[HTML][HTML] Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418
R Bhat, Y Xue, S Berg, S Hellberg, M Ormö… - Journal of Biological …, 2003 - ASBMB
Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that has been implicated in
pathological conditions such as diabetes and Alzheimer's disease. We report the
characterization of a GSK3 inhibitor, AR-A014418, which inhibits GSK3 (IC 50= 104±27 nM),
in an ATP-competitive manner (K i= 38 nM). AR-A014418 does not significantly inhibit cdk2
or cdk5 (IC 50> 100 μM) or 26 other kinases demonstrating high specificity for GSK3. We
report the co-crystallization of AR-A014418 with the GSK3β protein and provide a …
pathological conditions such as diabetes and Alzheimer's disease. We report the
characterization of a GSK3 inhibitor, AR-A014418, which inhibits GSK3 (IC 50= 104±27 nM),
in an ATP-competitive manner (K i= 38 nM). AR-A014418 does not significantly inhibit cdk2
or cdk5 (IC 50> 100 μM) or 26 other kinases demonstrating high specificity for GSK3. We
report the co-crystallization of AR-A014418 with the GSK3β protein and provide a …