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).
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。
- CAS 番号: 3064086-31-0
- 分子式: C38H38F2N10O8
- 分子量:800.77
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
PROTACs アイソフォーム固有の製品をすべて表示
More
生物活性
|
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.
-
Cell Line:HepG2 cells
-
Concentration:1, 10, 50, 100, 500, and 1000 nM
-
Incubation Time:4, 8, and 12 h
-
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.
-
Cell Line:HEK293A cells
-
Concentration:1, 10, 50, 100, 500, 1000, and 5000 nM
-
Incubation Time:8 h
-
Result:Demonstrated the highest degradation efficacy at 10 nM.
-
Cell Line:HepG2 cells
-
Concentration:1, 10, 50, 100, 500, 1000, and 10000 nM
-
Incubation Time:24 h
-
Result:Showed no detectable toxicity.
-
Cell Line:HepG2 cells
-
Concentration:10, 50, 100, and 200 nM; 10 and 50 nM (pre-treating with 5 µM of MG132 (HY-13259) for 30 min)
-
Incubation Time:8 h
-
Result:Degraded ASK1 levels.
MG132 (HY-13259) blocked degradation and led to ASK1 accumulation.
化学情報
-
CAS 番号 3064086-31-0
-
分子量 800.77
-
分子式 C38H38F2N10O8
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
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)