ME0328 1445251-22-8

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Molecular Weight:

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


Biological Activity


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.


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.


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.

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Product Categories : Epigenetics > PARP Inhibitor