1. Screening Libraries
  2. Oxygen Sensing Compound Library

氧感应化合物库 - Oxygen Sensing Compound Library

Cat. No.: HY-L045
Library Contents: XLSX PDF SDF

氧稳态调节是细胞中调节生理氧变化最基本的进程,氧稳态失调会导致包括癌症在内的各种疾病的发生。缺氧与癌症的发生发展密切相关,缺氧/氧感应信号通路在调控癌症进展中发挥重要作用。

缺氧诱导因子(HIF-1)作为一种转录因子,是主要的氧稳态调控因子。已经发现多种 HIF-1 靶基因,这些靶基因编码的蛋白在关键的发育和生理过程中发挥重要作用,包括血管生成及血管重塑、红细胞生成、葡萄糖转运、糖酵解、铁转运和细胞增殖与存活等。

HIF-1 是一种异源二聚体转录因子,由在细胞内稳定表达的 β 亚基及受氧调控的 α 亚基构成。HIF-1 的独特特征是通过细胞内的 O2浓度调节 HIF-1α 的表达及活性来实现的。当细胞处于正常氧浓度下,HIF-1α 在细胞内与脯氨酸羟化酶作用,发生脯氨酸羟化。羟化后的 HIF-1α 可以被泛素化酶von Hippel-Lindau(VHL)识别,从而被泛素化降解,细胞中几乎检测不到 HIF-1α 的存在。羟化本质上是氧化,脯氨酸羟化酶需要氧气作为底物,当缺乏氧气时,脯氨酸羟化酶就无法发挥作用,导致 HIF-1α 泛素化无法进行。同样,如果细胞中 VHL 失活,即使在高氧浓度下 HIF-1α 也无法被泛素化降解,结果是这种蛋白在细胞内积聚。积聚的 HIF-1α 与另一种 HIF 分子 ARNT(HIF-1β)结合,从而形成能够启动转录活性的 HIF 复合物。在细胞核中,HIF-1复合物与缺氧反应基因启动子区域上的缺氧反应原件 HRE 结合,募集其他转录因子,进而引发组织细胞的一系列缺氧适应反应。

MCE 提供 1415 种氧感应相关的化合物,这些化合物主要靶向 HIF/HIF Prolyl-Hydroxylase,MAPK/ERK,PI3K/AKT 等信号通路中的相关靶点,是研究缺氧,氧化应激及开发新的抗肿瘤药物的有用工具。

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 氧感应化合物库,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,1382 个产品以 10 mM 浓度提供,30 个产品以 2 mM 浓度提供,3 个产品以 3 mg/mL 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;对于溶液状态稳定、分子量不确定且溶解度不低于 3 mg/mL产品,我们提供 3 mg/mL 溶液。

  • 96-well Plate with Peelable Foil Seal
  • 384-well Microplate with Peelable Foil Seal
  • 96-well Storage Tubes with Rack
Size (Pre-dissolved Solution or Solid) Price Stock
30 μL/well Solution

10 mM , 2 mM and 3 mg/mL
Pre-dissolved Solution

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50 μL/well Solution

10 mM , 2 mM and 3 mg/mL
Pre-dissolved Solution

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100 μL/well Solution

10 mM , 2 mM and 3 mg/mL
Pre-dissolved Solution

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2 × 100 μL/well Solution

10 mM , 2 mM and 3 mg/mL
Pre-dissolved Solution

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Description
& Advantages

•   A unique collection of 1415 oxygen sensing related compounds for high throughput screening (HTS) and high content screening (HCS).

•   Targets such as HIF, HIF Prolyl-Hydroxylase, E1/E2/E3 Enzyme, ROS, PI3K, MAPK, etc.

•   Bioactivity and safety confirmed by preclinical research and clinical trials, some compounds have been approved by FDA.

•   A useful tool to study hypoxia, oxidative stress.

•   More detailed compound information with structure, IC50, and other chemical & biological data.

•   NMR and HPLC validated ensure high purity.

•   All compounds are in stock and continuously updated.

Product Details
Formulation:
A collection of 1415 oxygen sensing compounds supplied as pre-dissolved Solutions or Solid
Solution: 1382 compounds supplied in 10 mM solution, 30 compounds supplied in 2 mM solution, 3 compounds supplied in 3 mg/mL solution.
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
Composition

Oxygen Sensing Compound Library

Source: MedChem Express

Documentation

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