Go 6976

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Cat.No. 2253 - Go 6976 | C24H18N4O | CAS No. 136194-77-9
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: ≥98% (HPLC)
Datasheet
Citations (14)
Reviews
Literature

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
Storage Desiccate at -20°C
Purity ≥98% (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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 3.78 10

Preparing Stock Solutions

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

Certificate of Analysis / Product Datasheet
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References

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


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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

14 Citations for Go 6976

Citations are publications that use Tocris products. Selected citations for Go 6976 include:

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

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

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

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

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

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

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

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


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