Chemical Name: (2'Z,3'E)-6-Bromoindirubin-3'-oxime
Biological ActivityBIO is a potent ATP-competitive glycogen synthase kinase-3 (GSK-3) inhibitor (IC50 = 5 nM). Also inhibits cyclin-dependent kinases (cdks; IC50 values are <100 nM for cdk2 and 5 and sub micromolar for cdk1, cdk4 and cdk9). Maintains self-renewal and pluripotency in embryonic stem cells via activation of the Wnt signaling pathway in vitro; also promotes proliferation and dedifferentiation in cardiomyocytes.
Negative Control also available.
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GSK-3-selective inhibitors derived from tyrian purple indirubins.
Meijer et al.
Structural basis for the synthesis of indirubins as potent and selective inhibtors of glycogen synthase kinase-3 and cyclin dependent kinases.
Polychronopoulos et al.
The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes.
Tseng et al.
How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
Citations for BIO
The citations listed below are publications that use Tocris products. Selected citations for BIO include:
18 Citations: Showing 1 - 10
Nemo-like Kinase Drives Foxp3 Stability and Is Critical for Maintenance of Immune Tolerance by Regulatory T Cells.
Authors: Fleskens Et al.
Cell Rep 2019;26:3600
Trypanosoma cruzi Exploits Wnt Signaling Pathway to Promote Its Intracellular Replication in Macrophages.
Authors: Volpini Et al.
Front Immunol 2018;9:859
Myotome adaptability confers developmental robustness to somitic myogenesis in response to fibre number alteration.
Authors: Roy Et al.
Dev Biol 2017;431:321
TIAM1 Antagonizes TAZ/YAP Both in the Destruction Complex in the Cytoplasm and in the Nucleus to Inhibit Invasion of Intestinal Epithelial Cells.
Authors: Diamantopoulou Et al.
Cancer Cell 2017;31:621
Genomic integration of Wnt/β-catenin and BMP/Smad1 signaling coordinates foregut and hindgut transcriptional programs.
Authors: Stevens Et al.
Wnt signalling is a bi-directional vulnerability of cancer cells.
Authors: Duffy Et al.
A High-content screen identifies compounds promoting the neuronal differentiation and the midbrain DA neuron specification of human neural progenitor cells.
Authors: Rhim Et al.
A novel GSK3-regulated APC:Axin interaction regulates Wnt signaling by driving a catalytic cycle of efficient βcatenin destruction.
Authors: Pronobis Et al.
Rescue of an in vitro neuron phenotype identified in Niemann-Pick disease, type C1 induced pluripotent stem cell-derived neurons by modulating the WNT pathway and calcium signaling.
Authors: Efthymiou Et al.
Integrated β-catenin, BMP, PTEN, and Notch signalling patterns the nephron.
Authors: Lindström Et al.
Nat Chem Biol 2015;3:e04000
GSK3 inhibitors stabilize Wee1 and reduce cerebellar granule cell progenitor proliferation.
Authors: Penas Et al.
Nat Commun 2015;14:417
GSK3β-Dzip1-Rab8 cascade regulates ciliogenesis after mitosis.
Authors: Zhang Et al.
PLoS Biol 2015;13:e1002129
GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors.
Authors: Thorne Et al.
Stem Cells Transl Med 2015;11:58
Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors.
Authors: Naujok Et al.
BMC Res Notes 2014;7:273
Tissue-specific derepression of TCF/LEF controls the activity of the Wnt/β-catenin pathway.
Authors: Lu Et al.
Sci Rep 2014;5:5368
PAK-dependent STAT5 serine phosphorylation is required for BCR-ABL-induced leukemogenesis.
Authors: Berger Et al.
Cell Cycle 2014;28:629
GSK3 inhibitors regulate MYCN mRNA levels and reduce neuroblastoma cell viability through multiple mechanisms, including p53 and Wnt signaling.
Authors: Duffy Et al.
Mol Cancer Ther 2014;13:454
Slug and Sox9 cooperatively determine the mammary stem cell state.
Authors: Guo Et al.
World J Gastroenterol 2012;148:1015
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