10Z-Hymenialdisine (SK&F 108752) ((4Z)-4-(2-Amino-1,5-dihydro-5-oxo-4 H-imidazol-4-ylidene)-2-bromo-4,5,6,7-tetrahydropy rrolo[2,3-c]azepin-8(1H)-one)

Pan kinase inhibitor (IC50 values are 6, 10, 22, 28, 35, 40, 70, 80, 100, 470, 500, 600, 700 and 700nm or MEK-1, GSK-3beta, Cdk1/cyclin B, Cdk5/p25, CK1, Cdk2/cyclin A, Cdk2/cyclin E, ASK-gamma, Cdk3/cyclin E, Erk1, PKCgamma, Cdk4/cyclin D1, Cdk6/cyclin D2 and PKCalpha respectively.) Inhibits NF-kappaB activation and blocks IL-8 production in U937 cells (IC50 values are 1-2 and 0.34-0.48um respectively).\n\nSequence:\nC11H10BrN5O2\n\nSolubility:\nDMSO (~10mM)\n\nMolecular Weight:\n~324.13\n\nStorage and Stability:\nLyophilized powder may be stored at -20 degrees C. Stable for 12 months at -20 degrees C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20 degrees C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.

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SPECIFICATIONS

Catalog Number

145659

Size

500ug

Form

Supplied as a yellow solid.

Purity

~97% (HPLC)

References

1. Breton and Chabot-Fletcher (1997) The natural product hymenialdisine inhibits interleukin-8 production in U937 cells by inhibition of nuclear factor-kB. J.Pharmacol.Exp.Ther. 282:459. PMID: 9223588. 2. Meijer et al (2000) Inhibition of cyclin-dependent kinases, GSK-3b and CK1 by hymenialdisine, a marine sponge constituent. Chem.Biol. 7:51. PMID: 10662688. 3. Tasdemir et al (2002) Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1). J.Med.Chem. 45:529. PMID: 11784156.