Art. -Nr.: HY-108360

PDD 00017273

26 Cited Publications

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Based on 26 publication(s) in Google Scholar

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

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Reinheit: 99.64%
CAS. Nr.: 1945950-21-9
Formel: C₂₃H₂₆N₆O₄S₂
Molecular Weight:514.62

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PDD 00017273 Chemical Structure

CAS. Nr.: 1945950-21-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (26)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Chemical Information

CAS. Nr. 1945950-21-9
Appearance Solid
Molecular Weight 514.62
Formel C₂₃H₂₆N₆O₄S₂
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (26)

All IFHistological Imaging/StainingCell Proliferation/Viability AssayIPWB

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Journal Impact Factor

Nat Cell Biol

Full-length GSDME mediates pyroptosis independent from cleavage. [Abstract]

2024 Sep;26(9):1545-1557. PMID: 38997456
Mol Cell

Uracil processing by SMUG1 in the absence of UNG triggers homologous recombination and selectively kills BRCA1/2-deficient tumors. [Abstract]

2025 Mar 20;85(6):1072-1084.e10. PMID: 40010343
Nat Commun

Selective targeting of genome amplifications and repeat elements by CRISPR-Cas9 nickases to promote cancer cell death. [Abstract]

2025 Jun 2;16(1):5126. PMID: 40456709

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.
Nat Commun

Covalent PARylation of DNA base excision repair proteins regulates DNA demethylation. [Abstract]

2024 Jan 2;15(1):184. PMID: 38167803
Acta Pharm Sin B

PARylation promotes acute kidney injury via RACK1 dimerization-mediated HIF-1 α degradation. [Abstract]

2025 Sep;15(9):4673-4691. PMID: 41049746

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

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. [Abstract]

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. [Abstract]

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. [Abstract]

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. [Abstract]

Western blot analysis of PAR expression in PDD (PDD 00017273) (1 μmol/L)-treated HK2 cells.
Nucleic Acids Res

CHD1L maintains genome integrity by facilitating okazaki fragment maturation. [Abstract]

2026 Jun 22;54(12):gkag606. PMID: 42328796
Nucleic Acids Res

Nuclear poly(A)-binding protein and nucleolin utilize their RNA recognition motifs to read PAR chains. [Abstract]

2025 Oct 28;53(20):gkaf1090. PMID: 41182901
Proc Natl Acad Sci U S A

Muscle PARP1 inhibition extends lifespan through AMPKα PARylation and activation in Drosophila. [Abstract]

2023 Mar 28;120(13):e2213857120. PMID: 36947517
Cell Rep

Uncovering genetic interactions in the DNA repair network in response to endogenous damage and ionizing radiation. [Abstract]

2026 Jan 16;45(1):116850. PMID: 41546867
Cell Rep

PARP1-mediated PARylation activity is essential for oligodendroglial differentiation and CNS myelination. [Abstract]

2021 Oct 5;37(1):109695. PMID: 34610310
Clin Transl Med

PARylation of HMGA1 desensitizes esophageal squamous cell carcinoma to olaparib. [Abstract]

2024 Dec;14(12):e70111. PMID: 39690136
Br J Cancer

PARP inhibition leads to synthetic lethality with key splicing-factor mutations in myelodysplastic syndromes. [Abstract]

2024 Jul;131(2):231-242. PMID: 38806724
Sci Signal

PARP1-mediated PARylation of TEAD4 stabilizes the YAP1-TEAD4 complex and promotes growth and immune evasion in breast cancer cells. [Abstract]

2025 Oct 21;18(909):eadx2532. PMID: 41118450
Elife

Development and characterization of new tools for detecting poly(ADP-ribose) in vitro and in vivo. [Abstract]

2022 Apr 27;11:e72464. PMID: 35476036
Am J Physiol Cell Physiol

Increasing cellular NAD+ protects hepatocytes against palmitate-induced lipotoxicity by preventing PARP-1 inhibition and the mTORC1-p300 pathway activation. [Abstract]

2025 Mar 1;328(3):C776-C790. PMID: 39871470
Viruses

Role of PARP-1 in Human Cytomegalovirus Infection and Functional Partners Encoded by This Virus. [Abstract]

2022 Sep 15;14(9):2049. PMID: 36146855
FEBS Lett

Hyperosmotic stress induces PARP1-mediated HPF1-dependent mono(ADP-ribosyl)ation. [Abstract]

2026 Mar 31. PMID: 41914023
Cancer Rep (Hoboken)

Genomic and biological aspects of resistance to selective poly(ADP-ribose) glycohydrolase inhibitor PDD00017273 in human colorectal cancer cells. [Abstract]

2023 Feb;6(2):e1709. PMID: 36053937
J Obstet Gynaecol Res

The role of poly (ADP-ribose) glycohydrolase in phosphatase and tensin homolog deficiency endometrial cancer. [Abstract]

2023 Apr;49(4):1244-1254. PMID: 36759425
Res Sq

2026 Jun 17.
bioRxiv

2026 May 21.
bioRxiv

PARP16 is a Druggable Regulator of Ribosome MARylation and Protein Homeostasis in Ovarian Cancer Cells. [Abstract]

2026 Apr 2:2026.04.01.715986. PMID: 41959139
bioRxiv

2025 Nov 6.
Patent

US20240252689A1
bioRxiv

Chromatin regulator HELLS mediates SSB repair and responses to DNA alkylation damage. [Abstract]

2024 Dec 21:2024.12.19.629292. PMID: 39763743
bioRxiv

Global remodeling of ADP-ribosylation by PARP1 suppresses influenza A virus infection. [Abstract]

2024 Sep 19:2024.09.19.613696. PMID: 39345583

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9432 mL

9.7159 mL

19.4318 mL

5 mM

0.3886 mL

1.9432 mL

3.8864 mL

10 mM

0.1943 mL

0.9716 mL

1.9432 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

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].

MedChemExpress (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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. James DI, et al. First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to AZD2281. ACS Chem Biol. 2016 Nov 18;11(11):3179-3190. Epub 2016 Oct 12. [Content Brief]

[2]. Gravells P, et al. Specific killing of DNA damage-response deficient cells with inhibitors of poly(ADP-ribose) glycohydrolase. DNA Repair (Amst). 2017 Apr;52:81-91. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

PDD 00017273

26 Cited Publications

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PDD 00017273

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Peptidomimetic Library

Anti-Aging Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PDD 00017273

Biologische Aktivität

Chemical Information

Publications (26)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PDD 00017273

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Peptidomimetic Library

Anti-Aging Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PDD 00017273

Biologische Aktivität

Chemical Information

Publications (26)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PDD 00017273 Related Classifications

HY-108360 Related Classifications