1. 一站式药筛
  2. 化合物库
  3. 靶向赖氨酸的共价片段库
靶向赖氨酸的共价片段库 - Lysine Focused Covalent Fragment Library

Cat. No.: HY-L915

赖氨酸是设计靶向共价抑制剂(TCIs)及相关配体的第二常见氨基酸,其在人体蛋白中的丰度是半胱氨酸的三倍(5.8% 对 1.9%),这显著增加了可进行共价靶向的蛋白质数量,尤其考虑到许多蛋白缺乏可结合的半胱氨酸残基。此外,有研究表明,功能性氨基酸被突变替换的概率较低。赖氨酸通常在催化过程中扮演重要角色,充当碱或亲核试剂,并且对维持蛋白质的结构完整性及调控蛋白翻译后修饰(PTMs)至关重要。近年来针对赖氨酸的研究备受关注。

我们基于最新的研究收集了上百种不同类型的共价抑制剂。经过谨慎选择,构建了一组含有110多种亲电基团的结构过滤器。通过对结构过滤器选择的亲电性片段进行分析,去除任何具有琐碎或不需要的结构特征的分子。最终获得 445 个具有靶向赖氨酸共价修饰潜力的片段分子,用于基于片段的共价药物发现。

  • 96-well Plate with Peelable Foil Seal
  • 384-well Microplate with Peelable Foil Seal
  • 96-well Storage Tubes with Rack
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  • 生物活性
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活性描述 & 特点

Biological Activity

•   A unique collection of 445 fragments that show covalent binding with lysine.

•    Careful selection of warheads: only those with experimentally validated reactivity are chosen, avoiding over-reactive warheads and any alternative reactive functionalities.

•   A useful tool for the fragment-based approach to drug discovery (FBDD).

•   All compounds are available off the shelf.

•   LCMS or NMR validated to ensure high purity and quality.

产品详情

Product Details

Formulation:

This fragment library containing 445 fragments with warheads targeting lysine residue.

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

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

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    产品名称:
    Lysine Focused Covalent Fragment Library
    目录号:
    HY-L915
    需求量: