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| 化学名: | エンザスタウリン | | 英語化学名: | Enzastaurin (LY317615) | | 别名: | 1H-Pyrrole-2,5-dione, 3-(1-methyl-1H-indol-3-yl)-4-(1-(1-(2-pyridinylmethyl)-4-piperidinyl)-1H-indol-3-yl)-;Unii-uc96G28eqf;Enzastaurin,Enzstataurin,LY317615,170364-57-5,1H-Pyrrole-2,5-dione, 3-;3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(2-pyridinylmethyl)-4-piperidinyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione;Enzastaurin ( LY317615 );Enzastaurine;LY317615 (Enzastaurin);LY317615/Enzstataurin | | CAS番号: | 170364-57-5 | | 分子式: | C32H29N5O2 | | 分子量: | 515.6 | | EINECS: | | | カテゴリ情報: | Inhibitors;Smad;TGF-beta;TGF-beta/Smad;Intermediates & Fine Chemicals;Pharmaceuticals | | Mol File: | 170364-57-5.mol |  |
| 融点 | 249-261℃ | | 沸点 | 767.2±60.0 °C(Predicted) | | 比重(密度) | 1.34 | | RTECS 番号 | UX9626850 | | 闪点 | 417.8℃ | | 貯蔵温度 | -20°C | | 溶解性 | DMSO: soluble10mg/mL, clear (warmed) | | 外見 | powder | | 酸解離定数(Pka) | 7.88±0.60(Predicted) | | 色 | , light orange to dark orange-red | | 安定性： | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| 主な危険性 | Xn | | Rフレーズ | 22 | | WGK Germany | 3 | | HSコード | 29339900 |
| | エンザスタウリン Usage And Synthesis |
| 説明 | Enzastaurin (170364-57-5) is a potent and selective PKCβ inhibitor.? IC50 = 6, 39, 83 and 110 nM, for PKCβ, PKCα, PKCγ and PKCε respectively.1 Induces apoptosis in multiple myeloma cell lines via inhibition of the AKT signaling pathway.2 Induces mitotic missegregation and preferential cytotoxicity in colorectal cancer cells with chromosomal instability.3 Attenuates amphetamine-stimulated dopamine efflux.4 Inhibits blood-brain barrier leakiness in a mouse model.5 | | 使用 | PKCβ-selective inhibitor, suppresses angiogenesis. | | 使用 | Enzastaurin has been used in splicing analysis to study its effects on splicing of a mutated exon. | | 定義 | ChEBI: 3-(1-methyl-3-indolyl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-3-indolyl]pyrrole-2,5-dione is a member of indoles and a member of maleimides. | | Biochem/physiol Actions | Enzastaurin is a potent and PKCβ preferring inhibitor. Also, Enzastaurin inhibits AKT and GSK3β. Enzastaurin acts as anti-angiogenic and antineoplastic agent. | | 参考文献 | 1) Graff et al. (2005), The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts; Cancer Res. 65 7462
2) Rizvi et al. (2006) Enzastaurin (LY317615), a protein kinase Cβ inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines; Mol.Cancer Ther. 5 1783
3) Ouaret and Larsen (2014), Protein kinase Cβ inhibition by enzastaurin leads to mitotic missegregation and preferential cytotoxicity toward colorectal cancer cells with chromosomal instability (CIN); Cell Cycle 13 2697
4) Zestos et al. (2016), PKCβ Inhibitors Attenuate Amphetamine-Stimulated Dopamine Efflux; ACS Chem.Neurosci. 7 757
5) Stranahan et al. (2016), Blood-brain barrier breakdown promotes macrophage infiltration and cognitive impairment in leptin receptor-deficient mice; J.Cereb.Blood Flow Metab. 36 2108 |
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