Bisindolylmaleimide XI (HCl)

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: Bisindolylmaleimide XI (HCl)
• 英文别名: 3-[8-[(dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl]-4-(1-methylindol-3-yl)pyrrole-2,5-dione
• 化学式: C₂₈H₂₈N₄O₂
• 分子量: 452.5
• InChiKey: MJZPKYUVFUQNEV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  34
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  59.3
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Regulation of cardiac contractility and heart failure propensity
  申请人：Children's Hospital Medical Center

  公开号：EP1908827A2

  公开（公告）日：2008-04-09

  The methods and compositions of the present invention find use in altering expression of PKCα in transgenic animals. The compositions of the invention include isolated transgenic animal cells, transgenic tissue, transgenic animals, and transgenic mice. The transgenic animals of the invention exhibit altered PKCα activity. The methods allow generation of transgenic animals with altered expression of PKCα. The invention allows modulation of cardiac contractility. In particular, the invention provides a method for altering the susceptibility of a transgenic animal to cardiomyopathy. A transgenic animal of the invention finds use in identifying anti-cardiomyopathic compounds.

  本发明的方法和组合物可用于改变转基因动物中 PKCα 的表达。本发明的组合物包括分离的转基因动物细胞、转基因组织、转基因动物和转基因小鼠。本发明的转基因动物表现出改变的 PKCα 活性。本发明的方法可以产生 PKCα 表达改变的转基因动物。本发明可调节心脏收缩力。特别是，本发明提供了一种改变转基因动物对心肌病易感性的方法。本发明的转基因动物可用于鉴定抗心肌病化合物。
• Use of Protein Kinase C Delta (PKCD) Inhibitors to Treat Diabetes, Obesity and, Hepatic Steatosis
  申请人：Joslin Diabetes Center, Inc.

  公开号：EP2942060A1

  公开（公告）日：2015-11-11

  Described are methods of improving insulin sensitivity, and treating fatty liver disease (including non-alcoholic steatohepatitis (NASH)), by administering specific inhibitors of PKC delta.

  描述了通过施用特定的 PKC delta 抑制剂来改善胰岛素敏感性和治疗脂肪肝（包括非酒精性脂肪性肝炎（NASH））的方法。
• MEDIUM FOR CULTURING STEM CELLS, METHOD FOR CULTURING STEM CELLS, STEM CELL GROWTH PROMOTER, AND CELL COMPOSITION AND METHOD FOR PRODUCING SAME
  申请人：Kyowa Hakko Bio Co., Ltd.

  公开号：EP3511410A1

  公开（公告）日：2019-07-17

  An object of the present invention is to provide a technique for stably, inexpensively, and safely culturing stem cells having a differentiation ability while maintaining an undifferentiated state. The present invention relates to a medium for culturing stem cells, comprising at least one or more compounds selected from the group consisting of a ROCK inhibitor, a PKC inhibitor, a histone methyltransferase inhibitor, and a retinoic acid receptor agonist, and not containing a growth factor or having a low growth factor concentration; a method for culturing stem cells using the medium; a growth promoter for stem cell; as well as a cell composition containing stem cells or differentiated cells therefrom; and a method for producing the cell composition.

  本发明的目的是提供一种技术，稳定、廉价、安全地培养具有分化能力的干细胞，同时保持未分化状态。本发明涉及一种培养干细胞的培养基，该培养基包含至少一种或多种选自 ROCK 抑制剂、PKC 抑制剂、组蛋白甲基转移酶抑制剂和维甲酸受体激动剂的化合物，且不含生长因子或生长因子浓度较低；一种使用该培养基培养干细胞的方法；一种干细胞生长促进剂；以及一种含有干细胞或从中分化的细胞的细胞组合物；以及一种生产该细胞组合物的方法。
• Cancer treatment with compounds inhibiting PKC alpha
  申请人：Lu Zhimin

  公开号：US20060009492A1

  公开（公告）日：2006-01-12

  A chemotherapeutic cancer treatment with Gö7874, Gö6850, Gö7612, Gö7852, Ro31-7549, Ro31-8425, Ro31-8220, Ro31-0432 and NGIC-1 or chemical compounds with similar structures is administered to a mammal for the treatment of the cancer. The chemical compound is targeted to PKC α activity. Experiments indicate that Gö7874, Gö6850, Gö7612, Gö7852, Ro31-7549, Ro31-8425, Ro31-8220, Ro31-0432 and NGIC-1 and similar compounds to be effective for the treatment of breast cancer, leukemia, lung cancer, skin cancer, prostate cancer, liver cancer, brain tumor, cervical cancer, and cancers located in the digestive tract including gastric cancer and colorectal cancers. These treatments may be accomplished utilizing Gö7874, Gö6850, Gö7612, Gö7852, Ro31-7549, Ro31-8425, Ro31-8220, Ro31-0432 and NGIC-1 and chemical compounds with similar structures alone or in combination with prior art chemotherapy agents or with radiation therapy. In a preferred embodiment Gö7874, Gö6850, Gö7612, Gö7852, Ro31-7549, Ro31-8425, Ro31-8220, Ro31-0432 and NGIC-1 chemical compounds with similar structures is used for the treatment of cancer as a preventative drug by preventing cancer cell formation.

  向哺乳动物施用 Gö7874、Gö6850、Gö7612、Gö7852、Ro31-7549、Ro31-8425、Ro31-8220、Ro31-0432 和 NGIC-1 或具有类似结构的化合物进行癌症化疗，以治疗癌症。该化合物针对 PKC α 的活性。实验表明，Gö7874、Gö6850、Gö7612、Gö7852、Ro31-7549、Ro31-8425、Ro31-8220、Ro31-0432 和 NGIC-1 及类似化合物可有效治疗乳腺癌、白血病、肺癌、皮肤癌、前列腺癌、肝癌、脑瘤、宫颈癌和消化道癌症，包括胃癌和结肠直肠癌。这些治疗可以利用 Gö7874、Gö6850、Gö7612、Gö7852、Ro31-7549、Ro31-8425、Ro31-8220、Ro31-0432 和 NGIC-1 以及具有类似结构的化合物，单独使用或与现有技术的化疗药物或放射治疗联合使用。在一个优选的实施方案中，Gö7874、Gö6850、Gö7612、Gö7852、Ro31-7549、Ro31-8425、Ro31-8220、Ro31-0432 和具有类似结构的 NGIC-1 化合物通过阻止癌细胞的形成，作为预防药物用于癌症的治疗。
• REGULATION OF CARDIAC CONTRACTILITY AND HEART FAILURE PROPENSITY
  申请人：Children's Hospital Medical Center

  公开号：EP1664294A2

  公开（公告）日：2006-06-07