dASK1-VHL
dASK1-VHL is an ASK1 PROTAC degrader that recruits VHL. dASK1-VHL induces ubiquitination and proteasomal degradation of ASK1 by forming a ternary complex, and inhibits the downstream p38 MAPK signaling pathway. dASK1-VHL can be used in studies of metabolic dysfunction-associated steatohepatitis.
(Pink: ASK1 ligand (HY-174860); Blue: VHL ligand (HY-125845); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C48H57F2N11O8S
- 分子量:986.10
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
体外実験
dASK1-VHL (compound 60) (1 nM-10 μM; 8 h) is a potent VHL-dependent PROTAC that induces dose-dependent degradation of ASK1 in HepG2 cells[1].
dASK1-VHL (1 nM-10 μM) shows no cytotoxicity in the tested cell lines over the concentration range of 1 nM to 10000 nM[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, 100, 500, 1000, 10000 nM
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Incubation Time:8 h
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Result:Dose-dependently degraded ASK1, achieving maximum degradation (~60% reduction) at 50 nM.
Showed reduced efficacy at concentrations ≥ 100 nM, consistent with the Hook effect.
Had its ASK1 degradation completely abrogated by pretreatment with VH032, confirming VHL-dependent action.
Exhibited no detectable cytotoxicity across a wide concentration range (1 nM to 10 μM).
Parmacokinetics
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 6-8 weeks old, MCD diet-induced MASH)[1]
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Dosage:2 mg/kg
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Administration:i.p.; once daily; 14 days
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Result:Reduced hepatic ASK1 protein levels.
Decreased phosphorylation of p38 MAPK.
Reduced ASK1 ubiquitination in liver tissue.
Decreased hepatic lipid accumulation.
Left ASK1 mRNA expression unchanged relative to controls.
Did not alter protein levels of TAK1.
化学情報
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分子量 986.10
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
dASK1-VHL 関連分類
HY-174858 関連分類
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