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361558

Sigma-Aldrich

GSK-3 Inhibitor XV - Calbiochem

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

Sinônimo(s):

GSK-3 Inhibitor XV - Calbiochem

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About This Item

Fórmula empírica (Notação de Hill):
C25H14BrN3O6Ru
Peso molecular:
633.37
Código UNSPSC:
12352200

Nível de qualidade

Ensaio

≥98% (HPLC)

Formulário

solid

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
protect from light

cor

purple

solubilidade

DMSO: 6 mg/mL

Condições de expedição

wet ice

temperatura de armazenamento

−20°C

Descrição geral

The racemic mixture of a cell-permeable pyridocarbazolo-cyclopentadienyl Ruthenium complex that acts as a reversible, ATP-competitive, and highly potent inhibitor of GSK-3 (IC50 = 0.4 and 0.6 nM for GSK-3α and GSK-3β, respectively) with ∼5-fold selectivity over PIM-1 kinase (IC50 = 3 nM). Studies using isolated enantiomers have shown that the (R)-enantiomer is GSK-3-selective (IC50 = 0.35, 0.55, and 35 nM for GSK-3α GSK-3β, and Pim-1, respectively) and interferes with normal zebrafish embryo development (1 µM), while the (S)-enantiomer is Pim-1-selective (IC50 = 80, 90, and 3 nM for GSK-3α GSK-3β, and Pim-1, respectively) and exhibits no effect in embryo development at the same dosage.

Ações bioquímicas/fisiológicas

Cell permeable: yes
Product competes with ATP.
Reversible: yes
Target IC50: 0.4 and 0.6 nM for GSK-3α and GSK-3β, respectively

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 6 months at -20°C.

Outras notas

Atilla-Gokcumen, G.E., et al. 2006. ChemBioChem7, 1443.

Informações legais

Sold for research purposes only, pursuant to an agreement with University of Pennsylvania.Sold under license of U.S. Patent 7,488,817.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 2

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


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G Ekin Atilla-Gokcumen et al.
Chembiochem : a European journal of chemical biology, 7(9), 1443-1450 (2006-07-22)
A chiral second-generation organoruthenium half-sandwich compound is disclosed that shows a remarkable selectivity and cellular potency for the inhibition of glycogen synthase kinase 3 (GSK-3). The selectivity was evaluated against a panel of 57 protein kinases, in which no other
Rikke H Kofoed et al.
Neurobiology of disease, 136, 104720-104720 (2019-12-28)
Parkinson's disease (PD) is a currently incurable disease and the number of patients is expected to increase due to the extended human lifespan. α-Synuclein is a pathological hallmark of PD and variations and triplications of the gene encoding α-synuclein are
Xuzhe Zhang et al.
Molecular biology and evolution, 37(2), 507-523 (2019-10-22)
Evolution of highly invasive placentation in the stem lineage of eutherians and subsequent extension of pregnancy set eutherians apart from other mammals, that is, marsupials with short-lived placentas, and oviparous monotremes. Recent studies suggest that eutherian implantation evolved from marsupial
Lasse Reimer et al.
Brain pathology (Zurich, Switzerland), 31(1), 103-119 (2020-07-28)
Deposition of extensively hyperphosphorylated tau in specific brain cells is a clear pathological hallmark in Alzheimer's disease and a number of other neurodegenerative disorders, collectively termed the tauopathies. Furthermore, hyperphosphorylation of tau prevents it from fulfilling its physiological role as

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