GSK-3β Inhibitor II
Catalogue Number: C4599-APE
| Manufacturer: | Apexbio |
| Molecular Formula: | C14H10IN3OS |
| Physical state: | A crystalline solid |
| Type: | Kinase Inhibitors |
| Alias: | Tip-oxadiazole |
| Shipping Condition: | Blue Ice |
| Unit(s): | 10 mg, 5 mg |
Description
Description: IC50: 390 nM for GSK-3βGSK-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].In vivo: Up to now, there is no animal in vivo data reported.Clinical trial: So far, no clinical study has been conducted.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).
Additional Text
Storage Note
Store at -20°C
Smile String
IC1=CC(CSC2=NN=C(C3=CC=NC=C3)O2)=CC=C1
Solubility
≥15.33 mg/mL in DMSO with ultrasonic; ≥3.78 mg/mL in EtOH with ultrasonic; insoluble in H2O
C4599 CofA
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