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别名 | SJN 2511,ALK5 Inhibitor II | 储存条件 (自收到货起) |
3年 / -20°C / 粉状 1年 / -80°C / 溶于溶剂 |
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化学式 | C17H13N5 |
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分子量 | 287.32 | CAS号 | 446859-33-2 | ||||
Solubility (25°C)* | 体外 | DMSO | 57 mg/mL (198.38 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
体内(现配现用) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
产品描述 | RepSox (E-616452, SJN 2511, ALK5 Inhibitor II)是一种有效的,选择性TGFβR-1/ALK5抑制剂,作用于ATP与ALK5结合以及ALK5自磷酸化,无细胞试验中IC50分别为23 nM和4 nM。 | ||
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靶点 |
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体外研究 | RepSox抑制ATP结合到ALK5和抑制ALK5自磷酸化,IC50分别为23 nM和4 nM。RepSox抑制TGF-β 诱导的细胞PAI-1荧光素酶活性,IC50为18 nM。[1] RepSox在重编程中通过抑制转化生长因子-β(Tgf-β)信号,能够成功取代Sox2,这反过来又导致Nanog表达。RepSox诱导重编程不需要染色质重塑。RepSox对产生iPSCs是有效的。[2] |
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体内研究 | RepSox注射到囊胚,有助于在体内形成嵌合体胚胎。RepSox处理一天,足以取代转基因的Sox2。[2] |
激酶实验 | ALK5荧光偏振结合检测 | |
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使用纯化的重组GST-ALK5(残基198-503)检测化合物与ALK5结合。通过使用不同浓度的实验化合物,进行罗丹明绿色荧光标记的ATP竞争性抑制剂取代,计算结合pIC50。GST-ALK5加入到含 62.5 mM Hepes, pH 7.5, 1 mM DTT, 12.5 mM MgCl2, 1.25 mM CHAPS, 和1 nM 进行罗丹明绿色荧光标记配体的缓冲液中,根据酶的活性位点滴定,ALK5终浓度为10 nM。40μL酶/配体试剂加入到含1 μL不同浓度实验化合物的384孔实验板中。使用荧光分析仪立即对实验板进行读数,激发,发射和分色滤光片分别在485,530,和505 nm处。通过Acquest计算每孔的荧光偏振,然后导入到曲线拟合软件,用于构造浓度-反应曲线。 |
数据来源于[Data independently produced by , , Protein Cell, 2017, 8(4):273-283]
数据来源于[Data independently produced by , , Wound Repair Regen, 2017, 25(3):526-531]
数据来源于[Data independently produced by , , Dev Biol, 2017,421(2):149-160]
GelMA/PEDOT:PSS Composite Conductive Hydrogel-Based Generation and Protection of Cochlear Hair Cells through Multiple Signaling Pathways [ Biomolecules, 2024, 14(1)95] | PubMed: 38254695 |
Downregulation of Hsp90 and the antimicrobial peptide Mtk suppresses poly(GR)-induced neurotoxicity in C9ORF72-ALS/FTD [ Neuron, 2023, 111(9):1381-1390.e6] | PubMed: 36931278 |
M2-like tumor-associated macrophages promote epithelial-mesenchymal transition through the transforming growth factor β/Smad/zinc finger e-box binding homeobox pathway with increased metastatic potential and tumor cell proliferation in lung squamous cell carcinoma [ Cancer Sci, 2023, 10.1111/cas.15987] | PubMed: 37806311 |
Neural progenitor cells derived from fibroblasts induced by small molecule compounds under hypoxia for treatment of Parkinson's disease in rats [ Neural Regen Res, 2023, 18(5):1090-1098] | PubMed: 36254998 |
Slow Interstitial Fluid Flow Activates TGF-β Signaling and Drives Fibrotic Responses in Human Tenon Fibroblasts [ Cells, 2023, 12(17)2205] | PubMed: 37681937 |
Slow Interstitial Fluid Flow Activates TGF-β Signaling and Drives Fibrotic Responses in Human Tenon Fibroblasts [ Cells, 2023, 12(17)2205] | PubMed: 37681937 |
The Multi-Kinase Inhibitor RepSox Enforces Barrier Function in the Face of Both VEGF and Cytokines [ Biomedicines, 2023, 11(9)2431] | PubMed: 37760872 |
The Multi-Kinase Inhibitor RepSox Enforces Barrier Function in the Face of Both VEGF and Cytokines [ Biomedicines, 2023, 10.3390/biomedicines11092431] | PubMed: 37760872 |
CLIP-Seq analysis enables the design of protective ribosomal RNA bait oligonucleotides against C9ORF72 ALS/FTD poly-GR pathophysiology [ Sci Adv, 2023, 10.1126/sciadv.adf7997] | PubMed: 37948524 |
[Chemical reprogramming of human embryonic fibroblasts into neural progenitor cells in vitro] [ Nan Fang Yi Ke Da Xue Xue Bao, 2023, 10.12122/j.issn.1673-4254.2023.03.04] | PubMed: 37087579 |
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如果需要长期保存,请于零下二十度低温保存。禁止用于人体及治疗!
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