1. 一站式药筛
  2. 化合物库
  3. 蛋白降解靶向嵌合体连接子
蛋白降解靶向嵌合体连接子 - PROTAC Linker

Cat. No.: HY-L929

蛋白水解靶向嵌合体(PROTACs)是依托泛素-蛋白酶体系统的新型治疗策略,区别于传统小分子的结合位点占有模式,通过降解特定蛋白消除其功能,且不受靶向蛋白结合囊袋限制,适用范围更广。

PROTACs为异功能分子,核心组成包括靶蛋白结合配体(弹头)、E3连接酶招募配体及连接二者的PROTAC连接子,其中连接子是共价连接双配体的功能性分子链,通过连接靶蛋白结合配体与 E3 泛素连接酶结合配体以及构象调控促进三元复合物的形成,同时优化PROTACs理化性质以提升成药性,并降低脱靶风险。其设计需遵循长度匹配、柔性平衡等原则,可通过微小的结构变化影响PROTACs降解效率,连接子优化是PROTACs从研发走向临床、推动靶向蛋白降解技术产业化的关键环节。

MCE收集整理了1158个可应用的PROTAC Linker,涉及到柔性、刚性和半刚性等多种类型,其中柔性连接子(如 PEG 链、烷基链)构象灵活,适配性强;刚性连接子(如芳环、三唑环)多适用于具有明确晶体结构,能精准靶向的已知靶点;半刚性连接子兼顾灵活与精准,常用于优化PROTACs的理化性质以提升药物活性、改善降解效率,该化合物库可广泛应用于PROTACs 的研发中。

  • 96-well Plate with Peelable Foil Seal
  • 384-well Microplate with Peelable Foil Seal
  • 96-well Storage Tubes with Rack
- +

Compound Screening Libraries

Top Publications Citing Use of MCE Products

MCE 顾客使用化合物库产品发表的文献

  • 生物活性
  • 产品详情

活性描述 & 特点

Biological Activity

•    A unique collection of 1,158 compounds can be used for connecting target protein-binding ligands and E3 ubiquitin ligase-binding ligands.

•    It is obtained by AI screening based on 2D/3D similarity and can be used for optimizing the physicochemical properties of PROTACs and advancing drug development.

•    All compounds are available off the shelf.

•    All compounds are validated by LC-MS or NMR to ensure high purity and quality.

产品详情

Product Details

Formulation:

A compound library can be used for connecting target protein-binding ligands and E3 ubiquitin ligase-binding ligands.

Layout:

96-well storage tube or 96-well plate: 1st and 12th column are left empty.
384-well plate: the first two columns and the last two columns are left empty.
Compounds with different concentrations or dissolved in different solvents will be put on separate plates. This way of layout may increase the number of plates because there could be three solvents and three concentrations.
If you have other requirements, please let us know.

Container:

96- or 384-well Plate with Peelable Foil Seal; 96-well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode.

Storage:

-80°C

Shipping:

Blue ice or dry ice

相关服务推荐
定制您专属的化合物库
  •  特定化合物
  •  化合物数量
  •  产品排布图
  •  浓度
  •  形式(固体或溶液)
  •  YES
联系专家定制
  • 96-well Plate with Peelable Foil Seal
  • 384-well Microplate with Peelable Foil Seal
  • 96-well Storage Tubes with Rack

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:

* Container:

       留言给我们:

    Bulk Inquiry

    Inquiry Information

    产品名称:
    PROTAC Linker
    目录号:
    HY-L929
    需求量: