PCNA-I1
Based on 1 Customer Validation
PCNA-I1 is a selective small molecule inhibitor targeting proliferating cell nuclear antigen (PCNA) with anticancer activity. PCNA-I1 can stabilize the PCNA trimer structure (Kd=0.14-0.41μM), reduce its binding to chromatin, induce tumor cell cycle arrest, inhibit DNA replication and repair, and enhance the anti-tumor effect of DNA damaging agents. PCNA-I1 can be used in the study of targeted therapy for prostate cancer, lung cancer and other tumors.
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- Pureza: 98.78%
- No. CAS: 444930-42-1
- Fòrmula: C17H14N2O2S
- Peso molecular:310.37
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
PCNA-I1 (0.05-10 μM; 72 h) inhibits the cell viability of human prostate cancer (PC-3, LNCaP), breast cancer (MCF-7), melanoma (A375) cell lines in a concentration-dependent manner, with an average IC50 of 0.17 μM, which is significantly lower than that of normal cells[1].
PCNA-I1 (1 μM; 24-48 h) induces cell cycle arrest in S and G2/M phases and increases cell apoptosis[1].
PCNA-I1 (1 μM; 48 h) reduces PCNA binding to chromatin in PC-3 cells (NP-R fragment decreased by 50%), accompanied by nuclear p21 aggregation[1].
PCNA-I1 (1 μM; 24 h) increases the expression of γH2AX (a DNA damage marker) in PC-3 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-3, LNCaP (prostate cancer); MCF-7 (breast cancer); A375 (melanoma)
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Concentration:0.05, 0.1, 0.5, 1, 5, 10 μM
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Incubation Time:72 h
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Result:Dose-dependent inhibited cell growth with IC50 values: PC-3 (0.24 μM), LNCaP (0.14 μM), MCF-7 (0.15 μM), A375 (0.16 μM), while exhibited IC50 >1 μM against normal cells (e.g., HUVEC, mesenchymal stem cells).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c nude mice (8-10 weeks old) bearing LNCaP prostate cancer xenografts[3]
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Dosage:10 mg/kg
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Administration:Intravenous injection, 5 days/week for 2 consecutive weeks
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Result:Significantly retarded tumor growth, with tumor weight in treated mice being 28% of that in vehicle controls. No significant changes in body weight or hematology profiles (leukocytes, erythrocytes, thrombocytes) were observed, indicating minimal systemic toxicity.
Chemical Information
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No. CAS 444930-42-1
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Appearance Solid
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Peso molecular 310.37
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Fòrmula C17H14N2O2S
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Color Light yellow to yellow
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SMILES
O=C(N/N=C/C1=C(C2=CC=CC=C2C=C1)O)C3=C(C=CS3)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (322.20 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (275 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Tan Z, et al. Small-molecule targeting of proliferating cell nuclear antigen chromatin association inhibits tumor cell growth. Mol Pharmacol. 2012 Jun;81(6):811-9. [Content Brief]
[2]. Lu S, et al. Additive effects of a small molecular PCNA inhibitor PCNA-I1S and DNA damaging agents on growth inhibition and DNA damage in prostate and lung cancer cells. PLoS One. 2019 Oct 10;14(10):e0223894. [Content Brief]
[3]. Dillehay KL, et al. Antitumor effects of a novel small molecule targeting PCNA chromatin association in prostate cancer. Mol Cancer Ther. 2014 Dec;13(12):2817-26. [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 | 3.2220 mL | 16.1098 mL | 32.2196 mL | 80.5490 mL |
| 5 mM | 0.6444 mL | 3.2220 mL | 6.4439 mL | 16.1098 mL | |
| 10 mM | 0.3222 mL | 1.6110 mL | 3.2220 mL | 8.0549 mL | |
| 15 mM | 0.2148 mL | 1.0740 mL | 2.1480 mL | 5.3699 mL | |
| 20 mM | 0.1611 mL | 0.8055 mL | 1.6110 mL | 4.0275 mL | |
| 25 mM | 0.1289 mL | 0.6444 mL | 1.2888 mL | 3.2220 mL | |
| 30 mM | 0.1074 mL | 0.5370 mL | 1.0740 mL | 2.6850 mL | |
| 40 mM | 0.0805 mL | 0.4027 mL | 0.8055 mL | 2.0137 mL | |
| 50 mM | 0.0644 mL | 0.3222 mL | 0.6444 mL | 1.6110 mL | |
| 60 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3425 mL | |
| 80 mM | 0.0403 mL | 0.2014 mL | 0.4027 mL | 1.0069 mL | |
| 100 mM | 0.0322 mL | 0.1611 mL | 0.3222 mL | 0.8055 mL |
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