dASK1-VHL
dASK1-VHL is an orally active PROTAC degrader targeting ASK1. dASK1-VHL can effectively bind VHL and promote the selective degradation of ASK1. dASK1-VHL effectively reduces ASK1 protein levels, inhibits the activation of p38 MAPK, and reduces liver lipid content. dASK1-VHL provides new ideas for the study of Metabolic dysfunction-associated steatohepatitis (MASH).
(Pink: ASK1 ligand (HY-174860); Blue: VHL ligand (HY-125845); Black: linker).
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- 화학식: C48H57F2N11O8S
- 분자량:986.10
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
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Biological Activity
dASK1-VHL (Compound dASK1-VHL) (1-1000 nM, 8 h) mediates efficient and specific ASK1 degradation via VHL E3 ligase 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 nM, 10 nM, 50 nM, 100 nM, 500 nM, 1000 nM
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Incubation Time:8 h
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Result:Achieved a 60 % degradation rate of ASK1 protein (at a concentration of 50 nM).
Was specific for VHL-mediated degradation, and pretreatment with VHL ligand VH032 completely abolished ASK1 degradation.
| Species | Dose | Route | AUC0-inf | Cmax |
|---|---|---|---|---|
| Mice | 2 mg/kg | i.v. | 2719.67 ng·h/mL | / |
| Mice | 20 mg/kg | p.o. | 12913.87 ng·h/mL | 9429.3 ng/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57/Bl6 nude mice fed the MCD diet (4-6 weeks)[1]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection (i.p.), once daily for 14 days
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Result:Significantly reduced liver ASK1 protein and decreased p-p38 levels.
Caused no change in ASK1 mRNA and reduced ASK1 ubiquitination levels.
Reduced liver lipid accumulation.
Chemical Information
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분자량 986.10
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화학식 C48H57F2N11O8S
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SMILES
O=C(NC1=NC(C2=NN=CN2C(C)C)=CC=C1)C3=CC(NC(CCC(NCCOCCC(N[C@H](C(N4[C@@H](C[C@H](C4)O)C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)=O)C(C)(C)C)=O)=O)=O)=C(F)C=C3F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
dASK1-VHL Related Classifications
HY-174858 Related Classifications
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