Go 6976

Cat. No. 2253

Go 6976 C24H18N4O [136194-77-9]

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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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

References

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 citation for this product please let us know.

View Related Products by Target

Keywords: Go 6976, supplier, Potent, protein, kinases, C, inhibitors, PKC, inhibitor, selective, alpha, beta1, isozymes, Go6976

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