Home DNA Damage/DNA Repair PARP inhibitor ME0328

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ME0328 PARP inhibitor

Cat.No.S7438

ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
ME0328 PARP inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 321.37

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Quality Control

Batch: Purity: 99.95%
99.95

Solubility

In vitro
Batch:

DMSO : 64 mg/mL (199.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

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.

Chemical Information, Storage & Stability

Molecular Weight 321.37 Formula

C19H19N3O2

 Storage (From the date of receipt)
CAS No. 1445251-22-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(C1=CC=CC=C1)NC(=O)CCC2=NC3=CC=CC=C3C(=O)N2

Mechanism of Action

Targets/IC50/Ki
PARP3
0.89 μM
PARP1
6.3 μM
In vitro
ME0328 is soluble, cell permeable, and metabolically stable in human liver microsomes and rat hepatocytes. This compound (10 μM) results in a significant delay of γH2AX-foci resolution by affecting ARTD3 in A549 and MRC5 cells without significant toxicity.
Kinase Assay
Enzymatic Assays
Protein ADP-ribosylation is measured using hexahistidine-tagged ARTD proteins and recombinant histone proteins captured on 96-well Ni2+-chelating plates (5-PRIME). ADP-ribosylation reactions are initiated by addition of NAD+ (2% biotinylated), and modified reaction products are detected by chemiluminescence. Km values are estimated using plots of initial rates vs. NAD+ concentrations and linear curve fitting with GraphPad Prism. All compounds are dissolved in dimethyl sulfoxide (DMSO) to a stock concentration of 50 mM. Experiments to determine IC50 values are conducted with this compound concentrations in the range between 10 nM and 450 μM with a DMSO concentration of 1% (v/v). Measurements are carried out at an NAD+ concentration below Km for each transferase. IC50 values are estimated using curve fitting with GraphPad Prism. Reported values represent means ± SE of the fits of the curves based on duplicate or triplicate experiments, each determined based on three replicates.
References

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