BIO

BIO is a cell-permeable bis-indolo (indirubin) compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of GSK3α/β (IC₅₀ = 5 nM). ^1,2 Its specificity has been tested against various cyclin-dependent kinases (CDKs) (IC₅₀s = 83, 300, 320, and 10,000 nM for Cdk5/p25, Cdk2/A, Cdk1/B, and Cdk4/D₁, respectively). BIO was also tested for its specificity towards many other commonly studied kinases (IC₅₀ ≥10 µM), including MAP kinases, PKA, PKC isoforms, PKG, CK, and IRTK. ^1,2 Inhibition of GSK by BIO has been shown to result in the activation of the Wnt signaling pathway and sustained pluripotency in human and mouse embryonic stem cells (ESCs).³ BIO is reported to maintain self-renewal in human and mouse ESCs as well as induce the differentiation of neonatal cardiomyocytes.⁴

WARNING This product is not for human or veterinary use.

1. Meijer, L., Skaltsounis, A.L., Magiatis, P., et al. GSK-3-selective inhibitors derived from tyrian purple indirubins. Chem. Biol. 10(12), 1255-1266 (2003).

2. Polychronopoulos, P., Magiatis, P., Skaltsounis, A.L., et al. Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. J. Med. Chem. 47(4), 935-946 (2004).

3. Sato, N., Meijer, L., Skaltsounis, L., et al. Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor. Nat. Med. 10(1), 55-63 (2004).

4. Tseng, A.S., Engel, F.B., and Keating, M.T. The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes. Chem. Biol. 13(9), 957-963 (2006).