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Characteristics
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Isolated from sponge Axinella carteri. A potent inhibitor of mitogen-activated protein kinase kinase-1 (MEK-1) (IC50 = 6nM). Blocks the in vivo phosphorylation of the microtubule-binding protein tau at sites that are hyperphosphorylated by glycogen synthase kinase-beta (GSK-3beta) and CDK5/p35 in Alzheimer,'s disease. Inhibitor of DNA damage checkpoint at G2 phase(IC50 = 6 µM),cyclin-dependent kinasesCDK1/cyclin B (IC50 = 22 nM),CDK2/cyclin A (IC50= 70 nM), CDK2/cyclin E(IC50= 40 nM), CDK4/cyclin D1 (IC50 = 600 nM), CDK5/p25 (IC50 = 28 nM),GSK-3beta (IC50 = 10 nM),andcasein kinase 1(CK1) (IC50 = 35 nM).
Synonyms: 4-(2-Amino-4-oxo-2-imidazolidin-5-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one, Hymenialdisine
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