AR-A014418

• CAT Number: I022372
• CAS Number: 663214-64-0
• Molecular Formula: C27H27ClN6O4
• Molecular Weight: 535.00
• Purity: 98%
• Synonyms: AR-A014418
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Storage: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
• IUPAC Name: 5-chloro-3-[[4-[(2,4-diaminopyrimidin-5-yl)methyl]-6,7-dimethoxy-1-benzofuran-2-yl]methyl]-N,N-dimethyl-1H-indole-2-carboxamide
• InChI: InChI=1S/C27H27ClN6O4/c1-34(2)26(35)22-19(18-9-15(28)5-6-20(18)32-22)11-16-10-17-13(7-14-12-31-27(30)33-25(14)29)8-21(36-3)24(37-4)23(17)38-16/h5-6,8-10,12,32H,7,11H2,1-4H3,(H4,29,30,31,33)
• InChIKey: ASSNCSVJAZEMQG-UHFFFAOYSA-N
• SMILES: CN(C)C(=O)C1=C(C2=C(N1)C=CC(=C2)Cl)CC3=CC4=C(O3)C(=C(C=C4CC5=CN=C(N=C5N)N)OC)OC

AR-A014418（Cat No.:I022372）is a selective small molecule inhibitor of glycogen synthase kinase-3 (GSK-3), an enzyme involved in numerous cellular processes, including cell survival, metabolism, and neurodevelopment. By inhibiting GSK-3, AR-A014418 has shown potential in various therapeutic areas, including neurodegenerative diseases, such as Alzheimer’s disease, and cancer. GSK-3 is also implicated in regulating β-catenin, a key player in the Wnt signaling pathway, which is involved in tumor progression. Preclinical studies suggest that AR-A014418 may improve cognitive function and reduce tumor growth, with ongoing research to explore its clinical applications and safety.

Reference

1: Aristizabal Prada ET, Weis C, Orth M, Lauseker M, Spöttl G, Maurer J, Grabowski P, Grossman A, Auernhammer CJ, Nölting S. GSK3α/β: A Novel Therapeutic Target for Neuroendocrine Tumors. Neuroendocrinology. 2018;106(4):335-351. doi: 10.1159/000481887. Epub 2017 Oct 2. PubMed PMID: 28968593.
2: Zhang M, Zhang P, Liu Y, Zhou Y. GSK3 inhibitor AR-A014418 promotes osteogenic differentiation of human adipose-derived stem cells via ERK and mTORC2/Akt signaling pathway. Biochem Biophys Res Commun. 2017 Aug 19;490(2):182-188. doi: 10.1016/j.bbrc.2017.06.018. Epub 2017 Jun 8. PubMed PMID: 28602697.
3: Kunnimalaiyaan S, Gamblin TC, Kunnimalaiyaan M. Glycogen synthase kinase-3 inhibitor AR-A014418 suppresses pancreatic cancer cell growth via inhibition of GSK-3-mediated Notch1 expression. HPB (Oxford). 2015 Sep;17(9):770-6. doi: 10.1111/hpb.12442. Epub 2015 Jul 6. PubMed PMID: 26147011; PubMed Central PMCID: PMC4557650.
4: Martins DF, Rosa AO, Gadotti VM, Mazzardo-Martins L, Nascimento FP, Egea J, López MG, Santos AR. The antinociceptive effects of AR-A014418, a selective inhibitor of glycogen synthase kinase-3 beta, in mice. J Pain. 2011 Mar;12(3):315-22. doi: 10.1016/j.jpain.2010.06.007. Epub 2010 Aug 12. PubMed PMID: 20705523.
5: Gould TD, Einat H, Bhat R, Manji HK. AR-A014418, a selective GSK-3 inhibitor, produces antidepressant-like effects in the forced swim test. Int J Neuropsychopharmacol. 2004 Dec;7(4):387-90. Epub 2004 Jul 26. PubMed PMID: 15315719.