1-(2-Maleinimidylethyl)-4-(5-(4-methoxy-phenyl)-oxazol-2-yl)-pyridinium methansulfonat | 155862-97-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1-(2-Maleinimidylethyl)-4-(5-(4-methoxy-phenyl)-oxazol-2-yl)-pyridinium methansulfonat
• 英文别名: 1-(2-maleimidylethyl)-4-(5-(4-methoxyphenyl)oxazol-2-yl)pyridinium methanesulfonate；1-(2-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)ethyl)-4-(5-(4-methoxyphenyl)oxazol-2-yl)pyridin-1-ium methanesulfonate；methanesulfonate;1-[2-[4-[5-(4-methoxyphenyl)-1,3-oxazol-2-yl]pyridin-1-ium-1-yl]ethyl]pyrrole-2,5-dione
• CAS: 155862-97-8
• 化学式: CH₃O₃S*C₂₁H₁₈N₃O₄
• 分子量: 471.491
• InChiKey: WLUHMAZNVINQRC-UHFFFAOYSA-M

计算性质

• 辛醇/水分配系数(LogP)：
  1.39
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  142
• 氢给体数：
  0
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  adenylate kinase from Escherichia coli 、 1-(2-Maleinimidylethyl)-4-(5-(4-methoxy-phenyl)-oxazol-2-yl)-pyridinium methansulfonat 生成 adenylate kinase from Escherichia coli, labeled with PyMPO at surface cysteine Cys-77
  参考文献：
  名称：

  摘要：

  DOI：

文献信息

• Hydrophobically-modified protein compositions and methods
  申请人：Pepinsky Blake R.

  公开号：US20050119181A1

  公开（公告）日：2005-06-02

  Hydrophobically-modified proteins and methods of making them are described. A hydrophobic moiety is attached to a surface amino acid residue of the protein. The hydrophobic moiety can be a lipid or a peptide. Alternatively, the protein can be derivatized by a wide variety of chemical reactions that append a hydrophobic structure to the protein. The preferred protein is of mammalian origin and is selected from the group consisting of Sonic, Indian, and Desert hedgehog. The hydrophobic moiety is used as a convenient tether to which may be attached a vesicle such as a cell membrane, liposome, or micelle.

  描述了一种水疏性修饰蛋白质及其制备方法。将一种疏水基团附加到蛋白质的表面氨基酸残基上。该疏水基团可以是脂质或肽。或者，可以通过各种化学反应使蛋白质衍生出一个疏水结构。优选的蛋白质是哺乳动物来源的，并从Sonic，Indian和Desert hedgehog组中选择。该疏水基团可用作方便的系链，可附着细胞膜、脂质体或微胶束等载体。
• Methods and compositions for treating disorders involving excitotoxicity
  申请人：Galdes Alphonse

  公开号：US20080221037A1

  公开（公告）日：2008-09-11

  It is shown here that hedgehog polypeptides possess novel activities beyond phenotype specification. Using cultures derived from the embryonic day 14.5 (E14.5) rat ventral mesencephalon, we show that hedgehog is also trophic for dopaminergic neurons and other neurons which are sensitive to exotoxicity.

  这里显示出刺猬多肽具有超出表型规范的新颖活性。使用从胚胎第14.5天（E14.5）大鼠腹侧中脑衍生的培养基，我们展示了刺猬对多巴胺能神经元和其他对外毒性敏感的神经元也具有营养作用。
• Fluorescently or spin-labeled kinases for rapid screening and identification of novel kinase inhibitor scaffolds
  申请人：Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.

  公开号：EP2147979A1

  公开（公告）日：2010-01-27

  The present invention relates to a kinase labeled at an amino acid having a free thiol or amino group, wherein said amino acid is naturally present or introduced in the activation loop of said kinase, with (a) a thiol- or amino-reactive fluorophore sensitive to polarity changes in its environment; or (b) a thiol-reactive spin label, an isotope or an isotope-enriched thiol- or amino-reactive label, such that said fluorophore, spin label, isotope or isotope-enriched label does not inhibit the catalytic activity and does not interfere with the stability of the kinase. The invention furthermore relates to a method of screening for kinase inhibitor, a method of determining the kinetics of ligand binding and/or of dissociation of a kinase inhibitor and a method of generating mutated kinases suitable for the screening of kinase inhibitors using the kinase of the present invention.

  本发明涉及一种激酶，其标记在具有游离硫醇或氨基的氨基酸上，其中所述氨基酸天然存在或引入所述激酶的活化环中，具有(a)对其环境中极性变化敏感的硫醇或氨基反应荧光团；或 (b) 硫醇反应性自旋标签、同位素或同位素富集硫醇或氨基反应性标签，使得所述荧光团、自旋标签、同位素或同位素富集标签不抑制催化活性，也不干扰激酶的稳定性。本发明还涉及一种筛选激酶抑制剂的方法、一种确定配体结合动力学和/或激酶抑制剂解离动力学的方法，以及一种利用本发明的激酶生成适合筛选激酶抑制剂的突变激酶的方法。
• Development of fluorescently P-loop labeled kinases for screening of inhibitors
  申请人：Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.

  公开号：EP2241619A1

  公开（公告）日：2010-10-20

  The present invention relates to a kinase labeled at an amino acid naturally present or introduced in the P-loop of said kinase, wherein said labeling is effected at a free thiol or amino group of said amino acid and said label is (a) a thiol- or amino-reactive fluorophore sensitive to polarity changes in its environment; or (b) a thiol-reactive spin label, an isotope or an isotope-enriched thiol- or amino-reactive label, such that said fluorophore, spin label, isotope or isotope-enriched label does not inhibit the catalytic activity and does not interfere with the stability of the kinase. The invention furthermore relates to a method of screening for kinase inhibitors, a method of determining the kinetics of ligand binding and/or of dissociation of a kinase inhibitor and a method of generating mutated kinases suitable for the screening of kinase inhibitors using the kinase of the present invention.

  本发明涉及一种激酶，该激酶被标记在天然存在或被引入该激酶P环的氨基酸上，其中所述标记是在所述氨基酸的游离硫醇或氨基上实现的，所述标记是(a)对其环境中极性变化敏感的硫醇或氨基反应荧光团；或 (b) 硫醇反应性自旋标签、同位素或富含同位素的硫醇或氨基反应性标签，使得所述荧光团、自旋标签、同位素或富含同位素的标签不抑制激酶的催化活性，也不干扰激酶的稳定性。本发明还涉及一种筛选激酶抑制剂的方法、一种确定配体结合动力学和/或激酶抑制剂解离动力学的方法，以及一种利用本发明的激酶生成适合筛选激酶抑制剂的突变激酶的方法。
• Netrin-related compositions and uses
  申请人：University of Utah Research Foundation

  公开号：EP2359842A1

  公开（公告）日：2011-08-24

  The present invention relates to a polypeptide effective to promote angiogenesis for use in promoting angiogenesis, wherein said polypeptide is a netrin polypeptide.

  本发明涉及一种有效促进血管生成的多肽，用于促进血管生成，其中所述多肽是一种净蛋白多肽。