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Merck

361570

GSK-3β Inhibitor XXVII

The GSK-3β Inhibitor XXVII controls the biological activity of GSK-3β. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

GSK-3β Inhibitor XXVII, 3-Amino-6-(4-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-N-(pyridin-3-yl)pyrazine-2-carboxamide, HCl

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About This Item

Empirical Formula (Hill Notation):
C21H23N7O3S · 2.5HCl · 5H2O
Molecular Weight:
634.75
UNSPSC Code:
12352200
Assay:
≥99% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light

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assay

≥99% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

yellow

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

General description

A cell-permeable pyridinylpyrazinecarboxamide compound that acts as a highly potent, reversible, and ATP-competitive inhibitor of GSK-3β (Ki = 4.9 nM) with ~110-fold greater selectivity over Cdk2 (Ki = 540 nM). Shows only a trivial effect on the activities of 26-related kinases at much higher doses. Blocks GSK-3β-mediated phosphorylation of Ser396 in stably transfected 3T3 fibroblasts expressing four-repeat tau protein (IC50 = 76 nM). Readily crosses blood-brain barrier and exhibits desirable bioavailability and aqueous solubility.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
GSK-3β
Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Berg. S., et al. 2012. J. Med. Chem.55, 9107.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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