PKR Inhibitor | 1159885-47-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻唑类
• 英文名称: PKR Inhibitor
• 英文别名: (8Z)-8-(1H-imidazol-5-ylmethylidene)-6H-pyrrolo[2,3-g][1,3]benzothiazol-7-one
• CAS: 1159885-47-8；608512-97-6
• 化学式: C₁₃H₈N₄OS
• 分子量: 268.3
• InChiKey: VFBGXTUGODTSPK-BAQGIRSFSA-N

物化性质

• 沸点：
  674.6±55.0 °C(Predicted)
• 密度：
  1.604±0.06 g/cm3(Predicted)
• 溶解度：
  DMSO：可溶，12mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  19
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  98.9
• 氢给体数：
  2
• 氢受体数：
  4

制备方法与用途

生物活性
PKR-IN-C16（C16，Imidazolo-oxindole PKR抑制剂）是一种针对RNA依赖性蛋白激酶（PKR、Protein Kinase R、EIF2AK2）的特异性抑制剂。研究显示，在具有神经炎症成分的急性兴奋性毒性大鼠模型中，PKR-IN-C16能够阻止凋亡和IL-1β的产生。

靶点

Target	Value
PKR
IL-1β

文献信息

• Method for cellular RNA expression
  申请人：TRON TRANSLATIONALE ONKOLOGIE AN DER UNIVERSITATSMEDIZIN DER JOHANNES GUTENBE

  公开号：US10207009B2

  公开（公告）日：2019-02-19

  The present invention relates to expressing RNA in cells and, in particular, enhancing viability of cells in which RNA is to be expressed. Specifically, the present invention provides methods for expressing RNA in cells comprising the steps of preventing engagement of IFN receptor by extracellular IFN and inhibiting intracellular IFN signalling in the cells. Thus, preventing engagement of IFN receptor by extracellular IFN and inhibiting intracellular IFN signalling in the cells allows repetitive transfer of RNA into the cells.

  本发明涉及在细胞中表达 RNA，特别是提高要表达 RNA 的细胞的活力。具体地说，本发明提供了在细胞中表达 RNA 的方法，包括以下步骤：防止细胞外 IFN 受体与细胞内 IFN 信号结合。因此，防止细胞外 IFN 受体与细胞内 IFN 信号的接合和抑制细胞内 IFN 信号的传递可使 RNA 重复转移到细胞内。
• Composition for prevention or treatment of bronchial asthma comprising PKR inhibitor as active ingredient
  申请人：INDUSTRIAL COOPERATION FOUNDATION CHONBUK NATIONAL UNIVERSITY

  公开号：US10292969B2

  公开（公告）日：2019-05-21

  The present invention relates to a composition for prevention or treatment of bronchial asthma comprising a PKR inhibitor as an active ingredient. The PKR inhibitor and derivatives thereof according to the present invention can be used as a pharmaceutical for prevention, amelioration or treatment of bronchial asthma and as a supplementary health food because the PKR inhibitor and derivatives thereof reduce the total counts of inflammatory cells, eosinophils, neutrophils and lymphocytes in bronchoalveolar lavage fluid of neutrophilic severe asthma-induced mice, reduce airway inflammation and airway hyper-responsiveness, and reduce inflammatory mediators.

  本发明涉及一种用于预防或治疗支气管哮喘的组合物，其活性成分包括 PKR 抑制剂。根据本发明的 PKR 抑制剂及其衍生物可用作预防、改善或治疗支气管哮喘的药物和辅助保健食品，因为 PKR 抑制剂及其衍生物可减少中性粒细胞严重哮喘诱导小鼠支气管肺泡灌洗液中的炎症细胞、嗜酸性粒细胞、中性粒细胞和淋巴细胞的总计数，减少气道炎症和气道高反应性，并减少炎症介质。
• Methods and compositions for restoring homeostatic capacity of a subject
  申请人：Palo Alto Investors

  公开号：US10835134B2

  公开（公告）日：2020-11-17

  Methods of restoring homeostatic capacity of a subject are provided. Aspects of the invention further include compositions, systems and devices for practicing the methods. The methods and compositions described herein find use in a variety of applications. Aspects of certain embodiments of the methods include modulating a subject's autonomic nervous system in a manner sufficient to restore the homeostatic capacity of the subject. Aspects of other embodiments of the invention include administering to the subject an amount of an apoptosis modulator effective to at least partially restore homeostatic function of the neuroendocrine system of the subject.

  本发明提供了恢复受试者体内平衡能力的方法。本发明的各个方面还包括用于实施这些方法的组合物、系统和设备。本文所述的方法和组合物可用于多种应用。本发明方法的某些实施方案包括以足以恢复受试者平衡能力的方式调节受试者的自律神经系统。本发明其他实施方案的方面包括向受试者施用一定量的细胞凋亡调节剂，其有效量至少可部分恢复受试者神经内分泌系统的平衡功能。
• Methods for treating renal disease
  申请人：Beth Israel Deaconess Medical Center, Inc.

  公开号：US10940151B2

  公开（公告）日：2021-03-09

  The invention features methods for treating or reducing the likelihood of developing a renal disease by administering to a subject in need thereof an agent that decreases expression of a pathogenic APOL1. The agents of the method target various signaling pathways and decrease the level of the pathogenic APOL1 polypeptide.

  本发明的特点是通过向有需要的受试者施用能降低致病性 APOL1 表达的制剂来治疗或降低罹患肾病可能性的方法。该方法的制剂以各种信号通路为靶点，降低致病 APOL1 多肽的水平。
• EP2646557B1
  申请人：——

  公开号：EP2646557B1

  公开（公告）日：2017-08-09