PDD 00017273

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Cat.No. 5952 - PDD 00017273 | C23H26N6O4S2 | CAS No. 1945950-21-9
Description: Potent and selective poly (ADP ribose) glycohydrolase (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)
Citations (3)

Biological Activity

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. Cell permeable.

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

M. Wt 514.62
Formula C23H26N6O4S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1945950-21-9
PubChem ID 121398766
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 Data

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

Preparing Stock Solutions

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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Product Datasheets

Certificate of Analysis / Product Datasheet
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References are publications that support the biological activity of the product.

James et al (2016) First-in-class chemical probes against poly(ADP-ribose) glycohydrolase (PARG) inhibit DNA repair with differential pharmacology to Olaparib. ACS Chem.Biol. 11 3179 PMID: 27689388

Gravells et al (2017) Specific killing of DNA damage-response deficient cells with inhibitor of poly(ADP-ribose) glycohydrolase. DNA Repair 52 81 PMID: 28254358

If you know of a relevant reference for PDD 00017273, please let us know.

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Keywords: PDD 00017273, PDD 00017273 supplier, PDD00017273, potent, selective, PARG, poly-(ADP-ribose)-glycohydrolase, inhibits, inhibitors, DNA, repair, Other, Hydrolases, 5952, Tocris Bioscience

3 Citations for PDD 00017273

Citations are publications that use Tocris products. Selected citations for PDD 00017273 include:

Keuss et al (2019) Unanchored tri-NEDD8 inhibits PARP-1 to protect from oxidative stress-induced cell death. EMBO J 38 PMID: 30804002

Moore et al (2019) The CHD6 chromatin remodeler is an oxidative DNA damage response factor. Nat Commun 10 241 PMID: 30651562

Hanzlikova et al (2018) The Importance of Poly(ADP-Ribose) Polymerase as a Sensor of Unligated Okazaki Fragments during DNA Replication. Mol Cell 71 319 PMID: 29983321

Do you know of a great paper that uses PDD 00017273 from Tocris? Please let us know.

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