PDD00017272
Based on 1 publication(s) in Google Scholar
PDD00017272 is an inhibitor of poly(ADP-ribose) glycohydrolase (PARG) (EC50=4.8 nM) and an activator of PARP1/2. PDD00017272 inhibits its activity of hydrolyzing poly(ADP-ribose) (pADPr), resulting in the accumulation of pADPr on chromatin, interfering with DNA damage repair and replication processes, and inducing PARP1/2-dependent cytotoxicity. PDD00017272 can be used in cancer models with DNA repair defects (such as BRCA mutations) or resistance to PARP inhibitors. PDD00017272 has a PARG expression level-correlated inhibitory potency with EC50 of 9.2 nM (PARG cells), the tumor cells with lower PARG expression are more sensitive.
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- Reinheit: 99.01%
- CAS. Nr.: 1945950-20-8
- Formel: C23H25N5O4S3
- Molecular Weight:531.67
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PDD00017272
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Biologische Aktivität
PDD00017272 (PARGi) (10 μM; 4 h) induces a significant increase in the level of chromatin-bound pADPr in HEK293A PARG knockout cells, and the signal was mainly concentrated in S phase cells, indicating that inhibition of PARG leads to the accumulation of endogenous pADPr at replication forks[1].
PDD00017272 (compound 34f) (0-100 μM; 72 h) significantly increases the sensitivity of PARG knockout cells to the drug in HEK293A wild-type and PARG knockout cells (IC50=96 μM and 210 nM, respectively), indicating that it has a cytotoxic effect related to PARG activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293A wild-type cells and PARG KO cells
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Concentration:0.01-100 μM
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Incubation Time:72 h
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Result:Showed an IC50 of 210 ± 30 nM against PARG KO cells, whereas exhibited an IC50 of 96 ± 24 μM against wild-type cells.
Reconstitution with wild-type PARG rescued viability, while a catalytically inactive PARG mutant failed to do so, confirming dependency on PARG enzymatic activity.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1945950-20-8
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Appearance Solid
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Molecular Weight 531.67
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Formel C23H25N5O4S3
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Color White to off-white
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SMILES
O=S(C1=CC2=C(N(CC3=C(C)N=C(C)S3)C(N(CC4=CN=C(C)S4)C2=O)=O)C=C1)(NC5(C)CC5)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
Mutant p53 Directs PARP to Regulate Replication Stress and Drive Breast Cancer Metastasis. [Abstract]2026 Mar 28:2026.03.26.713220. PMID: 41928956
Lösungsmittel & Löslichkeit
DMSO : ≥ 25 mg/mL (47.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Nie L, et al. DePARylation is critical for S phase progression and cell survival. Elife. 2024 Apr 5;12:RP89303. [Content Brief]
[2]. Bohdan Waszkowycz, et al. Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides. J Med Chem. 2018 Dec 13;61(23):10767-10792. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8809 mL | 9.4043 mL | 18.8087 mL | 47.0217 mL |
| 5 mM | 0.3762 mL | 1.8809 mL | 3.7617 mL | 9.4043 mL | |
| 10 mM | 0.1881 mL | 0.9404 mL | 1.8809 mL | 4.7022 mL | |
| 15 mM | 0.1254 mL | 0.6270 mL | 1.2539 mL | 3.1348 mL | |
| 20 mM | 0.0940 mL | 0.4702 mL | 0.9404 mL | 2.3511 mL | |
| 25 mM | 0.0752 mL | 0.3762 mL | 0.7523 mL | 1.8809 mL | |
| 30 mM | 0.0627 mL | 0.3135 mL | 0.6270 mL | 1.5674 mL | |
| 40 mM | 0.0470 mL | 0.2351 mL | 0.4702 mL | 1.1755 mL |
PDD00017272 Related Classifications
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