361563

GSK-3 Inhibitor XXII, Compound A

• Synonym(s): GSK-3 Inhibitor XXII, Compound A, 6-Methyl-N-[3-[[3-(1-methylethoxy)propyl]carbamoyl]-1H-pyrazol-4-yl]pyridine-3-carboxamide
• Empirical Formula (Hill Notation): C₁₇H₂₃N₅O₃
• Molecular Weight: 345.40
• UNSPSC Code: 12352200

Properties

• assay: ≥95% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: green-gray
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

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.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable