Catalog Number: 2253
Chemical Name: 5,6,7,13-Tetrahydro-13-methyl-5-oxo-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-12-propanenitrile
Biological Activity
Potent protein kinase C (PKC) inhibitor (IC50 = 7.9 nM). Discriminates between Ca2+-dependent and -independent isoforms of PKC in vitro; selectively inhibits PKCα and PKCβ1 (IC50 values are 2.3 and 6.2 nM respectively). Does not inhibit the activity of PKCδ, -ε, or -ζ (IC50 > 3μM). Also inhibits TrkA, TrkB, JAK2 and JAK3 tyrosine kinases (IC50 values are 5, 30, 130 and 370 nM respectively), PKCμ (PKD1) and the mitotic spindle checkpoint.
Technical Data
  • M.Wt:
    378.43
  • Formula:
    C24H18N4O
  • Solubility:
    Soluble to 10 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at -20°C
  • CAS No:
    136194-77-9
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Pharmacologic abrogation of the mitotic spindle checkpoint by an indolocarbazole discovered by cellular screening efficiently kills cancer cells.
    Stolz A, Vogel C, Schneider V et al.
    Cancer Res
  2. Selective inhibition of protein kinase C isozymes by the indolocarbazole G� 6976
    Martiny-Baron et al.
    J.Biol.Chem., 1993;268:9194
  3. Immunological demonstration of protein kinase Cμ in murine tissues and various cell lines.
    Rennecke et al.
    Eur.J.Biochem., 1996;242:428
  4. Go 6976 is a potent inhibitor of neurotrophin-receptor intrinsic tyrosine kinase.
    Behrens et al.
    J.Neurochem., 1999;72:919
  5. Go6976 is a potent inhibitor of JAK2 and FLT3 tyrosine kinases with significant activity in primary acute myeloid leukaemia cells.
    Grandage et al.
    Br.J.Haematol., 2006;135:303
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Go 6976 include:

8 Citations: Showing 1 - 8
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  1. P53-dependent upregulation of neutral sphingomyelinase-2: role in doxorubicin-induced growth arrest.
    Authors: Shamseddine Et al.
    Cell Death Dis 2015;6:e1947
  2. Inhibition of protein kinase C by isojacareubin suppresses hepatocellular carcinoma metastasis and induces apoptosis in vitro and in vivo.
    Authors: Yuan Et al.
    Sci Rep 2015;5:12889
  3. Targeting a cell state common to triple-negative breast cancers.
    Authors: Muellner Et al.
    J Biol Chem 2015;11:789
  4. Systematic analysis of bacterial effector-postsynaptic density 95/disc large/zonula occludens-1 (PDZ) domain interactions demonstrates Shigella OspE protein promotes protein kinase C activation via PDLIM proteins.
    Authors: Yi Et al.
    J Neurosci 2014;289:30101
  5. A ROCK Inhibitor Blocks the Inhibitory Effect of Chondroitin Sulfate Proteoglycan on Morphological Changes of Mesenchymal Stromal/Stem Cells into Neuron-Like Cells.
    Authors: Lim and Joe
    PLoS Biol 2013;21:447
  6. Raf kinase inhibitory protein is required for cerebellar long-term synaptic depression by mediating PKC-dependent MAPK activation.
    Authors: Yamamoto Et al.
    Biomol Ther (Seoul) 2012;32:14254
  7. Identification of small molecule inhibitors of phosphatidylinositol 3-kinase and autophagy.
    Authors: Farkas Et al.
    J Biol Chem 2011;286:38904
  8. Facilitation of long-term potentiation by muscarinic M(1) receptors is mediated by inhibition of SK channels.
    Authors: Buchanan Et al.
    Neuron 2010;68:948

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