2-Thio(3-iodobenzyl)-5-(1-pyridyl)-[1,3,4]-oxadiazole

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2-Thio(3-iodobenzyl)-5-(1-pyridyl)-[1,3,4]-oxadiazole manufacturers
2-Thio(3-iodobenzyl)-5-(1-pyridyl)-[1,3,4]-oxadiazole Basic information
Product Name:2-Thio(3-iodobenzyl)-5-(1-pyridyl)-[1,3,4]-oxadiazole
Synonyms:TIBPO;GLYCOGEN SYNTHASE KINASE-3 INHIBITOR II;GSK-3 INHIBITOR II;Pyridine, 4-[5-[[(3-iodophenyl)Methyl]thio]-1,3,4-oxadiazol-2-yl]-;4-[5-[[(3-Iodophenyl)methyl]thio]-1,3,4-oxadiazol-2-yl]pyridine;GSK3.beta. Inhibitor II;GSK-3β Inhibitor II - CAS 478482-75-6 - Calbiochem;GSK3β Inhibitor II
CAS:478482-75-6
MF:C14H10IN3OS
MW:395.22
EINECS:
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Mol File:Mol File
2-Thio(3-iodobenzyl)-5-(1-pyridyl)-[1,3,4]-oxadiazole Structure
2-Thio(3-iodobenzyl)-5-(1-pyridyl)-[1,3,4]-oxadiazole Chemical Properties
Boiling point 532.6±60.0 °C(Predicted)
density 1.79±0.1 g/cm3(Predicted)
storage temp. -20C
solubility ≤3mg/ml in DMSO;10mg/ml in dimethyl formamide
form Yellow solid
pka0.97±0.10(Predicted)
color White to off-white
Safety Information
MSDS Information
2-Thio(3-iodobenzyl)-5-(1-pyridyl)-[1,3,4]-oxadiazole Usage And Synthesis
UsesGSK3β inhibitor II is an inhibitor of GSK3β. GSK3β inhibitor II can be used for research of Alzheimer’s disease (AD)[1].
DefinitionChEBI: 2-[(3-iodophenyl)methylthio]-5-pyridin-4-yl-1,3,4-oxadiazole is an aryl sulfide.
Biological Activitygsk-3β inhibitor ii is a gsk-3β inhibitor.glycogen synthase kinase-3 (gsk-3), a protein-serine kinase, is implicated in the hormonal control of various regulatory proteins. a number of substrates have been identified, which implicates gsk-3 in the regulation of several physiological processes. moreover, it has been reported that compounds that specifically inhibit gsk-3 activity may be useful in the treatment of diabetes.
in vitroin a previous study, by using a virtual screening strategy based on a methodology derived from the cats molecular descriptor, a novel compound class including gsk-3β inhibitor ii with inhibitory activity against the gsk-3 enzyme was identified via scaffold hopping. gsk-3β inhibitor ii was found to be a potent inhibitor of gsk-3β with the ic50 value of 390 nm. however, gsk-3β inhibitor ii was not able to inhibit another gsk-3 isoform, gsk-3α [1]. another study found that gsk-3β inhibitor ii could block the functional regulation of p53 through inhibiting gsk-3β, decreasing mdm2 levels, and modulating mitochondrial p53 apoptotic signaling [2].
IC 50390 nm for gsk-3β
references[1] naerum, l. ,nrskov-lauritsen, l. and olesen, p.h. scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors. bioorg.med.chem.lett. 12(11), 1525-1528 (2002).
[2] watcharasit, p. ,bijur, g.n.,song, l., et al. glycogen synthase kinase-3beta (gsk3beta) binds to and promotes the actions of p53. j.biol.chem. 278(49), 49972-48879 (2003).
2-Thio(3-iodobenzyl)-5-(1-pyridyl)-[1,3,4]-oxadiazole Preparation Products And Raw materials
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