Antibodies
ME0328
- 貨號 Cat. No.
- S7438
- 規格 Size
- 10mgã€50mg
- 品牌 Brand
- Selleckchem
Description
ME0328
Catalog No.S7438
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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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
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. | |||||
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| Targets | PARP3 | PARP1 | ||||
| IC50 | 0.89 μM | 6.3 μM [1] | ||||
| 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] | |||||
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Protocol(Only for 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. |
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Cell Assay: [1]
| Cell lines | A549 and MRC5 cells. |
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| 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. |
References
Chemical Information
| Molecular Weight (MW) | 321.37 |
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| Formula | C19H19N3O2 |
| CAS No. | 1445251-22-8 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 64 mg/mL (199 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 3,4-Dihydro-4-oxo-3,4-Dihydro-4-oxo-N-[(1S)-1-phenylethyl]-2-quinazolinepropanamide |
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