Home / Ubiquitin Ligase (E3) Inhibitors / PRT 4165

PRT 4165

Catalog #: 5047
5 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
5047/10
5047/50
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.

Product Datasheets

Reconstitution Calculator
Molarity Calculator

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.

=
÷

Molarity Calculator

=
x
x
g/mol

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

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

FAQs

No product specific FAQs exist for this product, however you may

View all Small Molecule FAQs

Reviews for PRT 4165

There are currently no reviews for this product. Be the first to review PRT 4165 and earn rewards!

Have you used PRT 4165?

Submit a review and receive an Amazon gift card.

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review
Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.