PDD 00017273

Name: PDD 00017273
Brand: Tocris Bioscience
SKU: 5952

Tocris Bioscience, part of Bio-Techne | Catalog # 5952

Citations (52)

COA / SDS

Potent and selective PARG inhibitor; cell permeable

Key Product Details

Description:	Potent and selective PARG inhibitor; cell permeable
Chemical Name:	1-[(1,3-Dimethyl-1H-pyrazol-5-yl)methyl]-1,2,3,4-tetrahydro-N-(1-methylcyclopropyl)-3-[(2-methyl-5-thiazolyl)methyl]-2,4-dioxo-6-quinazolinesulfonamide
Purity:	≥98% (HPLC)
Molecular Weight:	514.62

View Full Technical Details for PDD 00017273

Technical Data
Citations

Biological Activity for PDD 00017273

PDD 00017273 is a potent and selective poly (ADP ribose) glycohydrolase (PARG) inhibitor (IC₅₀ = 26 nM). Exhibits >350-fold selectivity for PARG over a panel of ion channels, enzymes and receptors, including PARP1 and ARH3. Maintains PAR chains and induces DNA double-stranded breaks in cells following DNA damage. Decreases colony formation of ZR-75-1 BRCA1 WT cells and inhibits cancer cell survival. Cell permeable.

Compound Libraries for PDD 00017273

PDD 00017273 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PDD 00017273 is reviewed on the chemical probes website.

Technical Data for PDD 00017273

M. Wt	514.62
Formula	C₂₃H₂₆N₆O₄S₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1945950-21-9
PubChem ID	121398766
InChi Key	IFWUBRBMMNTBRZ-UHFFFAOYSA-N
Smiles	O=C(C1=CC(S(NC2(CC2)C)(=O)=O)=CC=C1N3CC4=CC(C)=NN4C)N(CC5=CN=C(C)S5)C3=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PDD 00017273

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	51.46	100

Preparing Stock Solutions for PDD 00017273

The following data is based on the product molecular weight 514.62.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.94 mL	9.72 mL	19.43 mL
5 mM	0.39 mL	1.94 mL	3.89 mL
10 mM	0.19 mL	0.97 mL	1.94 mL
50 mM	0.04 mL	0.19 mL	0.39 mL

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References for PDD 00017273

References are publications that support the biological activity of the product.

Kliza Reading ADP-ribosylation signaling using chemical biology and interaction proteomics. Mol. Cell 2021 PMID: 34551281
Gravells Specific killing of DNA damage-response deficient cells with inhibitor of poly(ADP-ribose) glycohydrolase. DNA Repair 2017 PMID: 28254358
Houl Selective small molecule PARG inhibitor causes replication fork stalling and cancer cell death. Nat.Commun. 2019 PMID: 31827085
James First-in-class chemical probes against poly(ADP-ribose) glycohydrolase (PARG) inhibit DNA repair with differential pharmacology to Olaparib. ACS Chem.Biol. 2016 PMID: 27689388