PDD 00017273

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Cat.No. 5952 - PDD 00017273 | C23H26N6O4S2 | CAS No. 1945950-21-9
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)
Datasheet
Citations (4)
Reviews
Literature (2)

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 and inhibits cancer cell survival. 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.

Compound Libraries

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

Technical Data

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 Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
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.

Select a batch to recalculate based on the batch molecular weight:
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

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

Houl et al (2019) Selective small molecule PARG inhibitor causes replication fork stalling and cancer cell death. Nat.Commun. 10 5654 PMID: 31827085


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View Related Products by Product Action

View all Poly(ADP-ribose) Glycohydrolase Inhibitors

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

4 Citations for PDD 00017273

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

Houl et al (2019) Selective Small Molecule PARG Inhibitor Causes Replication Fork Stalling and Cancer Cell Death. Nat Commun 10 5654 PMID: 31827085

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


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Literature in this Area

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
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  • Cell Cycle and DNA Damage Repair
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Epigenetics in Cancer

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.