361569

GSK-3beta Inhibitor XXVI - Calbiochem

• Synonym(s): GSK-3beta Inhibitor XXVI - Calbiochem
• Empirical Formula (Hill Notation): C₂₁H₁₈N₄O
• Molecular Weight: 342.39
• MDL number: MFCD28144508
• UNSPSC Code: 12352200

Properties

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

Description

General description

This product has been discontinued.

A cell-permeable, pyrazolone GSK-3β inhibitor (IC₅₀ = 34 nM, in an enzymatic assay) that is highly selective among a panel of 40 kinases that have been profiled with more than 50 fold selectivity. It exhibits no off-target activity against a panel of 44 human and rodent CNS receptors, channels, and transporters except for some modest activity toward 5HT1a. It demonstrates neuroprotective activity of neurons in an oxidative stress model induced by homocysteic acid (HCA) from 1–20 µM, without observable cytotoxicity, and is superior to SB-216763 Cat. No. 361566) at 5 µM in cell micrographs. In addition, it is shown to attenuate locomotor activity in an chlordiazepoxide/amphetamine-induced hyperactivity mice model in vivo at 150 mg/kg.

A cell-permeable, pyrazolone GSK-3β inhibitor (IC₅₀ = 34 nM, in an enzymatic assay) that is highly selective among a panel of 40 kinases that have been profiled with more than 50 fold selectivity. It exhibits no off-target activity against a panel of 44 human and rodent CNS receptors, channels, and transporters except for some modest activity toward 5HT1a. It demonstrates neuroprotective activity of neurons in an oxidative stress model induced by homocysteic acid (HCA) from 1–20 µM, without observable cytotoxicity, and is superior to SB-216763 Cat. No. 361566) at 5 µM in cell micrographs. In addition, it is shown to attenuate locomotor activity in an chlordiazepoxide/amphetamine-induced hyperactivity mice model in vivo at 150 mg/kg.

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

Chen, W., et al. 2011. ChemMedChem6, 1587.

Legal Information

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

Safety Information

• Storage Class: 10-13 - German Storage Class 10 to 13