AS1842856

製品コードS8222 バッチS822204

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H22FN3O3
分子量 347.38 CAS No. 836620-48-5
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 2 mg/mL (5.75 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 AS1842856 is a cell-permeable inhibitor that blocks the transcription activity of Foxo1 with IC50 of 33 nM. It could directly bind to the active Foxo1, but not the Ser256-phosphorylated form. AS1842856 suppresses autophagy.
in vitro

AS1842856 predominantly suppresses Foxo1-mediated transactivation by directly binding to Foxo1. In HepG2 cells transiently transfected with a Foxo1 expression vector, this compound potently represses Foxo1-mediated promoter activity in a dose-dependent manner similar to that seen in insulin treatment. This chemical 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%. This inhibitor may suppress endogenous G6Pase and PEPCK activities by decreasing their mRNA levels, which may lead to inhibition of glucose production in Fao cells[1].
in vivo

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, whereas administration to normal mice has no effect on the fasting plasma glucose level. Treatment with this compound also suppresses an increase in plasma glucose level caused by pyruvate injection in both normal and db/db mice[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Fao cells
濃度 0, 0.1, 1, 10uM
反応時間 30min
実験の流れ

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 this compound, and relative concentration of phosphorylated Foxo1 protein is determined by Western blot analysis.
動物実験 動物モデル db/db mice, ICR mice
投薬量 100mg/kg
投与方法 Oral administration

参考

  • https://pubmed.ncbi.nlm.nih.gov/20736318/
  • http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4613185/?tool=pmcentrez

カスタマーフィードバック

Data from [Data independently produced by , , Biomaterials, 2017, 141:314-329]

Data from [Data independently produced by , , Biochim Biophys Acta Gene Regul Mech, 2017, 1860(6):674-684]

Data from [Data independently produced by , , J Cell Mol Med, 2018, doi:10.1111/jcmm.14073]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Synthetic organochlorines exert bone anabolic activity by modulating CCN3 signaling in osteoblasts [ Environ Int, 2025, 205:109862] PubMed: 41124813
1,25-dihydroxyvitamin D3 attenuates type 1 diabetes-related myocardial apoptosis and fibrosis by influencing the interaction of FoxO1 and p-Smad3 [ Int Immunopharmacol, 2025, 162:115128] PubMed: 40555153
FOXO1 enhances G6PD expression to promote cancer cell antioxidative capacity [ J Mol Cell Biol, 2025, mjaf021] PubMed: 41124013
Propofol in combination with salvianolic acid A protect against lipopolysaccharide-induced cardiac dysfunction and ferroptosis through activating the SIRT1/FoxO1 signaling under diabetic condition [ Ann Med, 2025, 57(1):2570796] PubMed: 41066684
The interplay between FOXO1 and glucocorticoid signaling in promoting the terminal differentiation of somatotropes [ Mol Cell Endocrinol, 2025, 606:112573] PubMed: 40381980
Fibulin1 as a Novel Target for Promoting the Biological Function of Bone Marrow Mesenchymal Stem Cells and Implant Osseointegration in Diabetic Patients [ Int Dent J, 2025, 75(6):103928] PubMed: 41075460
GYY4137 protects against type 2 diabetes mellitus-associated myocardial autophagy by suppressing FOXO1 signal pathway [ Anim Cells Syst (Seoul), 2025, 29(1):13-23] PubMed: 39777025
FoxO1/Rictor axis induces a nongenetic adaptation to ibrutinib via Akt activation in chronic lymphocytic leukemia [ J Clin Invest, 2024, 134(23)e173770] PubMed: 39436708
Genetic and pharmacological targeting of XBP1 alleviates hepatic ischemia reperfusion injury by enhancing FoxO1-dependent mitophagy [ Transl Res, 2024, S1931-5244(24)00051-3] PubMed: 38494125
Hyperglycemia-induced Sirt3 downregulation increases microglial aerobic glycolysis and inflammation in diabetic neuropathic pain pathogenesis [ CNS Neurosci Ther, 2024, 30(8):e14913] PubMed: 39123294

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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