BIO

Catalog # Availability Size / Price Qty
3194/10
3194/50
BIO | CAS No. 667463-62-9 | GSK-3 Inhibitors
1 Image
Description: Potent GSK-3 inhibitor; also inhibits cdks
Alternative Names: 6BIO

Chemical Name: (2'Z,3'E)-6-Bromoindirubin-3'-oxime

Purity: ≥98%

Product Details
Citations (18)
Supplemental Products
Reviews

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

M.Wt:
356.17
Formula:
C16H10BrN3O2
Solubility:
Soluble to 10 mM in DMSO and to 10 mM in ethanol
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
667463-62-9

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

Other Product-Specific Information:

Background References

  1. 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.
  2. GSK3 is a regulator of RAR-mediated differentiation.
    Gupta K, Gulen F, Sun L
    Leukemia, 2012;26(6):1277-85.
  3. 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.
  4. 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.
  5. GSK-3-selective inhibitors derived from tyrian purple indirubins.
    Meijer et al.
    Chem.Biol., 2003;10:1255
  6. 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
  7. The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes.
    Tseng et al.
    Chem.Biol., 2006;13:957
  8. How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
    Jorda et al.
    J.Med.Chem., 2018;61:9105

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Citations for BIO

The citations listed below are publications that use Tocris products. Selected citations for BIO include:

18 Citations: Showing 1 - 10

  1. 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
  2. Trypanosoma cruzi Exploits Wnt Signaling Pathway to Promote Its Intracellular Replication in Macrophages.
    Authors: Volpini Et al.
    Front Immunol  2018;9:859
  3. Myotome adaptability confers developmental robustness to somitic myogenesis in response to fibre number alteration.
    Authors: Roy Et al.
    Dev Biol  2017;431:321
  4. 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
  5. Genomic integration of Wnt/β-catenin and BMP/Smad1 signaling coordinates foregut and hindgut transcriptional programs.
    Authors: Stevens Et al.
    Development  2017;144:1283
  6. Wnt signalling is a bi-directional vulnerability of cancer cells.
    Authors: Duffy Et al.
    Oncotarget  2016;7:60310
  7. 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
  8. 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
  9. 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
  10. Integrated β-catenin, BMP, PTEN, and Notch signalling patterns the nephron.
    Authors: Lindstr&#246;m Et al.
    Nat Chem Biol  2015;3:e04000

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