dASK1
dASK1 is a PROTAC degrader of ASK1 that recruits cereblon. dASK1 promotes ASK1 degradation in a dose- and time-dependent manner via the ubiquitin-proteasome pathway. dASK1 can be used in studies of metabolic dysfunction-associated steatohepatitis.
(Pink: ASK1 ligand (HY-174860); Blue: Cereblon ligand (HY-10984); Black: linker).
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- CAS No.: 3064086-31-0
- Formule: C38H38F2N10O8
- Masse moléculaire:800.77
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
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Cereblon |
In Vitro
dASK1 (compound 35) (1-1000 nM; 4-12 h) potently degrades ASK1 in HepG2 and HEK293A cells, achieving a maximum degradation rate of 70% after treatment at 100 nM for 8 h. Its mechanism of action is proteasome-dependent and does not induce cytotoxicity[1].
dASK1 (1-10000 nM) shows no cytotoxicity in the tested cell lines even at the highest concentration of 10000 nM[1].
dASK1 (10-200 nM; 8 h) mediates proteasome-dependent ASK1 degradation in HepG2 cells[1].
dASK1 forms specific hydrogen bonds and π-sulfur interactions with ASK1 and CRBN proteins in molecular docking studies[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2, HEK293A
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Concentration:1, 10, 100, 500, 1000 nM (WB); 1, 10, 100, 500, 1000, 10000 nM (MTT assay)
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Incubation Time:4, 8, 12 h (WB); 24 h (MTT assay)
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Result:Achieved a maximum 70% reduction in ASK1 protein levels at 100 nM in HepG2 cells after 8 hours.
Showed increased ASK1 levels at higher concentrations consistent with the Hook effect.
Demonstrated the most significant degradation after 8-hour incubation compared to 4-hour or 12-hour treatments.
Exhibited similar degradation patterns and Hook effect at higher concentrations in HEK293A cells.
Had ASK1 degradation blocked by proteasome inhibitor MG132 pretreatment, confirming proteasome dependence.
Showed no detectable cytotoxicity across the 1 nM to 10 μM concentration range after 24 hours.
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Cell Line:HepG2 cells
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Concentration:10 nM, 50 nM, 100 nM, 200 nM (dASK1); 5 μM (MG132 pre-incubation)
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Incubation Time:8 h (dASK1); 30 min (MG132 pre-incubation)
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Result:Reduced ASK1 protein levels compared to the untreated control.
Blocked the dASK1-mediated reduction of ASK1 protein, with ASK1 levels returning to near-control levels when cells were pre-treated with MG132.
Chemical Information
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CAS No. 3064086-31-0
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Masse moléculaire 800.77
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
dASK1 Related Classifications
HY-174862 Related Classifications
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