Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that has been implicated in pathological conditions such as diabetes and Alzheimer′s disease. GSK3 inhibitor, AR-A014418, inhibits GSK3 (IC50 = 104 nM), in an ATP-competitive manner (Ki = 38 n
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of glycogen synthase kinase 3 beta
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
AR-A014418 is a selective and effective GSK3β inhibitor with an IC 50 value of 104 +/- 27 nM; no significant inhibition on 26 other kinases.
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.Bhat R, Xue Y, Berg S, Hellberg S, Ormö M, Nilsson Y, Radesäter AC, Jerning E, Markgren PO, Borgegård T et al.. (2003) Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418.. J Biol Chem, 278 (46):(45937-45). [PMID:12928438]
4.Koh SH, Kim Y, Kim HY, Hwang S, Lee CH, Kim SH. (2007) Inhibition of glycogen synthase kinase-3 suppresses the onset of symptoms and disease progression of G93A-SOD1 mouse model of ALS.. Exp Neurol, 205 (2):(336-46). [PMID:17433298]
5.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]
6.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]
7.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]
8.Stoica R et al.. (2014) ER-mitochondria associations are regulated by the VAPB-PTPIP51 interaction and are disrupted by ALS/FTD-associated TDP-43.. Nat Commun, 5 (3996). [PMID:24893131]
9.Chi D et al.. (2020) LINC01207 Predicts Poor Prognosis and Suppresses Cell Growth and Metastasis via Regulating GSK-3ß/ß-Catenin Signaling Pathway in Malignant Glioma.. Med Sci Monit, 26 (e923189). [PMID:32533688]
10.Kobayashi M et al.. (2016) Wnt-ß-catenin signaling regulates ABCC3 (MRP3) transporter expression in colorectal cancer.. Cancer Sci, 107 (12):(1776-1784). [PMID:27709738]
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