AS1842856

製品コードS8222 バッチS822204

化学情報

	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	2 mg/mL warmed with 50ºC water bath (5.75 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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, 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].
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 AS1842856 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 AS1842856, 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

[1] Takeyuki Nagashima,et al.Mol Pharmacol.2010,78(5):961-970.

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：

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
TRIM15 forms a regulatory loop with the AKT/FOXO1 axis and LASP1 to modulate the sensitivity of HCC cells to TKIs [ Cell Death Dis, 2023, 14(1):47]	PubMed: 36670097
Accumulation of branched-chain amino acids reprograms glucose metabolism in CD8+ T cells with enhanced effector function and anti-tumor response [ Cell Rep, 2023, 42(3):112186]	PubMed: 36870057
Melatonin-Mediated Suppression of mtROS-JNK-FOXO1 Pathway Alleviates Hypoxia-Induced Apoptosis in Porcine Granulosa Cells [ Antioxidants -Basel), 2023, 12(10)1881]	PubMed: 37891959
Melatonin-Mediated Suppression of mtROS-JNK-FOXO1 Pathway Alleviates Hypoxia-Induced Apoptosis in Porcine Granulosa Cells [ Antioxidants (Basel), 2023, 12(10)1881]	PubMed: 37891959
Dose-dependent expression of GFI1 alters metabolism in the haematopoietic progenitors and MLL::AF9-induced leukaemic cells [ Br J Haematol, 2023, 10.1111/bjh.18939]	PubMed: 37423893
Resveratrol Upregulates Senescence Marker Protein 30 by Activating AMPK/Sirt1-Foxo1 Signals and Attenuating H2O2-Induced Damage in FAO Rat Liver Cells [ J Nutr Sci Vitaminol (Tokyo), 2023, 10.3177/jnsv.69.388]	PubMed: 37940580
Telomerase RNA TERC and the PI3K-AKT pathway form a positive feedback loop to regulate cell proliferation independent of telomerase activity [ Nucleic Acids Res, 2022, gkac179]	PubMed: 35323972
Laminaria japonica Polysaccharide Suppresses Atherosclerosis via Regulating Autophagy-Mediated Macrophage Polarization [ J Agric Food Chem, 2022, 10.1021/acs.jafc.1c07483]	PubMed: 35167294
FOXO1 Is a Key Mediator of Glucocorticoid-Induced Expression of Tristetraprolin in MDA-MB-231 Breast Cancer Cells [ Int J Mol Sci, 2022, 23(22)13673]	PubMed: 36430156

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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