1. PROTAC Apoptosis
  2. PROTACs ASK1
  3. dASK1

dASK1 是一种选择性的基于 CRBN 的凋亡信号调节激酶 1 (ASK1) 的 PROTAC 靶向降解剂。dASK1 能够与 ASK1 形成稳定的三元复合物,通过泛素-蛋白酶体途径促进 ASK1 快速且持续的降解。dASK1 表现出强大的 ASK1 降解能力。dASK1 可用于肝炎的研究。(结构:粉色:ASK1 配体 (HY-174860);蓝色:E3 连接酶配体 (HY-10984);黑色:连接子;E3 配体-连接子偶联物 (HY-174863))

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dASK1 Chemical Structure

dASK1 Chemical Structure

CAS No. : 3064086-31-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1]. (Structure Note: Pink: ASK1 ligand (HY-174860); Blue: E3 ligase ligand (HY-10984); Black: linker; E3-linker (HY-174863))

体外研究
(In Vitro)

dASK1 (Compound 35) (1-5000 nM, 4-12 h) 可诱导 HepG2 和 HEK293A 细胞中 ASK1 的降解[1]

dASK1 (1 nM to 10 μM, 24 h) 在 HepG2 细胞中未显示出可检测的毒性[1]

dASK1 (10-200 nM, 8 h) 在 HepG2 细胞中降解 ASK1 的作用显示出蛋白酶体依赖性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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.

Western Blot Analysis[1]

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 Cytotoxicity Assay[1]

Cell Line: HepG2 cells
Concentration: 1, 10, 50, 100, 500, 1000, and 10000 nM
Incubation Time: 24 h
Result: Showed no detectable toxicity.

Western Blot Analysis[1]

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: MG132 (HY-13259) blocked degradation and led to ASK1 accumulation.
分子量

800.77

Formula

C38H38F2N10O8

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
dASK1
目录号:
HY-174862
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