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
Biological ActivityPDD 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.
External Portal InformationChemicalprobes.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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Complete Your Research
First-in-class chemical probes against poly(ADP-ribose) glycohydrolase (PARG) inhibit DNA repair with differential pharmacology to Olaparib.
James et al.
ACS Chem.Biol., 2016;11:3179
Specific killing of DNA damage-response deficient cells with inhibitor of poly(ADP-ribose) glycohydrolase.
Gravells et al.
DNA Repair, 2017;52:81
Selective small molecule PARG inhibitor causes replication fork stalling and cancer cell death.
Houl et al.
Citations for PDD 00017273
The citations listed below are publications that use Tocris products. Selected citations for PDD 00017273 include:
4 Citations: Showing 1 - 4
Unanchored tri-NEDD8 inhibits PARP-1 to protect from oxidative stress-induced cell death.
Authors: Keuss Et al.
EMBO J 2019;38
Selective Small Molecule PARG Inhibitor Causes Replication Fork Stalling and Cancer Cell Death.
Authors: Houl Et al.
Nat Commun 2019;10:5654
The CHD6 chromatin remodeler is an oxidative DNA damage response factor.
Authors: Moore Et al.
Nat Commun 2019;10:241
The Importance of Poly(ADP-Ribose) Polymerase as a Sensor of Unligated Okazaki Fragments during DNA Replication.
Authors: Hanzlikova Et al.
Mol Cell 2018;71:319
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