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ME0328

Catalog No. T6578   CAS 1445251-22-8

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

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ME0328 Chemical Structure
ME0328, CAS 1445251-22-8
Pack Size Availability Price/USD Quantity
5 mg In stock $ 47.00
10 mg In stock $ 67.00
25 mg In stock $ 148.00
50 mg In stock $ 278.00
100 mg In stock $ 493.00
1 mL * 10 mM (in DMSO) In stock $ 48.00
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Purity: 99.84%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
Targets&IC50 PARP3:0.89 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]
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 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 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. (Only for Reference)
Molecular Weight 321.37
Formula C19H19N3O2
CAS No. 1445251-22-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL (186.7 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Lindgren AE, et al. ACS Chem Biol. 2013, 8(8), 1698-1703.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cardiovascular Disease Compound Library NO PAINS Compound Library Anti-COVID-19 Compound Library DNA Damage & Repair Compound Library Anti-Prostate Cancer Compound Library Anti-Aging Compound Library Anti-Ovarian Cancer Compound Library Anti-Pancreatic Cancer Compound Library Bioactive Compound Library

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Keywords

ME0328 1445251-22-8 Chromatin/Epigenetic DNA Damage/DNA Repair PARP inhibit poly ADP ribose polymerase ME 0328 ME-0328 Inhibitor inhibitor

 

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