Home Ubiquitin E3 Ligase inhibitor - BMI-1 inhibitor PRT4165

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PRT4165 E3 Ligase inhibitor

Cat.No.S5315

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 E3 Ligase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 235.24

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Chemical Information, Storage & Stability

Molecular Weight 235.24 Formula

C15H9NO2

 Storage (From the date of receipt)
CAS No. 31083-55-3 -- Storage of Stock Solutions

Synonyms NSC600157 Smiles C1=CC=C2C(=C1)C(=O)C(=CC3=CN=CC=C3)C2=O

Solubility

In vitro
Batch:

DMSO : 11 mg/mL (46.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Bmi1/Ring1A [1]
3.9 μM
BMI-1 [1]
(Cell-free assay)
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. This compound 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 this chemical show increasing numbers of cells in G2/M[2].
References

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