| Identification | Back Directory | [Name]
2-THIO(3-IODOBENZYL)-5-(1-PYRIDYL)-[1,3,4]-OXADIAZOLE | [CAS]
478482-75-6 | [Synonyms]
TIBPO
GSK-3 INHIBITOR II
GSK3β Inhibitor II
GSK3.beta. Inhibitor II
GLYCOGEN SYNTHASE KINASE-3 INHIBITOR II
GSK-3β Inhibitor II - CAS 478482-75-6 - Calbiochem
2-THIO(3-IODOBENZYL)-5-(1-PYRIDYL)-[1,3,4]-OXADIAZOLE
4-[5-[[(3-Iodophenyl)methyl]thio]-1,3,4-oxadiazol-2-yl]pyridine
2-[(3-iodophenyl)methylsulfanyl]-5-pyridin-4-yl-1,3,4-oxadiazole
Pyridine, 4-[5-[[(3-iodophenyl)Methyl]thio]-1,3,4-oxadiazol-2-yl]- | [Molecular Formula]
C14H10IN3OS | [MDL Number]
MFCD04974171 | [MOL File]
478482-75-6.mol | [Molecular Weight]
395.22 |
| Chemical Properties | Back Directory | [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 | [pka]
0.97±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Definition]
ChEBI: 2-[(3-iodophenyl)methylthio]-5-pyridin-4-yl-1,3,4-oxadiazole is an aryl sulfide. | [Biological Activity]
gsk-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 vitro]
in 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 50]
390 nm for gsk-3β | [storage]
Store at -20°C | [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). |
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