1. Cell Cycle/DNA Damage
  2. Poly(ADP-ribose) Glycohydrolase (PARG)
  3. PDD 00017273

PDD 00017273 is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG), with an IC50 of 26 nM, and a KD of 1.45 nM.

For research use only. We do not sell to patients.

CAS No. : 1945950-21-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of PDD 00017273:

Top Publications Citing Use of Products

    PDD 00017273 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jun 2;16(1):5126.  [Abstract]

    PDD 00017273 (20 nM, 0-3 days). Evaluation of SK-N-BE(2)C cell proliferation in the presence of Cas9D10A targeting different loci or small molecule inhibitors (SMIs) to be used in combination with Cas9D10A.

    PDD 00017273 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Sep;15(9):4673-4691.

    Double staining of PAR and LTL in PDD 00017273 (PDD) (10 mg/kg, i.p., 12 h before CIS)-treated mice with CIS-induced AKI.

    PDD 00017273 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Sep;15(9):4673-4691.

    PAS staining indicating tubular injury in mice with CIS-induced AKI with or without PDD 00017273 (PDD) (10 mg/kg, i.p., 12 h before CIS).

    PDD 00017273 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Sep;15(9):4673-4691.

    MTT cell survival assay of HK2 cells at different PDD 00017273 (PDD) doses for 24 h.

    PDD 00017273 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Sep;15(9):4673-4691.

    Co-IP assay indicates the level of PARylated RACK1 in CIS-induced cells treated with PDD 00017273 (PDD, 1 μmol/L).

    PDD 00017273 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Sep;15(9):4673-4691.

    Western blot analysis of PAR expression in PDD (PDD 00017273) (1 μmol/L)-treated HK2 cells.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PDD 00017273 is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG), with an IC50 of 26 nM, and a KD of 1.45 nM[1][2].

    IC50 & Target

    IC50: 26 nM (PARG)[1]
    KD: 1.45 nM (PARG)[1]

    In Vitro

    PDD 00017273 is a potent inhibitor of PARG, with an IC50 of 26 nM, and a KD of 1.45 nM. PDD 00017273 (10 μM) does not inhibit five common Cytochrome P450 enzymes. PDD 00017273 (30 μM) modestly increasess phosphorylated H2AX (γH2AX) intensity, PDD 00017273 also decreases in NAD/H through PARG inhibition after DNA damage. PDD 00017273 suppresses the ZR-75-1 cells carring BRCA1 and BRCA2 wild type, and exhibits less potent activities against MDA-MB-436 cells carry the 5396 + 1G>A mutation in BRCA1[1]. PDD 00017273 (0.3 μM) inhibits degradation of PAR polymers in MCF7 cells. PDD 00017273 (0.3 μM) also reduces the viability of BRCA1, BRCA2, PALB2, FAM175A, and BARD1 depleted cells. PDD 00017273 stalls replication forks and induces DNA damage that requires homologous recombination (HR) for repair[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    514.62

    Formula

    C23H26N6O4S2

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=S(C1=CC2=C(N(CC3=CC(C)=NN3C)C(N(CC4=CN=C(C)S4)C2=O)=O)C=C1)(NC5(C)CC5)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (48.58 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9432 mL 9.7159 mL 19.4318 mL
    5 mM 0.3886 mL 1.9432 mL 3.8864 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.86 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.86 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.64%

    References
    Kinase Assay
    [1]

    Briefly, PARG in vitro assays are conducted in a total volume of 15 μL in a standard 384-well format. A total of 5 μL of human full length PARG used at a final reaction concentration of 65 pM, is added to 5 μL of Bt-NAD ribosylated PARP1 substrate at a final reaction concentration of 4.8 nM in assay buffer (50 mM Tris pH 7.4, 0.1 mg/mL BSA, 3 mM EDTA, 0.4 mM EGTA, 1 mM DTT, 0.01% Tween 20, 50 mM KCl). The reaction is incubated at RT for 10 min, and then 5 μL of detection reagent is added. Detection reagent consists of 42 nM mAb anti-6HIS XL665 and 2.25 nM streptavidin europium cryptate, both at 3× working stock concentrations (final concentrations of 14 nM and 0.75 nM, respectively), in detection buffer (50 mM Tris pH 7.4, 0.1 mg/mL BSA and 100 mM KF). Following incubation at RT for 60 min in the dark, TR-FRET signal is measured at λEx 340 nm and λEm 665 nm and λEm 620 nm using a PHERAstar FS plate reader. The ratio is calculated as [Em665/EM620] × 104 for each well and used to calculate percent inhibition for test compounds[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    HeLa cells are seeded in 30 μL of media at 1 × 104 cells/mL in Greiner 384-well plates. A total of 16-24 h later, cells are treated with inhibitors (8 pt dose response, 0.01-30 μM, triplicates) or vehicle (DMSO) control. The outer wells are left undosed to account for edge effects. After 72 h, 50 μL of 3.7% formaldehyde/PBS is added to each well, and cells are fixed for 20 min. Cells are then rinsed twice with PBS and stained for 1 h with Hoechst 33342/PBS (1:2000) in the dark. After two further rinses with PBS, images are captured and nuclei counted on a CellInsight. The maximum number of fields are captured from each triplicate well, which approximated to at least 1000 nuclei in vehicle-dosed wells[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9432 mL 9.7159 mL 19.4318 mL 48.5795 mL
    5 mM 0.3886 mL 1.9432 mL 3.8864 mL 9.7159 mL
    10 mM 0.1943 mL 0.9716 mL 1.9432 mL 4.8580 mL
    15 mM 0.1295 mL 0.6477 mL 1.2955 mL 3.2386 mL
    20 mM 0.0972 mL 0.4858 mL 0.9716 mL 2.4290 mL
    25 mM 0.0777 mL 0.3886 mL 0.7773 mL 1.9432 mL
    30 mM 0.0648 mL 0.3239 mL 0.6477 mL 1.6193 mL
    40 mM 0.0486 mL 0.2429 mL 0.4858 mL 1.2145 mL
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
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    Cat. No.:
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