1-Azakenpaullone is a cell-permeable, potent and selective glycogen synthase kinase 3 inhibitor 3β (GSK3β) with 100-fold lower cross-reactivity with CDKs. 1-Azakenpaullone can be used as a "gold standard" for GSK3 inhibition together with BIO and CHIR9902
Storage Temp
Protected from light,Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 5;Inhibitor of glycogen synthase kinase 3 beta
1.Eldar-Finkelman H, Schreyer SA, Shinohara MM, LeBoeuf RC, Krebs EG. (1999) Increased glycogen synthase kinase-3 activity in diabetes- and obesity-prone C57BL/6J mice.. Diabetes, 48 (8):(1662-6). [PMID:10426388]
2.Nikoulina SE, Ciaraldi TP, Mudaliar S, Mohideen P, Carter L, Henry RR. (2000) Potential role of glycogen synthase kinase-3 in skeletal muscle insulin resistance of type 2 diabetes.. Diabetes, 49 (2):(263-71). [PMID:10868943]
3.Kunick C, Lauenroth K, Leost M, Meijer L, Lemcke T. (2004) 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.. Bioorg Med Chem Lett, 14 (2):(413-6). [PMID:14698171]
4.Cai Z, Zhao Y, Zhao B. (2012) Roles of glycogen synthase kinase 3 in Alzheimer's disease.. Curr Alzheimer Res, 9 (7):(864-79). [PMID:22272620]
5.Hurtado DE, Molina-Porcel L, Carroll JC, Macdonald C, Aboagye AK, Trojanowski JQ, Lee VM. (2012) Selectively silencing GSK-3 isoforms reduces plaques and tangles in mouse models of Alzheimer's disease.. J Neurosci, 32 (21):(7392-402). [PMID:22623685]
6.Takashima A, Noguchi K, Sato K, Hoshino T, Imahori K. (1993) Tau protein kinase I is essential for amyloid beta-protein-induced neurotoxicity.. Proc Natl Acad Sci USA, 90 (16):(7789-93). [PMID:8356085]
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E2305186