NSC636819
Based on 1 Customer Validation
NSC636819 is a competitive and selective inhibitor of KDM4A/KDM4B. KDM4A/KDM4B are potential progression factors for prostate cancer. NSC636819 has the potential for the research of cancer diseases, especially prostate cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.90%
- No. CAS: 1618672-71-1
- Fòrmula: C22H12Cl4N2O4
- Peso molecular:510.15
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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
Actividad biológica
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KDM4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
16.5 μM
Compound: 4, NSC636819
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Cytotoxicity against human LNCAP cells after 3 days by MTT assay
Cytotoxicity against human LNCAP cells after 3 days by MTT assay
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[PMID: 24971742] |
NSC636819 (compound 4) targets KDM4A and KDM4B with Ki of 5.5 μM and 3.0 μM, respectively[1].
NSC636819 (100 μM; 30 min) inhibits the demethylation activity of KDM4A and KDM4B and significantly reduces the level of H3K9me3 in LNCaP cells[1].NSC636819 (5-20 μM; 3 d) is cytotoxic (LNCaP IC50 = 16.5 μM) and induces apoptosis in LNCaP cells[1].NSC636819 (C-4) (10-20 μM; 2 d) strongly induces the expression of both TRAIL and its receptor DR5 selectively (mRNA and protein) in both TRAIL-sensitive (Calu-6 and MDA-MB231) and TRAIL-resistant cancer cells (A549 and H1299)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP cells
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:3 days
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Result:Almost completely blocked the demethylating activity toward H3K9me3 at 5 μM.
Resulted the inhibition of KDM4A/KDM4B,that specifically inhibits the demethylating activity of H3K9me3 and strongly blocks cell growth.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A549 Lung cancer xenograft model in mice[2]
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Dosage:20 mg/kg, 40 mg/kg
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Administration:ip; 5 times per weeks, 27 days; with or without ONC201 (i.p.; 25 mg/kg, 1 time a week).
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Result:Dose-dependently inhibited the tumor growth, and sensitized tumors to TRAIL.
Induced tumor expression of TRAIL, DR5 and the level of cleaved caspase-7 and H3K9me3, whereas decreased the expression of KDM4A in xenograft tumors.
Chemical Information
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No. CAS 1618672-71-1
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Appearance Solid
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Peso molecular 510.15
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Fòrmula C22H12Cl4N2O4
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Color Yellow to orange
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SMILES
ClC1=C(Cl)C=CC(/C=C/C2=C([N+]([O-])=O)C=C([N+]([O-])=O)C(/C=C/C3=CC(Cl)=C(Cl)C=C3)=C2)=C1
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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 : 5.1015 mg/mL (10.00 mM; Need ultrasonic and warming; 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 (274 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Chu CH, et al. KDM4B as a target for prostate cancer: structural analysis and selective inhibition by a novel inhibitor. J Med Chem. 2014;57(14):5975-5985. [Content Brief]
[2]. Wang J, et al. Silencing the epigenetic silencer KDM4A for TRAIL and DR5 simultaneous induction and antitumor therapy. Cell Death Differ. 2016 Nov 1;23(11):1886-1896. [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 | 1.9602 mL | 9.8010 mL | 19.6021 mL | 49.0052 mL |
| 5 mM | 0.3920 mL | 1.9602 mL | 3.9204 mL | 9.8010 mL |
NSC636819 Related Classifications
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