dASK1
dASK1 is a selective and cereblon (CRBN)-based PROTAC degrader of apoptosis signal-regulating kinase 1 (ASK1). dASK1 forms a stable ternary complex with ASK1, facilitating ASK1 rapid and sustained degradation via the ubiquitin-proteasome pathway. dASK1 demonstrates potent ASK1 degradation. dASK1 can be used for the research of steatohepatitis.
(Pink: ASK1 ligand (HY-174860); Blue: Cereblon ligand (HY-10984); Black: linker).
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- No. CAS: 3064086-31-0
- Fòrmula: C38H38F2N10O8
- Peso molecular:800.77
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Cereblon |
dASK1 (Compound 35) (1-5000 nM, 4-12 h) induces degradation of ASK1 in HepG2 and HEK293A cells[1].
dASK1 (1 nM to 10 μM, 24 h) shows no detectable toxicity in HepG2 cells[1].
dASK1 (10-200 nM, 8 h) shows proteasome dependence in degrading ASK1 in HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:1, 10, 50, 100, 500, and 1000 nM
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Incubation Time:4, 8, and 12 h
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Result:Demonstrated the highest degradation efficacy, achieving a maximum reduction of 70% in ASK1 protein levels at 100 nM.
Showed the most significant reduction in ASK1 protein levels at 8 h.
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Cell Line:HEK293A cells
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Concentration:1, 10, 50, 100, 500, 1000, and 5000 nM
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Incubation Time:8 h
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Result:Demonstrated the highest degradation efficacy at 10 nM.
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Cell Line:HepG2 cells
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Concentration:1, 10, 50, 100, 500, 1000, and 10000 nM
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Incubation Time:24 h
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Result:Showed no detectable toxicity.
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Cell Line:HepG2 cells
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Concentration:10, 50, 100, and 200 nM; 10 and 50 nM (pre-treating with 5 µM of MG132 (HY-13259) for 30 min)
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Incubation Time:8 h
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Result:Degraded ASK1 levels.
MG132 (HY-13259) blocked degradation and led to ASK1 accumulation.
Chemical Information
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No. CAS 3064086-31-0
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Peso molecular 800.77
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Fòrmula C38H38F2N10O8
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SMILES
O=C(NCCOCCNC1=CC=CC(C(N2C3C(NC(CC3)=O)=O)=O)=C1C2=O)CCC(NC4=C(F)C=C(F)C(C(NC5=NC(C6=NN=CN6C(C)C)=CC=C5)=O)=C4)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
dASK1 Related Classifications
HY-174862 Related Classifications
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