10Z-Hymenialdisine
Chemical Name: (4Z)-4-(2-Amino-1,5-dihydro-5-oxo-4H-imidazol-4-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8(1H)-one
Purity: ≥97%
Biological Activity
Pan kinase inhibitor (IC50 values are 6, 10, 22, 28, 35, 40, 70, 80, 100, 470, 500, 600, 700 and 700 nM for MEK1, GSK-3β, Cdk1/cyclin B, Cdk5/p25, CK1, Cdk2/cyclin A, Cdk2/cyclin E, ASK-γ, Cdk3/cyclin E, Erk1, PKCγ, Cdk4/cyclin D1, Cdk6/cyclin D2 and PKCα respectively.) Inhibits NF-κB activation and blocks IL-8 production in U937 cells (IC50 values are 1-2 and 0.34-0.48 μM respectively).Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1).
Tasdemir et al.
J.Med.Chem., 2002;45:529 -
How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
J.Med.Chem., 2018;61:9105 -
Inhibition of cyclin-dependent kinases, GSK-3β and CK1 by hymenialdisine, a marine sponge constituent.
Meijer et al.
Chem.Biol., 2000;7:51 -
The natural product hymenialdisine inhibits interleukin-8 production in U937 cells by inhibition of nuclear factor-κB.
Breton and Chabot-Fletcher
J.Pharmacol.Exp.Ther., 1997;282:459
Product Datasheets
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