7BIO

7BIO is a derivative of indirubin (Item No. 14155) that triggers a rapid cell death process that is distinct from apoptosis and devoid of cytochrome c release or caspase activation.¹ Furthermore, in contrast to other indirubin derivatives, 7BIO has only marginal activity against the classic indirubin targets, cyclin-dependent kinases and GSK3.^1,2 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).^1,3 It also inhibits Aurora B and C kinases with IC₅₀ values of 4.6 and 0.7 µM, respectively.^1,4

WARNING This product is not for human or veterinary use.

1. Ribas, J., Bettayeb, K., Ferandin, Y., et al. 7-Bromoindirubin-3'-oxime induces caspase-independent cell death. Oncogene 25(47), 6304-6318 (2006).

2. Ferandin, Y., Bettayeb, K., Kritsanida, M., et al. 3'-Substituted 7-halogenoindirubins, a new class of cell death inducing agents. J. Med. Chem. 49(15), 4638-4649 (2006).

3. Myrianthopoulos, V., Kritsanida, M., Gaboriaud-Kolar, N., et al. Novel inverse binding mode of indirubin derivatives yields improved selectivity for DYRK kinases. ACS Med. Chem. Lett. 4(1), 22-26 (2013).

4. 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. Med. Chem. 50(17), 4027-4037 (2007).