Cat. No. 2253
Chemical Name: 5,6,7,13-Tetrahydro-13-methyl-5-oxo
Biological ActivityPotent 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.
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
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, supplier, Potent, protein, kinases, C, inhibitors, PKC, inhibitor, selective, alpha, beta1, isozymes, Go6976
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April 12 - 15, 2015