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| | 4-(3-ピリジン-2-イル-1H-ピラゾール-4-イル)キノリン 製品概要 |
| 化学名: | 4-(3-ピリジン-2-イル-1H-ピラゾール-4-イル)キノリン | | 英語化学名: | LY-364947 | | 别名: | LY 364947 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline;LY-364947, 396129-53-6;Transforming Growth Factor-β Type I Receptor Kinase Inhibitor;LY-364947;LY-364947, >=98%;LY364947;HTS466284; LY-364947;TGF-β RI Kinase Inhibitor;[3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole | | CAS番号: | 396129-53-6 | | 分子式: | C17H12N4 | | 分子量: | 272.3 | | EINECS: | | | カテゴリ情報: | API;Inhibitors;Smad;TGF-beta | | Mol File: | 396129-53-6.mol |  |
| | 4-(3-ピリジン-2-イル-1H-ピラゾール-4-イル)キノリン 物理性質 |
| 融点 | >230℃ (dec.) | | 沸点 | 490.8±45.0 °C(Predicted) | | 比重(密度) | 1.283±0.06 g/cm3(Predicted) | | 貯蔵温度 | 2-8°C | | 溶解性 | DMSO: soluble2mg/mL, clear | | 酸解離定数(Pka) | 8.94±0.50(Predicted) | | 外見 | powder | | 色 | white to beige | | 安定性： | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. | | InChIKey | IBCXZJCWDGCXQT-UHFFFAOYSA-N |
| | 4-(3-ピリジン-2-イル-1H-ピラゾール-4-イル)キノリン Usage And Synthesis |
| 外観 | 白色〜うすい黄色, 結晶〜粉末 | | 溶解性 | メタノール溶状：1mg/mL | | 説明 | LY-364947 (396129-53-6) is a selective ALK5 inhibitor, IC50 = 59, 400 and 1400 nM for TGF-β RI, TGF-β RII and MLK-7K, respectively.1 Inhibits Smad2 phosphorylation induced by TGF-β as well as fibronectin expression and MDA-MB-231 cell invasion.2 LY-364947 abolishes resistance of glioblastoma-initiating cells to radiation.3?Cell permeable. | | 使用 | LY 364947, is a potent ATP-competitive inhibitor of Tgf-b signaling. | | 定義 | ChEBI: LY 364947 is a member of the class of pyrazoles carrying pyridin-2-yl and quinolin-4-yl substituents at positions 3 and 4 respectively. It has a role as a TGFbeta receptor antagonist. It is a member of pyrazoles, a member of pyridines and a member of quinolines. | | 生物活性 | Selective inhibitor of TGF- β type-I receptor (TGF- β RI, TGFR-I, T β R-I, ALK-5) (IC 50 values are 59, 400 and 1400 nM for TGR- β RI, TGF- β RII and MLK-7K respectively). Inhibits TGF- β -dependent luciferase production in mink lung cells (p3TP lux) and growth in mouse fibroblasts (NIH 3T3) (IC 50 values are 47 and 89 nM respectively). Suppresses invasion of MDA-MB-231 breast cancer cells in a matrigel invasion assay. | | Biochem/physiol Actions | LY-364947 is a selective, ATP-competitive inhibitor of Transforming Growth Factor-β Type I receptor kinase (TGF-β RI, ALK5) with IC50 = 59 nM. It is much less potent at related kinases, with IC50 = 400 nM for TGF-β RII and IC50 = 1400 nM for mixed lineage kinase-7 (MLK-7), a kinase in the MAP kinase signal pathway and closely related to TGF-β RII. LY-364947 inhibits TGF-β-dependent cellular growth (IC50 = 81 nM) in NIH 3T3 mouse fibroblasts. | | in vitro | ly364947 was quickly identified as a potent inhibitor (ic50= 51 nm) and was chosen as a platform for sar development. compounds were further evaluated as inhibitors of tgf-β-dependent luciferase production in mink lung cells (p3tp lux) and growth in mouse fibroblasts (nih 3t3) [1]. | | in vivo | in a rat model of nmda-induced retinal degeneration, simultaneous injection of nmda and the tgf-β inhibitor ly364947 slightly but significantly attenuated the reduction in number of cells in the ganglion cell layer and almost completely prevented the enhancement of capillary degeneration. [3]. | | 貯蔵 | Store at RT | | 参考文献 | 1) Sawyer?et al. (2003),?Synthesis and activity of new aryl-and hetero-aryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain; J. Med. Chem.,?46?3953
2) Shiou?et al. (2006),?Smad4-dependent regulation of urokinase plasminogen activator secretion and RNA stability associated with invasiveness by autocrine and paracrine transforming growth factor-beta; J. Biol. Chem.,?281?33971
3) Hardee?et al. (2012),?Resistance of glioblastoma-initiating cells to radiation mediated by the tumor microenvironment can be abolished by inhibiting transforming growth factor-β; Cancer Res.,?72?4119 |
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