AS1842856
作者：齐岳
发布时间：2023-09-13
17:40:10
点击数：
产品名称：AS1842856
产品描述：
| 产品描述 | AS1842856, a cell-permeable inhibitor, can block the transcription activity of Foxo1 (IC50: 33 nM). It can directly bind to the active Foxo1, but not the Ser256-phosphorylated form. |
| 靶点活性 | Foxo1:33nM |
| 体外活性 | AS1842856 predominantly suppresses Foxo1-mediated transactivation by directly binding to Foxo1. In HepG2 cells transiently transfected with a Foxo1 expression vector, AS1842856 potently represses Foxo1-mediated promoter activity in a dose-dependent manner similar to that seen in insulin treatment.AS1842856 administered at 0.1 μM inhibits Foxo3a- and Foxo4-mediated promoter activity by 3 and 20%, respectively. In contrast, Foxo1-mediated promoter activity is decreased by 70%. Foxo1 inhibitor AS1842856 may suppress endogenous G6Pase and PEPCK activities by decreasing their mRNA levels, which may lead to inhibition of glucose production in Fao cells[1]. |
| 体内活性 | Oral administration of AS1842856 to diabetic db/db mice leads to a drastic decrease in fasting plasma glucose level via the inhibition of hepatic gluconeogenic genes while administration to normal mice does not affect on the fasting plasma glucose level. Treatment with AS1842856 also suppresses an increase in plasma glucose level caused by pyruvate injection in both normal and db/db mice[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 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 7 mg/mL(20.2 mM)
Ethanol: <1 mg/mL
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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