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Merck
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Documentos Principais

361569

Millipore

GSK-3beta Inhibitor XXVI - Calbiochem

Sinônimo(s):

GSK-3beta Inhibitor XXVI - Calbiochem

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About This Item

Fórmula empírica (Notação de Hill):
C21H18N4O
Peso molecular:
342.39
Número MDL:
Código UNSPSC:
12352200

Ensaio

≥95% (HPLC)

Nível de qualidade

Formulário

solid

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
protect from light

cor

white

solubilidade

DMSO: 50 mg/mL, light yellow

Condições de expedição

ambient

temperatura de armazenamento

2-8°C

Descrição geral

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.

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

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

Informações legais

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

Código de classe de armazenamento

10-13 - German Storage Class 10 to 13


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