PNR-7-02
Based on 1 publication(s) in Google Scholar
PNR-7-02 is a dual Rev1 and human DNA polymerase η (hpol η) inhibitor, with an IC50 value of 8 μM against hpol η. PNR-7-02 binds to hpol η to disrupt the orientation of template DNA and block the catalytic function of hpol η. When used in combination with Cisplatin (HY-17394), PNR-7-02 induces DNA damage and replication stress in cells with intact hpol η function. PNR-7-02 can be used in mechanism studies related to chronic myeloid leukemia and ovarian cancer.
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- Reinheit: 98.0%
- CAS. Nr.: 1633660-76-0
- Formel: C24H16ClN3O2S
- Molecular Weight:445.92
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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
Publications Citing Use of MedChemExpress (MCE) PNR-7-02
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Biologische Aktivität
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DNA Polymerases 8 μM (IC50) |
PNR-7-02 inhibits human Pol η function by binding its little finger domain and synergizes with Cisplatin (HY-17394) to kill chronic myeloid leukaemia and ovarian cancer cell lines[1].
PNR-7-02 potently inhibits purified hpol η with an IC50 of 8 μM in a fluorescence-based activity assay[2].
PNR-7-02 (8-24 μM; 5 min) inhibits purified hpol η, hRev1, and hpol λ with equal potency (IC50 = 8 μM) and is 3-fold less potent against hpol κ[2].
PNR-7-02 (20-100 μM; 10-60 min) binds to purified hpol η near the little finger domain's L-helix, protecting Arg351 from HPG modification, and induces conformational changes in the palm domain at high concentrations[2].
PNR-7-02 acts synergistically with CDDP to reduce viability in hpol η-proficient HAP-1 cells (CI = 0.47-0.59) but does not affect CDDP sensitivity in hpol η-deficient HAP-1 cells; PNR-7-02 alone has EC50 values of 4.6 μM and 5.6 μM in hpol η-proficient and -deficient cells, respectively[2].
PNR-7-02 (0.1-1 μM) enhances CDDP-induced γH2AX formation (a marker of DNA damage/replication stress) by ~3-fold in hpol η-proficient HAP-1 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1633660-76-0
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Appearance Solid
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Molecular Weight 445.92
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Formel C24H16ClN3O2S
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Color Light yellow to yellow
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SMILES
O=C1NC(NC(/C1=C\C2=CN(CC3=CC4=C(C=CC=C4)C=C3)C5=C2C=C(Cl)C=C5)=O)=S
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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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Cell Rep
2026 Jun 23;45(6):117461. PMID: 42207643
Lösungsmittel & Löslichkeit
DMSO : 1 mg/mL (2.24 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)
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)
Reinheit & Dokumentation
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Data Sheet (280 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]. Ler AAL, et al. DNA Damage Tolerance Pathways in Human Cells: A Potential Therapeutic Target. Front Oncol. 2022;11:822500. Published 2022 Feb 7. [Content Brief]
[2]. Zafar MK, et al. A Small-Molecule Inhibitor of Human DNA Polymerase η Potentiates the Effects of Cisplatin in Tumor Cells. Biochemistry. 2018;57(7):1262-1273. [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 | 2.2426 mL | 11.2128 mL | 22.4255 mL | 56.0639 mL |
PNR-7-02 Related Classifications
HY-117664 Related Classifications
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