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Submit ReviewGo 6976
Description: Potent protein kinase C inhibitor; selective for α and β isozymes
Chemical Name: 5,6,7,13-Tetrahydro-13-methyl-5-oxo-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-12-propanenitrile
Purity: ≥95% (HPLC)
Biological Activity for Go 6976
Go 6976 is a 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 for Go 6976
| M. Wt | 378.43 |
| Formula | C24H18N4O |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 136194-77-9 |
| PubChem ID | 3501 |
| InChI Key | VWVYILCFSYNJHF-UHFFFAOYSA-N |
| Smiles | O=C(NC3)C1=C3C(C4=CC=CC=C4N5CCC#N)=C5C2=C1C6=C(C=CC=C6)N2C |
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.
Solubility Data for Go 6976
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.78 | 10 |
Preparing Stock Solutions for Go 6976
The following data is based on the product molecular weight 378.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 26.42 mL | 132.12 mL | 264.25 mL |
| 0.5 mM | 5.28 mL | 26.42 mL | 52.85 mL |
| 1 mM | 2.64 mL | 13.21 mL | 26.42 mL |
| 5 mM | 0.53 mL | 2.64 mL | 5.28 mL |
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Product Datasheets for Go 6976
References for Go 6976
References are publications that support the biological activity of the product.
Martiny-Baron et al (1993) Selective inhibition of protein kinase C isozymes by the indolocarbazole Gö 6976 J.Biol.Chem. 268 9194 PMID: 8486620
Rennecke et al (1996) Immunological demonstration of protein kinase Cμ in murine tissues and various cell lines. Eur.J.Biochem. 242 428 PMID: 8973662
Behrens et al (1999) Go 6976 is a potent inhibitor of neurotrophin-receptor intrinsic tyrosine kinase. J.Neurochem. 72 919 PMID: 10037462
Grandage et al (2006) Go6976 is a potent inhibitor of JAK2 and FLT3 tyrosine kinases with significant activity in primary acute myeloid leukaemia cells. Br.J.Haematol. 135 303 PMID: 16956345
Stolz et al (2009) Pharmacologic abrogation of the mitotic spindle checkpoint by an indolocarbazole discovered by cellular screening efficiently kills cancer cells. Cancer Res. 69 3874 PMID: 19366805
If you know of a relevant reference for Go 6976, please let us know.
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Keywords: Go 6976, Go 6976 supplier, Potent, protein, kinases, C, inhibitors, inhibits, PKC, inhibitor, selective, alpha, beta1, isozymes, Go6976, Protein, Kinase, 2253, Tocris Bioscience
16 Citations for Go 6976
Citations are publications that use Tocris products. Selected citations for Go 6976 include:
Buckles et al (2020) Rapid exposure of macrophages to drugs resolves four classes of effects on the leading edge sensory pseudopod: Non-perturbing, adaptive, disruptive, and activating PLoS One 15 PMID: 32469878
Shamseddine et al (2015) P53-dependent upregulation of neutral sphingomyelinase-2: role in doxorubicin-induced growth arrest. Cell Death Dis 6 e1947 PMID: 26512957
Yuan et al (2015) Inhibition of protein kinase C by isojacareubin suppresses hepatocellular carcinoma metastasis and induces apoptosis in vitro and in vivo. Sci Rep 5 12889 PMID: 26245668
Yi et al (2014) 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. J Neurosci 289 30101 PMID: 25124035
Farkas et al (2011) Identification of small molecule inhibitors of phosphatidylinositol 3-kinase and autophagy. J Biol Chem 286 38904 PMID: 21930714
Yeganeh et al (2019) Autophagy is required for lung development and morphogenesis. J Clin Invest 130 2904 PMID: 31162135
Lim and Joe (2013) A ROCK Inhibitor Blocks the Inhibitory Effect of Chondroitin Sulfate Proteoglycan on Morphological Changes of Mesenchymal Stromal/Stem Cells into Neuron-Like Cells. PLoS Biol 21 447 PMID: 24404335
Buchanan et al (2010) Facilitation of long-term potentiation by muscarinic M(1) receptors is mediated by inhibition of SK channels. Neuron 68 948 PMID: 21145007
Muellner et al (2015) Targeting a cell state common to triple-negative breast cancers. J Biol Chem 11 789 PMID: 25699542
Yamamoto et al (2012) Raf kinase inhibitory protein is required for cerebellar long-term synaptic depression by mediating PKC-dependent MAPK activation. Biomol Ther (Seoul) 32 14254 PMID: 23055494
Schneberger et al (2018) Organic barn dust inhibits surfactant protein D production through protein kinase-c alpha dependent increase of GPR116. PLoS One 13 e0208597 PMID: 30543664
Lewis and Golsteyn (2016) Cancer cells that survive checkpoint adaptation contain micronuclei that harbor damaged DNA. Cell Cycle 15 3131 PMID: 27636097
Tam et al (2016) Tyrosine Binding Protein Sites Regulate the Intracellular Trafficking and Processing of Amyloid Precursor Protein through a Novel Lysosome-Directed Pathway. PLoS One 11 e0161445 PMID: 27776132
Shu et al (2014) Orexin-A promotes cell migration in cultured rat astrocytes via Ca2+-dependent PKCα and ERK1/2 signals. PLoS One 9 e95259 PMID: 24748172
Lei et al (2017) PKC-α Triggers EGFR Ubiquitination, Endocytosis and ERK Activation in Podocytes Stimulated with High Glucose. Cell Physiol Biochem 42 281 PMID: 28535513
Zhang et al (2017) Protein kinase D at the Golgi controls NLRP3 inflammasome activation. J Exp Med 214 2671 PMID: 28716882
Do you know of a great paper that uses Go 6976 from Tocris? Please let us know.
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