BIO
Chemical Name: (2'Z,3'E)-6-Bromoindirubin-3'-oxime
Purity: ≥98%
Biological Activity
BIO 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.
Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Beta-catenin patterns the cell cycle during maternal-to-zygotic transition in urochordate embryos.
Dumollard R, Hebras C, Besnardeau L, McDougall A
Dev Biol, 2013;384(2):331-42. -
GSK3 is a regulator of RAR-mediated differentiation.
Gupta K, Gulen F, Sun L
Leukemia, 2012;26(6):1277-85. -
Integrated beta-catenin, BMP, PTEN, and Notch signalling patterns the nephron.
Lindstrom N, Lawrence M, Burn S, Johansson J, Bakker E, Ridgway R, Chang C, Karolak M, Oxburgh L, Headon D, Sansom O, Smits R, Davies J, Hohenstein P
Elife, 2015;3(0):e04000. -
Prostaglandin E2 promotes survival of naive UCB T cells via the Wnt/beta-catenin pathway and alters immune reconstitution after UCBT.
Li L, Kim H, Nellore A, Patsoukis N, Petkova V, McDonough S, Politikos I, Nikiforow S, Soiffer R, Antin J, Ballen K, Cutler C, Ritz J, Boussiotis V
Blood Cancer J, 2014;4(0):e178. -
GSK-3-selective inhibitors derived from tyrian purple indirubins.
Meijer et al.
Chem.Biol., 2003;10:1255 -
Structural basis for the synthesis of indirubins as potent and selective inhibtors of glycogen synthase kinase-3 and cyclin dependent kinases.
Polychronopoulos et al.
J.Med.Chem., 2004;47:935 -
The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes.
Tseng et al.
Chem.Biol., 2006;13:957 -
How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
J.Med.Chem., 2018;61:9105
Product Datasheets
Citations for BIO
The citations listed below are publications that use Tocris products. Selected citations for BIO include:
18 Citations: Showing 1 - 10
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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
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Trypanosoma cruzi Exploits Wnt Signaling Pathway to Promote Its Intracellular Replication in Macrophages.
Authors: Volpini Et al.
Front Immunol 2018;9:859
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Myotome adaptability confers developmental robustness to somitic myogenesis in response to fibre number alteration.
Authors: Roy Et al.
Dev Biol 2017;431:321
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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
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Genomic integration of Wnt/β-catenin and BMP/Smad1 signaling coordinates foregut and hindgut transcriptional programs.
Authors: Stevens Et al.
Development 2017;144:1283
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Wnt signalling is a bi-directional vulnerability of cancer cells.
Authors: Duffy Et al.
Oncotarget 2016;7:60310
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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.
Elife 2015;5:16237
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A novel GSK3-regulated APC:Axin interaction regulates Wnt signaling by driving a catalytic cycle of efficient βcatenin destruction.
Authors: Pronobis Et al.
Cell 2015;4:e08022
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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.
Elife 2015;4:230
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Integrated β-catenin, BMP, PTEN, and Notch signalling patterns the nephron.
Authors: Lindström Et al.
Nat Chem Biol 2015;3:e04000
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GSK3 inhibitors stabilize Wee1 and reduce cerebellar granule cell progenitor proliferation.
Authors: Penas Et al.
Nat Commun 2015;14:417
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GSK3β-Dzip1-Rab8 cascade regulates ciliogenesis after mitosis.
Authors: Zhang Et al.
PLoS Biol 2015;13:e1002129
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GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors.
Authors: Thorne Et al.
Stem Cells Transl Med 2015;11:58
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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
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Tissue-specific derepression of TCF/LEF controls the activity of the Wnt/β-catenin pathway.
Authors: Lu Et al.
Sci Rep 2014;5:5368
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PAK-dependent STAT5 serine phosphorylation is required for BCR-ABL-induced leukemogenesis.
Authors: Berger Et al.
Cell Cycle 2014;28:629
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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
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Slug and Sox9 cooperatively determine the mammary stem cell state.
Authors: Guo Et al.
World J Gastroenterol 2012;148:1015
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