BIO

Описание

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). 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.

Использование

6-bromoindirubin-3′-oxime (BIO) has been used:

• in MTT 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) cell proliferation assay
• as 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)

Общее описание

A 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).

Биологическая активность

Potent and selective, ATP-competitive glycogen synthase kinase-3 (GSK-3) inhibitor (IC 50 values are 5, 83, 300, 320 and > 10 000 nM at GSK-3, CDK5/p25, CDK2/cyclin A, CDK1/cyclin B and other common kinases respectively). Maintains self-renewal and pluripotency in embryonic stem cells via activation of the Wnt signaling pathway in vitro .