Home / PARG Inhibitors / PDD 00017273

PDD 00017273

Catalog #: 5952
18 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
5952/10
5952/1
PDD 00017273 | CAS No. 1945950-21-9 | PARG Inhibitors
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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%

Product Details
Citations (18)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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.

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
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1945950-21-9

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.

Background References

  1. The CHD6 chromatin remodeler is an oxidative DNA damage response factor
    S Moore, ND Berger, MS Luijsterbu, CG Piett, FKT Stanley, CU Schräder, S Fang, JA Chan, DC Schriemer, ZD Nagel, H van Attiku, AA Goodarzi
    Nat Commun, 2019;10(1):241.
  2. 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
  3. Specific killing of DNA damage-response deficient cells with inhibitor of poly(ADP-ribose) glycohydrolase.
    Gravells et al.
    DNA Repair, 2017;52:81
  4. Selective small molecule PARG inhibitor causes replication fork stalling and cancer cell death.
    Houl et al.
    Nat.Commun., 2019;10:5654
  5. Differential regulation of breast cancer bone metastasis by PARP1 and PARP2
    H Zuo, D Yang, Q Yang, H Tang, YX Fu, Y Wan
    Nat Commun, 2020;11(1):1578.

Product Datasheets

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Citations for PDD 00017273

The citations listed below are publications that use Tocris products. Selected citations for PDD 00017273 include:

18 Citations: Showing 1 - 10

  1. Poly ADP-ribosylation of SET8 leads to aberrant H4K20 methylation in mammalian nuclear genome.
    Authors: Pierre-Olivier Et al.
    Commun Biol  2022;5:1292
  2. MDM2 binds and ubiquitinates PARP1 to enhance DNA replication fork progression.
    Authors: Matthias Et al.
    Cell Rep  2022;39:110879
  3. PARP inhibition impedes the maturation of nascent DNA strands during DNA replication.
    Authors: Margarita Et al.
    Nat Struct Mol Biol  2022;29:329-338
  4. CARM1 regulates replication fork speed and stress response by stimulating PARP1.
    Authors: Mark T Et al.
    Mol Cell  2021;81:784-800.e8
  5. Loss of nuclear DNA ligase III reverts PARP inhibitor resistance in BRCA1/53BP1 double-deficient cells by exposing ssDNA gaps.
    Authors: Jiri Et al.
    Mol Cell  2021;81:4692-4708.e9
  6. XRCC1 prevents toxic PARP1 trapping during DNA base excision repair.
    Authors: Keith W Et al.
    Mol Cell  2021;81:3018-3030.e5
  7. CDKL5 kinase controls transcription-coupled responses to DNA damage.
    Authors: Rachel Et al.
    EMBO J  2021;40:e108271
  8. NAD+ bioavailability mediates PARG inhibition-induced replication arrest, intra S-phase checkpoint and apoptosis in glioma stem cells.
    Authors: Mai Et al.
    NAR Cancer  2021;3:zcab044
  9. Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes Ovarian Cancer Cells to Poly ADP-Ribose Polymerase Inhibitors and Platinum Agents.
    Authors: Amber Et al.
    Front Oncol  2021;11:745981
  10. Pathological mutations in PNKP trigger defects in DNA single-strand break repair but not DNA double-strand break repair.
    Authors: Keith W Et al.
    Nucleic Acids Res  2020;48:6672-6684

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