JNJ-1013
Based on 1 Customer Validation
JNJ-1013 is a potent and selective IRAK1 PROTAC degrader with an IC50s of 72, 443, 1071 nM for IRAK1, IRAK4, VHL FP respectively. JNJ-1013 induces apoptosis and increases the expression of cleavaged PARP. JNJ-1013 decreases the expression IRAK1, p-IKBα, pSTAT3(Tyr705) (Pink: ligand for target protein (HY-138834); black: linker (HY-Y1760); Blue: E3 ligase ligand (HY-112078)).
(Pink: IRAK1 Target protein ligand; Blue: VHL ligand (HY-112078); Black: linker).
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- Pureza: 99.97%
- No. CAS: 2597343-08-1
- Fòrmula: C46H55N9O7S
- Peso molecular:878.05
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Ver todos los productos específicos de isoformas PROTACs
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Actividad biológica
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IRAK1 72 nM (IC50) |
IRAK4 443 nM (IC50) |
VHL FP 1071 nM (IC50) |
JNJ-1013 (Degrader-3; 1.5-10000 nM; 24 h) dose-dependently degrades IRAK1 protein with an DC50 value of 3 nM.[1].
JNJ-1013 (1 µM) decreased the expression of MG-132 (HY-13259) stiyumed IRAK1 in a dose-dependent manner[1].
JNJ-1013 (0.01, 0.03, 0.1, 0.3, 1 µM; 24 h) decreases the expression IRAK1, p-IKBα, pSTAT3(Tyr705) and increases the expression of cleavaged PARP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells
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Concentration:1.5-10000 nM
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Incubation Time:24 h
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Result:Decreased the expression of IRAK1 in a dose-dependent manner.
Chemical Information
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No. CAS 2597343-08-1
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Appearance Solid
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Peso molecular 878.05
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Fòrmula C46H55N9O7S
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Color Light yellow to yellow
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SMILES
COC(C=C1N(CC2)CCC2OCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(N[C@H](C4=CC=C(C5=C(C)N=CS5)C=C4)C)=O)=O)=O)=C(C=C1)NC(C6=CC=CC(C7=CC=NN7)=N6)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 25 mg/mL (28.47 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 (protect from light). 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 (protect from light). 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 (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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, 6 months; -20°C, 1 month (protect from light). 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 | 1.1389 mL | 5.6944 mL | 11.3889 mL | 28.4722 mL |
| 5 mM | 0.2278 mL | 1.1389 mL | 2.2778 mL | 5.6944 mL | |
| 10 mM | 0.1139 mL | 0.5694 mL | 1.1389 mL | 2.8472 mL | |
| 15 mM | 0.0759 mL | 0.3796 mL | 0.7593 mL | 1.8981 mL | |
| 20 mM | 0.0569 mL | 0.2847 mL | 0.5694 mL | 1.4236 mL | |
| 25 mM | 0.0456 mL | 0.2278 mL | 0.4556 mL | 1.1389 mL |