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| | 2-(3-(6-メチルピリジン-2-イル)-1H-ピラゾール-4-イル)-1,5-ナフチリジン 製品概要 |
| 化学名: | 2-(3-(6-メチルピリジン-2-イル)-1H-ピラゾール-4-イル)-1,5-ナフチリジン | | 英語化学名: | ALK5 inhibitor II | | 别名: | ALK5 INHIBITOR I;2-(3-(6-METHYLPYRIDIN-2-YL)-1H-PYRAZOL-4-YL)-1,5-NAPHTHYRIDINE;2-(3-(6-Methylpyridine-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine;SJN 2511;2-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]-1,5-naphthyridine;E 616452;E616452;1,5-Naphthyridine, 2-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]- | | CAS番号: | 446859-33-2 | | 分子式: | C17H13N5 | | 分子量: | 287.32 | | EINECS: | | | カテゴリ情報: | Selective inhibitor of the TGF-β type I receptor ALK5.;Smad;TGF-beta;Inhibitors | | Mol File: | Mol File |  |
| | 2-(3-(6-メチルピリジン-2-イル)-1H-ピラゾール-4-イル)-1,5-ナフチリジン 物理性質 |
| 融点 | 195 °C | | 沸点 | 501.9±50.0 °C(Predicted) | | 比重(密度) | 1.296±0.06 g/cm3(Predicted) | | 貯蔵温度 | 2-8°C | | 溶解性 | DMSO: >20mg/mL | | 外見 | Yellow solid | | 酸解離定数(Pka) | 10.05±0.50(Predicted) | | 色 | Pale yellow | | 安定性： | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. | | InChIKey | LBPKYPYHDKKRFS-UHFFFAOYSA-N |
| 主な危険性 | T | | Rフレーズ | 25 | | Sフレーズ | 45 | | RIDADR | UN 2811 | | WGK Germany | 3 |
| | 2-(3-(6-メチルピリジン-2-イル)-1H-ピラゾール-4-イル)-1,5-ナフチリジン Usage And Synthesis |
| 外観 | 黄色〜黄褐色, 結晶〜粉末 | | 溶解性 | メタノールに溶ける。 | | 説明 | RepSox (446859-33-2) is a potent (IC50?ALK5 auto-P= 4 nM; IC50?TGF-β cellular assay = 23 nM) inhibitor of the TGF-β type I receptor (ALK5).1?RepSox can replace Sox2 in reprogramming adult cells into pluripotent stem cells via induction of Nanog transcription.2?It was able to convert astrocytes into neuronal cells as part of a small molecule cocktail (along with valproic acid and CHIR99021).3,4 | | 使用 | Alk 5 Inhibitor II is a selective ATP competitive inhibitor of transforming growth factor-β (TGFβ). A potential drug for the treatment of fibrosis and cancer. | | 使用 | RepSox has been used as an inhibitor of autophosphorylation of the transforming growth factor β type I receptor kinase (ALK5). It has also been used as a basal media component for culturing human Pluripotent stem cells. | | 定義 | ChEBI: 1,5-naphthyridine, 2-[3-(6-methyl-2-pyridinyl)-1h-pyrazol-4-yl]- is a pyrazolopyridine. | | Biochem/physiol Actions | RepSox Inhibits TGF-beta receptor signaling. Retroviral transduction of Sox2, Oct4, and Klf4 genes results in direct reprogramming of somatic cells into induced pluripotent stem cells (iPSCs). | | 貯蔵 | +4°C | | 参考文献 | 1) Gellibert?et al. (2004),?Identification of 1,5-Naphthyridine Derivatives as a Novel Series of Potent and Selective TGF-β Type I Receptor Inhibitors; J. Med. Chem.?47?4494
2) Ichida?et al.?(2009),?A Small-molecule Inhibitor of TGF-β Signaling Replaces Sox2 in Reprogramming by Inducing Nanog; Cell Stem Cell?5?491
3) Cheng?et al.?(2015),?Direct Conversion of astrocytes into neuronal cells by a drug cocktail;?Cell Res.?25?1269
4) Cheng?et al.?(2014),?Generation of neural progenitor cells by chemical cocktails and hypoxia; Cell Res.?24?665 |
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