2. PROTAC Apoptosis MAPK/ERK Pathway
  3. PROTACs ASK1 p38 MAPK
  4. dASK1-VHL

dASK1-VHL 是一种有口服活性的靶向 ASK1 的 PROTAC 降解剂。dASK1-VHL 能有效结合 VHL 并促进 ASK1 选择性降解。dASK1-VHL 有效降低 ASK1 蛋白水平，抑制了 p38 MAPK 的激活，并减少了肝脏脂质含量。dASK1-VHL 为 MASH 的研究提供新思路 (粉色: ASK1 ligand 1 (HY-174860); 蓝色: E3 ligand (S,R,S)-AHPC (HY-125845); 黑色: Linker, (S,R,S)-AHPC-CO-C2-PEG-NHCO-C2-COOH (HY-174861)。

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dASK1-VHL Chemical Structure

dASK1-VHL Chemical Structure

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dASK1-VHL 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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 1 (HY-174860); Blue: E3 ligand (S,R,S)-AHPC (HY-125845); Black: Linker, (S,R,S)-AHPC-CO-C2-PEG-NHCO-C2-COOH (HY-174861)[1].

体外研究
(In Vitro)

dASK1-VHL (Compound dASK1-VHL) (1-1000 nM, 8 h) 在HepG2 细胞中通过 VHL E3 连接酶介导高效、特异的 ASK1 降解[1]。

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

dASK1-VHL 相关抗体:

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 1 nM, 10 nM, 50 nM, 100 nM, 500 nM, 1000 nM
Incubation Time: 8 h
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.
体内研究
(In Vivo)

dASK1-VHL (Compound dASK1-VHL) (2 mg/kg, i.p, 每日一次持续14天) 通过泛素-蛋白酶体途径降解 ASK1，显著改善 C57/Bl6 小鼠中 MASH 病理特征[1]。

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

Animal Model: Male C57/Bl6 nude mice fed the MCD diet (4-6 weeks)[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 14 days
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.
分子量

986.10

Formula

C48H57F2N11O8S
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

dASK1-VHL 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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.

Keywords:

dASK1-VHLPROTACsASK1p38 MAPKApoptosis signal-regulating kinase 1MAP3K5MAPKKK5Mitogen-activated protein kinase kinase kinase 5MEK kinase 5HepG2 cellsC57BL/6MASHInhibitorinhibitorinhibit

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