ME0328

製品コードS7438 バッチS743801

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₉H₁₉N₃O₂

分子量

321.37

CAS No.

1445251-22-8

Solubility (25°C)*

体外

DMSO

64 mg/mL (199.14 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
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. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	Enzymatic Assays
キナーゼアッセイ	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.
細胞アッセイ	細胞株	A549 and MRC5 cells.
	濃度	~10 μM
	反応時間	72 hours
	実験の流れ	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.

参考

https://pubmed.ncbi.nlm.nih.gov/23742272/

カスタマーフィードバック

: Data from [Data independently produced by , , Nat Commun, 2017, 8:15110.]

: Data from [Data independently produced by , , Breast Cancer Res Treat, 2018, 172(1):23-32]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Parp3 assists muscle function and skeletal muscle differentiation by selectively adjusting H3K27me3 enrichment [ iScience, 2025, 28(4):112267]	PubMed: 40248123
PARP3 promotes macrophage inflammation via mono ADP ribosylation of Ppia Glu140 [ Mol Med, 2025, 31(1):216]	PubMed: 40461998
Curcumin sensitizes lymphoma cells to DNA damage agents through regulating Rad51-dependent homologous recombination [Zhao Q Biomed Pharmacother, 2018, 97:115-119]	PubMed: 29080451
Inhibition of Parp1 by BMN673 Effectively Sensitizes Cells to Radiotherapy by Upsetting the Balance of Repair Pathways Processing DNA Double-Strand Breaks [ Mol Cancer Ther, 2018, 17(10):2206-2216]	PubMed: 29970481
PARP3 inhibitors ME0328 and olaparib potentiate vinorelbine sensitization in breast cancer cell lines [Sharif-Askari B Breast Cancer Res Treat, 2018, 172(1):23-32]	PubMed: 30039287
The Development of a Biotinylated NAD+-Applied Human Poly(ADP-Ribose) Polymerase 3 (PARP3) Enzymatic Assay. [ SLAS Discov, 2018, 23(6):545-553]	PubMed: 29676938
PARP3 is a promoter of chromosomal rearrangements and limits G4 DNA. [Day TA, et al. Nat Commun, 2017, 8:15110]	PubMed: 28447610
CRISPR-mediated targeting of HER2 inhibits cell proliferation through a dominant negative mutation [Wang H Cancer Lett, 2017, 385:137-143]	PubMed: 27815036

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。