For research use only. Not for therapeutic Use.
AS1842856（Cat No.:I002883） is a potent cell-permeable inhibitor that specifically targets the transcriptional activity of Foxo1, a key regulator of cellular processes. It exhibits an IC50 of 33nM and binds directly to activated Foxo1. Interestingly, it does not interact with phosphorylated Foxo1 at Ser256. In addition to inhibiting Foxo1, AS1842856 also demonstrates inhibitory effects on autophagy. This compound shows promise in the field of cellular regulation and may have potential applications in diseases where Foxo1 and autophagy play critical roles.
| Catalog Number | I002883 |
| CAS Number | 836620-48-5 |
| Synonyms | AS1842856; AS-1842856; AS 1842856.;5-amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid |
| Molecular Formula | C18H22FN3O3 |
| Purity | ≥95% |
| Target | Autophagy |
| Solubility | Soluble in DMSO |
| Storage | -20°C |
| IUPAC Name | 5-amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxoquinoline-3-carboxylic acid |
| InChI | InChI=1S/C18H22FN3O3/c1-2-22-9-11(18(24)25)17(23)14-13(22)8-12(15(19)16(14)20)21-10-6-4-3-5-7-10/h8-10,21H,2-7,20H2,1H3,(H,24,25) |
| InChIKey | MOMCHYGXXYBDCD-UHFFFAOYSA-N |
| SMILES | CCN1C=C(C(=O)C2=C1C=C(C(=C2N)F)NC3CCCCC3)C(=O)O |
| Reference | 1:Cell Cycle. 2014;13(23):3759-67. doi: 10.4161/15384101.2014.965977. Targeting FoxO1 with AS1842856 suppresses adipogenesis.Zou P,Liu L,Zheng L,Liu L,Stoneman RE,Cho A,Emery A,Gilbert ER,Cheng Z, PMID: 25483084 PMCID: PMC4613185 DOI: 10.4161/15384101.2014.965977 </br><span>Abstract:</span> Hyperplasia (i.e., increased adipogenesis) contributes to excess adiposity, the hallmark of obesity that can trigger metabolic complications. As FoxO1 has been implicated in adipogenic regulation, we investigated the kinetics of FoxO1 activation during adipocyte differentiation, and tested the effects of FoxO1 antagonist (AS1842856) on adipogenesis. We found for the first time that the kinetics of FoxO1 activation follows a series of sigmoid curves, and reveals the phases relevant to clonal expansion, cell cycle arrest, and the regulation of PPARγ, adiponectin, and mitochondrial proteins (complexes I and III). In addition, multiple activation-inactivation transitions exist in the stage of terminal differentiation. Importantly, persistent inhibition of FoxO1 with AS1842856 almost completely suppressed adipocyte differentiation, while selective inhibition in specific stages had differential effects on adipogenesis. Our data present a new view of FoxO1 in adipogenic regulation, and suggest AS1842856 can be an anti-obesity agent that warrants further investigation. |
