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AS1842856 是一种 Foxo1 抑制剂 (IC50=30 nM),具有特异性,可阻断 Foxo1 的转录活性,直接结合活化 FoxO1 而降低其活性。AS1842856 具有抑制自噬的活性。
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AS1842856 是一种 Foxo1 抑制剂 (IC50=30 nM),具有特异性,可阻断 Foxo1 的转录活性,直接结合活化 FoxO1 而降低其活性。AS1842856 具有抑制自噬的活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 267 | 现货 | |
2 mg | ¥ 376 | 现货 | |
5 mg | ¥ 690 | 现货 | |
10 mg | ¥ 872 | 现货 | |
25 mg | ¥ 1,680 | 现货 | |
50 mg | ¥ 2,970 | 现货 | |
100 mg | ¥ 4,390 | 现货 | |
200 mg | ¥ 6,280 | 现货 | |
500 mg | ¥ 9,490 | 现货 |
产品描述 | AS1842856 is a Foxo1 inhibitor (IC50=30 nM) that specifically blocks the transcriptional activity of Foxo1 and reduces its activity by directly binding to activated FoxO1. AS1842856 has autophagy inhibitory activity. |
靶点活性 | FOXO1:33nM |
体外活性 | 方法:大鼠肝癌 Fao 细胞用 AS1842856 (0-10 µM) 处理 18 h,通过 RT-PCR 检测基因表达水平。 结果:用 AS1842856 处理 Fao 细胞导致 G6Pase 和 PEPCK 的 mRNA 水平受到剂量依赖性抑制,Foxo1 mRNA 水平没有差异。[1] 方法:基底样乳腺癌细胞系 (MDA-MB-468、BT549) 和 胶质母细胞瘤细胞系 (LN229、DBTRG A172、LN18) 用 AS1842856 (0.2-1 µM) 处理 5 天,进行 Colony formation assay。 结果:经 AS1842856 处理的样品经 200 nM 药物处理后细胞较少,经 500 nM 和 1 µM 药物处理后进一步减少。[2] |
体内活性 | 方法:为研究对糖尿病的作用,将 AS1842856 (100 mg/kg,6% cyclodextrin) 口服给药给糖尿病 db/db 小鼠,给药三次。 结果:对糖尿病 db/db 小鼠口服 AS1842856 通过抑制肝脏糖异生基因导致空腹血糖水平急剧下降,而对正常小鼠的给药对空腹血糖水平没有影响。AS1842856 治疗还抑制了正常和 db/db 小鼠中丙酮酸注射引起的血糖水平升高。[1] |
细胞实验 | Fao cells are serum-starved (1 h) and incubated for 30 min with either insulin or AS1842856 at the indicated concentration. Protein lysates are prepared from cells treated with either insulin or AS1842856, and relative concentration of phosphorylated Foxo1 protein is determined by Western blot analysis. (Only for Reference) |
分子量 | 347.38 |
分子式 | C18H22FN3O3 |
CAS No. | 836620-48-5 |
Smiles | CCn1cc(C(O)=O)c(=O)c2c(N)c(F)c(NC3CCCCC3)cc12 |
密度 | 1.370 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | DMSO: 3.47 mg/mL (10 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+90% Saline: 0.1 mg/mL (0.29 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. |
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