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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C17H23N5O3
Molecular Weight:
345.40
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
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assay

≥95% (HPLC)

Quality Level

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

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

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)


Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificates of Analysis (COA)

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