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PRT 4165

Catalog #: 5047
5 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
5047/10 In Stock10 mg / $111
5047/50 In Stock50 mg / $455

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PRT 4165 | CAS No. 31083-55-3 | Ubiquitin Ligase (E3) Inhibitors
1 Image
Description: Inhibitor of Bmi1/Ring1A; blocks histone H2A ubiquitination

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

Purity: ≥99%

Product Details
Citations (5)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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.

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

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Citations for PRT 4165

The citations listed below are publications that use Tocris products. Selected citations for PRT 4165 include:

5 Citations: Showing 1 - 5

  1. Establishment of developmental gene silencing by ordered polycomb complex recruitment in early zebrafish embryos.
    Authors: Patrick J Et al.
    Elife  2022;11
  2. The Polycomb Repressor Complex 1 Drives Double-Negative Prostate Cancer Metastasis by Coordinating Stemness and Immune Suppression.
    Authors: Yan Et al.
    Cancer Cell  2019;36:139-155.e10
  3. SCL/TAL1 cooperates with Polycomb RYBP-PRC1 to suppress alternative lineages in blood-fated cells.
    Authors: Chagraoui Et al.
    Nat Commun  2018;9:5375
  4. BMI1 regulates androgen receptor in prostate cancer independently of the polycomb repressive complex 1.
    Authors: Zhu Et al.
    Nat Commun  2018;9:500
  5. CBFβ-SMMHC Inhibition Triggers Apoptosis by Disrupting MYC Chromatin Dynamics in Acute Myeloid Leukemia.
    Authors: Carsten Et al.
    Cell  2018;174:172-186.e21

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