1. 一站式药筛
  2. 化合物库
  3. 生物活性化合物库系列
  4. 根据产品结构分类
  5. 半胱氨酸靶向共价片段库
半胱氨酸靶向共价片段库 - Cysteine Targeted Covalent Fragment Library

Cat. No.: HY-L154

共价抑制剂是一种可以通过共价键特异性结合靶蛋白并抑制其生物学功能的小分子。虽然长期以来,共价靶向在药物发现中一直处于次要地位,但随着越来越多关于此类药物成功用于临床的报道,共价药物正逐渐得到认可。目前,半胱氨酸是多种共价药物中最常见的共价氨基酸残基,各种能与半胱氨酸发生反应的弹头正在被开发出来,为共价药物开发提供了关键的砌块结构。

为了满足针对半胱氨酸的共价抑制剂的开发需求,MCE收录了3148种包含不同靶向半氨酸共价弹头的片段化合物。MCE半胱氨酸靶向共价片段库主要使用以下共价弹头设计而成:Acrylamides、Propiolic acid ester、 Dimethylamine functionalized acrylamides、 Chloroacetamides、 Acrylonitrile、2-Cyanoacrylamide、 Aziridine, Haloacetamide等。所有化合物均符合RO3 原则,可以用于基于片段的共价药物设计

我们将在明确您的产品用途后,向符合资质的客户通过定制合成服务的方式提供 MCE 半胱氨酸靶向共价片段库,我们为该库中的所有产品提供溶液包装或粉末包装。溶液包装中,3131 个产品以 10 mM 浓度提供,1 个产品以 2 mM 浓度提供。

溶液包装中,我们对于溶液状态稳定且溶解度不低于 10 mM 的产品,提供 10 mM 溶液;对于溶液状态稳定且溶解度介于 2~10 mM 的产品,我们提供 2 mM 溶液。

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

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MCE 顾客使用化合物库产品发表的文献

  • 生物活性
  • 产品详情
  • 产品资料
  • 化合物库组成

活性描述 & 特点

Biological Activity

•   A unique collection of 3148 fragments with different covalent warheads that target cysteine.

•    Contains various covalent warheads targeting cysteine residue.

•   Compounds were pre-filtered with the Rule of Three restrictions: MW 100-300 Da, H-donors ≤3, H-acceptors ≤3 and cLogP ≤3.

•   A useful tool for development covalent drugs.

•   Validated NMR and HPLC to ensure high purity and quality.

•   All compounds are in stock and continuously updated.

产品详情

Product Details

Formulation:

A collection of 3148 fragments with various warheads targeting cysteine residue supplied as pre-dissolved Solutions or Solid.
Solution: 3131 compounds supplied in 10 mM solution, 1 compounds supplied in 2 mM solution.

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

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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:
    Cysteine Targeted Covalent Fragment Library
    目录号:
    HY-L154
    需求量: