6-Bromoindirubin-3'-oxime

DescriptionBIO 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). 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. 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). BIO is reported to maintain self-renewal in human and mouse ESCs as well as induce the differentiation of neonatal cardiomyocytes.

Uses6-bromoindirubin-3′-oxime (BIO) has been used:in MTT 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) cell proliferation assayas a medium supplement in embryonic stem cells (ESCs)for the inhibition of glycogen synthase kinase 3 β (GSK-3β) in human dermal papilla cells (hDPCs)

General DescriptionA cell-permeable, highly potent, selective, reversible, and ATP-competitive inhibitor of GSK-3α/β (IC50 = 5 nM). Specificity was confirmed using various Cdk′s (IC50 = 83 nM for Cdk5/p25, 300 nM for Cdk2/cyclin A, 320 nM for Cdk1/cyclin B, and 10 μM for Cdk4/cyclin D1), MAP kinases, PKA, PKC isoforms, PKG, CK, and IRTK (IC50 ≥ 10 μM). Inhibition of GSK by BIO has been shown to result in the activation of the Wnt signaling pathway and sustained pluripotency of human and murine embryonic stem cells (ESCs).

DefinitionChEBI: 6-bromoindirubin-3'-oxime is a member of the class of biindoles that is indirubin substituted at position 6 by a bromo group and in which the keto group at position 3' has undergone condensation with hydroxylamine to form the corresponding oxime. It has a role as an EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor and an EC 2.7.11.26 (tau-protein kinase) inhibitor. It is a ketoxime, an organobromine compound, a member of oxindoles and a biindole.