PRT4165

Catalog No.S5315

PRT4165 Chemical Structure

Molecular Weight(MW): 235.24

PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro.

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Biological Activity

Description PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro.
Targets
Bmi1/Ring1A [1]
()
3.9 μM
In vitro

PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation in vivo and in vitro. It inhibits the accumulation of all detectable ubiquitin at sites of DNA double-strand breaks (DSBs), the retention of several DNA damage response proteins in foci that form around DSBs, and the repair of the DSBs. PRT4165 inhibits both RNF2 and RING 1A, which are partially redundant paralogues that together account for the E3 ubiquitin ligase activity found in PRC1 complexes, but not RNF8 nor RNF168. U2OS cells treated with increasing concentrations of PRT4165 show increasing numbers of cells in G2/M[2].

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: HeLa cells
  • Concentrations: 50 μM
  • Incubation Time: 5 h
  • Method: HeLa cells are transfected with Bmi1-FLAG, Ring1A and HA-ubiquitin. Twenty-four hours post transfection the cells are treated with either solvent (0.5% DMSO, 0.5% PEG400) or 50 μM PRT4165 for 5 hours. Bmi1-FLAG is immunoprecipitated from cell lysates, and conjugated ubiquitin is detected by Western-blot with anti-HA antibody.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: CD-1 mice
  • Formulation: sesame oil containing 10% ethanol
  • Dosages: 4 mg/kg and 8 mg/kg
  • Administration: intraluminally injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 11 mg/mL (46.76 mM)
Ethanol 4 mg/mL (17.0 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 235.24
Formula

C15H9NO2

CAS No. 31083-55-3
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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E3 Ligase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID