Hymenialdisine Analogue 1 is an indole derivative of Hymenialdisine, a potent inhibitor of a variety of kinases including MEK-1, GSK-3B, and CKI. It also exhibits inhibition of the G2 cell cycle checkpoint at the micromolar concentrations. This compound exhibits very potent inhibition of Chk2 activity in the low nanomolar range (IC50=8nM). Exhibits an increased selectivity for the checkpoint kinases over natural Hymenialdisine.
Sharma, V., and Tepe, J.J.: Bioorg. & Medicinal Chem. Letters, 14, 4319 (2004), Sharma, V., et al.: J. Med. Chem., 47, 3700 (2004)