ME0328

Catalog No.S7438

For research use only.

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

ME0328 Chemical Structure

CAS No. 1445251-22-8

Selleck's ME0328 has been cited by 6 Publications

2 Customer Reviews

Purity & Quality Control

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Biological Activity

Description ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
Targets
PARP3 [1] PARP1 [1]
0.89 μM 6.3 μM
In vitro

ME0328 is soluble, cell permeable, and metabolically stable in human liver microsomes and rat hepatocytes. ME0328 (10 μM) results in a significant delay of γH2AX-foci resolution by affecting ARTD3 in A549 and MRC5 cells without significant toxicity. [1]

Protocol (from reference)

Kinase Assay:

[1]

  • 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 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.

Cell Research:

[1]

  • Cell lines: A549 and MRC5 cells.
  • Concentrations: ~10 μM
  • Incubation Time: 72 hours
  • Method:

    Compound cytotoxicity in A549 and MRC5 cells is evaluated using WST-1 assays. A549 cells are cultured in Dulbecco’s Modified Eagle’s Medium supplemented with 10% fetal calf serum (FCS), penicillin, and streptomycin. MRC5 cells are cultured in Minimal Essential Medium supplemented with 10% FCS, penicillin, streptomycin, and l-glutamine. Both cell lines are maintained in a humidified incubator at 37°C and 5% CO2.

Solubility (25°C)

In vitro

DMSO 64 mg/mL
(199.14 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 321.37
Formula

C19H19N3O2

CAS No. 1445251-22-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1=CC=CC=C1)NC(=O)CCC2=NC3=CC=CC=C3C(=O)N2

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
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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.

Molarity Calculator

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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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