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

dASK1-VHL 是一种有口服活性的靶向 ASK1PROTAC 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)。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

dASK1-VHL Chemical Structure

dASK1-VHL Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

查看 PROTACs 亚型特异性产品:

查看 p38 MAPK 亚型特异性产品:

  • 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.

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
  • 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 *
= × ×

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.

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
dASK1-VHL
目录号:
HY-174858
需求量: