Catalog Number: 1532
Alternate Names: SK&F 108752
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
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
  • M.Wt:
    324.13
  • Formula:
    C11H10BrN5O2
  • Solubility:
    Soluble to 10 mM in DMSO
  • Purity:
    >97%
  • Storage:
    Store at -20°C
  • CAS No:
    82005-12-7
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. 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
  2. Inhibition of cyclin-dependent kinases, GSK-3β and CK1 by hymenialdisine, a marine sponge constituent.
    Meijer et al.
    Chem.Biol., 2000;7:51
  3. 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

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