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.
别名:
GSK-3β Inhibitor XXVII, 3-Amino-6-(4-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-N-(pyridin-3-yl)pyrazine-2-carboxamide, HCl
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
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
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)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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