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
• Empirical Formula (Hill Notation): C₂₁H₂₃N₇O₃S · 2.5HCl · 5H₂O
• Molecular Weight: 634.75
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• 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

Description

General description

A cell-permeable pyridinylpyrazinecarboxamide compound that acts as a highly potent, reversible, and ATP-competitive inhibitor of GSK-3β (K_i = 4.9 nM) with ~110-fold greater selectivity over Cdk2 (K_i = 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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable