PRT4165

Synonyms: NSC600157

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.

PRT4165 Chemical Structure

PRT4165 Chemical Structure

CAS: 31083-55-3

Selleck's PRT4165 has been cited by 4 publications

Purity & Quality Control

Batch: Purity: 98.80%
98.80

PRT4165 Related Products

Choose Selective E3 Ligase Inhibitors

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] BMI-1 [1]
(Cell-free assay)
3.9 μM 3.9 μM
In vitro
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].
Cell Research 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.

Chemical Information & Solubility

Molecular Weight 235.24 Formula

C15H9NO2

CAS No. 31083-55-3 SDF --
Smiles C1=CC=C2C(=C1)C(=O)C(=CC3=CN=CC=C3)C2=O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 11 mg/mL ( (46.76 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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

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