Description
7BIO is a derivative of indirubin that triggers a rapid cell death process that is distinct from apoptosis and devoid of cytochrome c release or caspase activation. Furthermore, in contrast to other indirubin derivatives, 7BIO has only marginal activity against the classic indirubin targets, cyclin-dependent kinases and GSK3. Instead, 7BIO inhibits FLT3 (IC50 = 0.34 μM) and the dual-specificity tyrosine phosphorylation-regulated kinases, DYRK1A and DYRK2 (IC50s = 1.9 and 1.3 μM, respectively). It also inhibits Aurora B and C kinases with IC50 values of 4.6 and 0.7 μM, respectively.
References
[1] ribas j, bettayeb k, ferandin y, et al. 7-bromoindirubin-3′-oxime induces caspase-independent cell death[j]. oncogene, 2006, 25(47): 6304-6318.
[2] myrianthopoulos v, kritsanida m, gaboriaud-kolar n, et al. novel inverse binding mode of indirubin derivatives yields improved selectivity for dyrk kinases[j]. acs medicinal chemistry letters, 2012, 4(1): 22-26.
[3] myrianthopoulos v, magiatis p, ferandin y, et al. an integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases b and c by a series of 7-substituted indirubins[j]. journal of medicinal chemistry, 2007, 50(17): 4027-4037.
