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Description
Overview
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.
GSK-3 Inhibitor XXII, Compound A - Calbiochem Certificates of Analysis
Title
Lot Number
361563
References
Reference overview
Uno. Y., et al. 2009. Brain Res.1296, 148.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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.
Form
Green-grey solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₁₇H₂₃N₅O₃
Structure formula
Purity
≥95% by HPLC
Solubility
DMSO (50 mg/ml)
Storage
+2°C to +8°C
Protect from light
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
