PDD00017273

Catalog No.S8862 Batch:S886201

Technical Data

Formula	C₂₃H₂₆N₆O₄S₂
Molecular Weight	514.62	CAS No.	1945950-21-9
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (194.31 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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.

Targets

PARG ^[1]
(Cell-free assay)

26 nM

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Hela cells Concentrations 0.01-30 μM Incubation Time 72 h Method 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 inhibitors (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.

Cell Assay:^{^[1]}

Cell lines
Hela cells
Concentrations
0.01-30 μM
Incubation Time
72 h
Method
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 inhibitors (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.

References

[1] James DI, et al. ACS Chem Biol. 2016, 11(11):3179-3190.

Selleck's PDD00017273 has been cited by 11 publications

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
The regulation loop of MARVELD1 interacting with PARP1 in DNA damage response maintains genome stability and promotes therapy resistance of cancer cells [ Cell Death Differ, 2023, 10.1038/s41418-023-01118-z]	PubMed: 36750717
Fatty acid oxidation facilitates DNA double-strand break repair by promoting PARP1 acetylation [ Cell Death Dis, 2023, 14(7):435]	PubMed: 37454129
Quantitative Detection of DNA-Protein Crosslinks and Their Post-Translational Modifications [ J Vis Exp, 2023, (194).]	PubMed: 37154555
PARP1 Inhibition Halts EBV+ Lymphoma Progression by Disrupting the EBNA2/MYC Axis [ bioRxiv, 2023, 2023.07.05.547847]	PubMed: 37461649
The three-dimensional structure of Epstein-Barr virus genome varies by latency type and is regulated by PARP1 enzymatic activity [ Nat Commun, 2022, 13(1):187]	PubMed: 35039491
Micropeptide PACMP inhibition elicits synthetic lethal effects by decreasing CtIP and poly(ADP-ribosyl)ation [ Mol Cell, 2022, S1097-2765(22)00085-5]	PubMed: 35219381
PARP1 and CHK1 coordinate PLK1 enzymatic activity during the DNA damage response to promote homologous recombination-mediated repair [ Nucleic Acids Res, 2021, gkab584]	PubMed: 34197606
PARP1 blockade is synthetically lethal in XRCC1 deficient sporadic epithelial ovarian cancers [ Cancer Lett, 2020, 469:124-133]	PubMed: 31669203

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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