Home Metabolism FOX inhibitor - Autophagy inhibitor AS1842856

AS1842856

Catalog No.S8222

For research use only.

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.

AS1842856 Chemical Structure

CAS No. 836620-48-5

Selleck's AS1842856 has been cited by 22 publications

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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.
Targets
Foxo1 [1]
(In HepG2 cells)
33nM
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].
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3L1 preadipocytes NIHGXG5HfW6ldHnvckBie3OjeR?= NIi5ZW8yNjEEoN88US=> M3njVlEzKGSjeYO= NFnZNJFx\XK|aYP0[Y51KHS{ZXH0cYVvfCCxZjDj[YxteyC5aYToJGFUOTh2Mki1OkAp\GG7czCwMVEzMSCjbH3vd5Qh[2:vcHzleIVtgSCycnX2[Y51\WRidHjlJIFlcXCxZ3Xu[ZNqew>? NHfJU449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS4N|A5PCd-MkW0PFMxQDR:L3G+
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot p-JNK / JNK / p-P38 / P38 / p-ERK / ERK ; FoxO1 / FoxO3a / FoxO4 ; Sox2 / Musashi / Nestin / GFAP 26568463 30404794 27448972
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 (from reference)

Cell Research:

[1]
  • Cell lines: Fao cells
  • Concentrations: 0, 0.1, 1, 10uM
  • Incubation Time: 30min
  • Method:

    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)
Animal Research:

[1]
  • Animal Models: db/db mice, ICR mice
  • Dosages: 100mg/kg
  • Administration: Oral administration
  • (Only for Reference)

Solubility (25°C)

In vitro

 DMSO 23 mg/mL warmed
(66.2 mM)
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
Formula

C18H22FN3O3
CAS No. 836620-48-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN1C=C(C(=O)C2=C1C=C(C(=C2N)F)NC3CCCCC3)C(=O)O

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