AS1842856
For research use only.
Catalog No.S8222
16 publications
CAS No. 836620-48-5
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.
4 Customer Reviews
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(E-F) Images and results from microfluidic devices containing human kidney capillaries from young healthy kidneys (n = 6 per group, 2 donors) (E) or aged hypertensive kidneys (n = 5 per group, 1 donor) (F), stimulated to undergo sprouting angiogenesis with VEGF. In the presence of the FOXO1 inhibitor AS1842856 both healthy capillaries and aged capillaries successfully form new capillaries with tip-stalk structures. FOXO1 inhibition enables angiogenic capacity in kidney MVECs like that seen in HUVECs. Capillaries engineered from aged hypertensive kidneys had a higher tendency to form new vascular structures, although these did not show tip cell morphology (F, lower left images). FOXO1 inhibition enhanced new vessel formation with obvious tip cell morphology. Note bpV was less effective in aged capillary.
Biomaterials, 2017, 141:314-329. AS1842856 purchased from Selleck.
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(B) The effects of inactivating FOXO1 and Bcl2 on myoblast apoptosis. AnnexinV-FITC-PI detection method was employed for the detection of apoptotic cells by flow cytometry. PI was used as a counterstain to discriminate dead cells from apoptotic ones. The ratio of apoptotic cells was calculated based on AnnexinV and PI straining. Q1 represents the necrotic cell potion, Q2: apoptotic cells in the late stage; Q3: apoptotic cells in the early stage; Q4: normal cells. (C) The plot of cell proliferation analysis in different cell cycles. (D) The plot of cell apoptosis analysis in different stages. AS1842856 (FOXO1 inhibitor) and ABT199 (Bcl2 inhibitor) were utilized for specific knockdown of FOXO1 and Bcl2 activities in myoblast for 24 h at the concentration of 10 μM with equal volume of DMSO as control groups (n = 4). *P b 0.05; **P b 0.01.
Biochim Biophys Acta Gene Regul Mech, 2017, 1860(6):674-684. AS1842856 purchased from Selleck.
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AS1842856 treatment on the mRNA levels of gluconeogenic genes in Ad‐PANDER‐infected HepG2 cells.
J Cell Mol Med, 2018, doi:10.1111/jcmm.14073. AS1842856 purchased from Selleck.
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The plot of cell proliferation analysis in different cell cycles. Foxo1 inhibitor: AS1842856
Biochim Biophys Acta, 2017, 1860(6):674-684. AS1842856 purchased from Selleck.
Purity & Quality Control
Choose Selective FOX Inhibitors
Biological Activity
| Description | 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. | ||||||||||||||||
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| 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]. |
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| Cell Data |
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| Assay |
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| 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]. |
Protocol
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Solubility (25°C)
| In vitro | DMSO | 23 mg/mL (66.2 mM) |
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| Water | Insoluble | |
| Ethanol | 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.
Chemical Information
| Molecular Weight | 347.38 |
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| Formula | C18H22FN3O3 |
| CAS No. | 836620-48-5 |
| Storage |
powder in solvent |
| Synonyms | N/A |
| Smiles | CCN1C=C(C(=O)C2=C1C=C(C(=C2N)F)NC3CCCCC3)C(=O)O |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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