GSK-3 Inhibitor XXII, Compound A

A cell-permeable pyrazolopyridine compound that acts as a potent inhibitor against both GSK-3α and GSK-3β (IC₅₀ = 2.3 and 2 nM, respectively, in the presence of 0.5 µM of ATP) with much reduced or little activity toward a panel of 27 other commonly studied kinases. Shown to selectively inhibit the phosphorylation of cellular tau on GSK-specific serine/threonine residues, but not those targeted by non-GSK kinases, both in primary rat cortical neuron cultures (up to 30 µM) in vitro and in mice (up to 26 mg/kg/day p.o.) in vivo. Chronic oral treatment of compound A is also reported to significantly reduce insoluble tau aggregate formation by up to 70% (26 mg/kg/day p.o.) in brain tissues from JNPL3 mice expressing human 4R0N tau with a FTDP-17 (P301L) mutation.

Packaged under inert gas

Uno. Y., et al. 2009. Brain Res.1296, 148.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)