)
Citations (5)
Literature (3)

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 ≥99% (HPLC)
CAS Number 31083-55-3
PubChem ID 207893
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 Data for PRT 4165

Solvent Max Conc. mg/mL Max Conc. mM
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.

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

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References for PRT 4165

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

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, 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

5 Citations for PRT 4165

Citations are publications that use Tocris products. Selected citations for PRT 4165 include:

Patrick J et al (2022) Establishment of developmental gene silencing by ordered polycomb complex recruitment in early zebrafish embryos. Elife 11 PMID: 34982026

Yan et al (2019) The Polycomb Repressor Complex 1 Drives Double-Negative Prostate Cancer Metastasis by Coordinating Stemness and Immune Suppression. Cancer Cell 36 139-155.e10 PMID: 31327655

Zhu et al (2018) BMI1 regulates androgen receptor in prostate cancer independently of the polycomb repressive complex 1. Nat Commun 9 500 PMID: 29402932

Chagraoui et al (2018) SCL/TAL1 cooperates with Polycomb RYBP-PRC1 to suppress alternative lineages in blood-fated cells. Nat Commun 9 5375 PMID: 30560907

Do you know of a great paper that uses PRT 4165 from Tocris? Please let us know.

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Literature in this Area

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