PDD00017273

製品コードS8862 バッチS886201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C23H26N6O4S2
分子量 514.62 CAS No. 1945950-21-9
Solubility (25°C)* 体外 DMSO 100 mg/mL (194.31 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 PDD00017273 is a potent and selective poly (ADP ribose) glycohydrolase (PARG) inhibitor with an IC50 of 26 nM. PDD00017273 exhibits >350-fold selectivity for PARG over a panel of ion channels, enzymes and receptors, including PARP1 and ARH3.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Hela cells
濃度 0.01-30 μM
反応時間 72 h
実験の流れ

HeLa cells are seeded in 30 μL media at 1×104 cells/mL in 384-well plates. 16-24 h later, cells are treated with this compound (8 pt dose response, 0.01-30 μM, triplicates) or vehicle (DMSO) control. The outer wells are left un-dosed to account for edge effects. After 72 h, 50 μL of 3.7% Formaldehyde/PBS is added to each well and cells are fixed for 20 min. Cells are then rinsed twice with PBS and stained for 1 h with Hoechst 33342/PBS (1:2000) in the dark. After two further rinses with PBS, images are captured and nuclei counted on a CellInsight.

参考

  • https://pubmed.ncbi.nlm.nih.gov/27689388/

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：

XRCC1 mediates PARP1- and PAR-dependent recruitment of PARP2 to DNA damage sites [ Nucleic Acids Res, 2025, 53(4)gkaf086] PubMed: 39970298
The deubiquitination-PARylation positive feedback loop of the USP10-PARP1 axis promotes DNA damage repair and affects therapeutic efficacy of PARP1 inhibitor [ Oncogene, 2025, 44(29):2515-2529] PubMed: 40316740
PARP1 promotes replication-independent DNA double-strand break formation after acute DNA-methylation damage [ bioRxiv, 2025, 2025.07.10.663928] PubMed: 40672314
SLX4IP acts in parallel to FANCM to limit BLM-dependent replication stress at ALT telomeres [ bioRxiv, 2025, 2025.05.28.656696] PubMed: 40501906
FANCA Deficiency Induces Oncogenic R-Loop Dependent Synthetic Lethality with PARP1 Inhibitors [ Res Sq, 2025, rs.3.rs-6080272] PubMed: 40630542
PARP enzyme de novo synthesis of protein-free poly(ADP-ribose) [ Mol Cell, 2024, S1097-2765(24)00864-5] PubMed: 39536748
SNF2L suppresses nascent DNA gap formation to promote DNA synthesis [ Nucleic Acids Res, 2024, gkae903] PubMed: 39413208
Minimizing DNA trapping while maintaining activity inhibition via selective PARP1 degrader [ Cell Death Dis, 2024, 15(12):898] PubMed: 39695097
CHK1 inhibitor induced PARylation by targeting PARG causes excessive replication and metabolic stress and overcomes chemoresistance in ovarian cancer [ Cell Death Discov, 2024, 10(1):278] PubMed: 38862485
The three-dimensional structure of the EBV genome plays a crucial role in regulating viral gene expression in EBVaGC [ Nucleic Acids Res, 2023, 10.1093/nar/gkad936] PubMed: 37889078

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。

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