AS 1842856

Biological Activity

AS 1842856 is a potent and selective Foxo1 inhibitor (IC₅₀ values are 33 nM at Foxo1 and >1 μM at Foxo3a and Foxo4); decreases Foxo-mediated promoter activity by 70%, 20% and 3% at Foxo1, Foxo4 and Foxo3, respectively. Regulates gluconeogenesis both in vitro and in vivo. Attenuates fasting plasma glucose level in diabetic db/db mice. Also suppresses autophagy, adipocyte differentiation and soluble guanylyl cyclase expression. Also inhibits STAT3 signaling in NSCLC. Orally bioavailable.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Discovery of novel forkhead box O1 inhibitors for treating type 2 diabetes: improvement of fasting glycemia in diabetic db/db mice.
   Nagashima et al.
   Mol.Pharmacol., 2010;78:961
2. FoxO1 antagonist suppresses autophagy and lipid droplet growth in adipocytes.
   Liu et al.
   Cell Cycle, 2016;15:2033
3. Antagonism of forkhead box subclass O transcription factors elicits loss of soluble guanylyl cyclase expression.
   Galley et al.
   Mol.Pharmacol., 2019;95:629

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