An inhibitor of GSK-3beta and cyclin-dependent kinases
Form:
Free Base
Research Area:
Cancer
REVIEW Indirubin, also known as isoindigotin, is an inhibitor of cyclin-dependent kinases (CDK1/cyclin B (IC50 = 10µM), CDK2/cyclin A (IC50 = 2.2µM), CDK2/cyclin E (IC50 = 7.5µM), CDK4/cyclin D1 (IC50 = 12µM), CDK5/p35 (IC50 = 5.5µM)) and of GSK-3beta (IC50 = 600nM). Studies investigating functional isoindigos show that they have the ability to disrupt cell growth and proliferation. The compound is a potent aryl hydrocarbon receptor ligand and is found in human urine and fetal bovine serum. Synthesized isoindigo-based oligothiophenes are used to study heterojunction solar cells.
REFERENCES
[1]
Wu, K M., et al., 1985. [Potential antileukemic agents, synthesis of derivatives of indirubin, indigo, and isoindigotin]. Yao xue xue bao = Acta pharmaceutica Sinica. 20(11): 821-6. PMID: 3869774
[2]
Leclerc, S., et al., 2001. Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors? The Journal of biological chemistry. 276(1): 251-60. PMID: 11013232
[3]
Adachi, J., et al., 2001. Indirubin and indigo are potent aryl hydrocarbon receptor ligands present in human urine. The Journal of biological chemistry. 276(34): 31475-8. PMID: 11425848
[4]
Wee, Xi Kai., et al., 2009. Synthesis and evaluation of functionalized isoindigos as antiproliferative agents. Bioorganic & medicinal chemistry. 17(21): 7562-71. PMID: 19783149
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