361558
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.
Synonym(s):
GSK-3 Inhibitor XV - Calbiochem
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About This Item
Empirical Formula (Hill Notation):
C25H14BrN3O6Ru
Molecular Weight:
633.37
UNSPSC Code:
12352200
Quality Level
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
purple
solubility
DMSO: 6 mg/mL
shipped in
wet ice
storage temp.
−20°C
General description
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.
Biochem/physiol Actions
Cell permeable: yes
Product competes with ATP.
Reversible: yes
Target IC50: 0.4 and 0.6 nM for GSK-3α and GSK-3β, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Atilla-Gokcumen, G.E., et al. 2006. ChemBioChem7, 1443.
Legal Information
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
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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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
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
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