HS-243
Based on 1 Customer Validation
HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC50 values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.95%
- No. CAS: 848249-10-5
- Fòrmula: C17H16N4O3
- Peso molecular:324.33
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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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IRAK inhibitor 2IRAK Inhibitor
Actividad biológica
Descripciòn
IC50 & Target
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IRAK4 20 nM (IC50) |
IRAK-1 24 nM (IC50) |
CLK4 662 nM (IC50) |
In Vitro
HS-243 (0-10 μM, 24 h) inhibits cell survival by 21% for AN3-CA (pancreatic cancer cell), and 13% for SKOV-3 (ovarian cancer cell)[1].
HS-243 (10 μM, 24 h) potently reduces the proinflammatory response of RA cells and macrophages, significantly reduces the secretion of 15 cytokines, including IL-8, CD14, GRO-α, MIP-1a, MIP-3a, uPAR, Osteopontin, MMP-9, MCP-1, I-TAC, TIM-3, IP-10, GDF-15, and RANTES[1].
HS-243 shows minimal to no percentage of inhibition against IRAK-4 Y262T or Y262A mutants at 0.3 and 1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-OV-3, AN3-CA, H460, ES-2, SK-UT-1B, COLO205, Bx-PC-3
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Concentration:1 nM, 10 nM, 100 nM, 1 μM, 10 μM, and 10 μM+IL-1β (30 ng/ml)
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Incubation Time:24 h
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Result:Inhibited cell survival by 21% for AN3-CA (pancreatic), and 13% for SKOV-3 (ovarian). The addition of IL-1β in conjunction with HS-243 increased cell death to 46% in SK-OV-3 (ovarian), 33% in AN3-CA (pancreatic), and 31% in H460 (colon).
Chemical Information
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No. CAS 848249-10-5
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Appearance Solid
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Peso molecular 324.33
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Fòrmula C17H16N4O3
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Color White to off-white
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SMILES
O=C(NC1=NC2=CC=CC=C2N1CCC)C3=CC=CC([N+]([O-])=O)=C3
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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 1 year -20°C 6 months
Solvente y solubilidad
In Vitro:
DMSO : 41.67 mg/mL (128.48 mM; Need ultrasonic; 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0833 mL | 15.4164 mL | 30.8328 mL | 77.0820 mL |
| 5 mM | 0.6167 mL | 3.0833 mL | 6.1666 mL | 15.4164 mL | |
| 10 mM | 0.3083 mL | 1.5416 mL | 3.0833 mL | 7.7082 mL | |
| 15 mM | 0.2056 mL | 1.0278 mL | 2.0555 mL | 5.1388 mL | |
| 20 mM | 0.1542 mL | 0.7708 mL | 1.5416 mL | 3.8541 mL | |
| 25 mM | 0.1233 mL | 0.6167 mL | 1.2333 mL | 3.0833 mL | |
| 30 mM | 0.1028 mL | 0.5139 mL | 1.0278 mL | 2.5694 mL | |
| 40 mM | 0.0771 mL | 0.3854 mL | 0.7708 mL | 1.9270 mL | |
| 50 mM | 0.0617 mL | 0.3083 mL | 0.6167 mL | 1.5416 mL | |
| 60 mM | 0.0514 mL | 0.2569 mL | 0.5139 mL | 1.2847 mL | |
| 80 mM | 0.0385 mL | 0.1927 mL | 0.3854 mL | 0.9635 mL | |
| 100 mM | 0.0308 mL | 0.1542 mL | 0.3083 mL | 0.7708 mL |
HS-243 Related Classifications
HY-134911 Related Classifications
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