Gö 6976An inhibitor of certain forms of PKC, Trks, and JAKs

Gö 6976 (CAS 136194-77-9)

Gandouml 6976, CAS 136194-77-9 is rated 5.0 out of 5 by 1.
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Synonym: 12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole
Application: An inhibitor of certain forms of PKC, Trks, and JAKs
CAS Number: 136194-77-9
Purity: ≥99%
Molecular Weight: 378.43
Molecular Formula: C24H18N4O
* Refer to Certificate of Analysis for lot specific data (including water content).
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Gö 6976 is a very potent PKC (protein kinase C ) inhibitor with high selectivity for the PKC isotypes α and β. Inhibits PKCα (IC50=2.3nM) and PKCβ1 (IC50=6.2nM) but has no effect on δ, ε or γ isotypes. Potent antagonist of HIV-1 induction. Gö 6976 is an inhibitor of JAK2, Trk A and Trk B.


References

1. Qatsha, K A., et al., 1993. Gö 6976, a selective inhibitor of protein kinase C, is a potent antagonist of human immunodeficiency virus 1 induction from latent/low-level-producing reservoir cells in vitro. Proceedings of the National Academy of Sciences of the United States of America. 90(10): 4674-8. PMID: 7685108
2. Wenzel-Seifert, K., et al., 1994. N-protein kinase C isoenzymes may be involved in the regulation of various neutrophil functions. Biochemical and biophysical research communications. 200(3): 1536-43. PMID: 8185608
3. Martiny-Baron, G., et al., 1993. Selective inhibition of protein kinase C isozymes by the indolocarbazole Gö 6976. The Journal of biological chemistry. 268(13): 9194-7. PMID: 8486620
4. Gschwendt, M., et al., 1996. Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. FEBS letters. 392(2): 77-80. PMID: 8772178

Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/ml), and water (partly).
Storage :
Store at -20° C
Melting Point :
279.02° C (Predicted)
Boiling Point :
652.31° C at 760 mmHg (Predicted)
Density :
1.42 g/cm3 (Predicted)
Refractive Index :
n20D 1.77 (Predicted)
IC50 :
PKCγ: IC50 = 2 nM (human); PKCα : IC50 = 2.3 nM; TrkA: IC50 = 5 nM; PKCβ1: IC50 = 6.2 nM; PKC: IC50 = 7.9 nM
Ki Data :
JAK3: Ki= 0.63 nM (human); Rsk-2: Ki= 2.51 nM (human); Tyk 2: Ki= 3.16 nM (human); IRAK-4: Ki= 12.59 nM (human); ARK-2: Ki= 12.59 nM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
3501
MDL Number :
MFCD00236434
Beilstein Registry :
8588138
SMILES :
CN1C2=CC=CC=C2C3=C4C(=C5C6=CC=CC=C6N(C5=C31)CCC#N)CNC4=O

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Certificate of Analysis

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Gö 6976  Product Citations

See how others have used Gö 6976. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 27543462  Sulen, A. et al. 2016. Pharmacol. Res. 113: 216-227.

PMID: # 27619995  Wu, Y. et al. 2016. J. Immunol.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Robinson Robinson, KA. Et al. (PubMed 25330241) found that G 6976, an inhibitor of certain forms of PKC, Trks, and JAKs, reverses hyperglycemia-induced insulin resistance independently of cPKC inhibition in adipocytes. -SCBT Publication Review
Date published: 2015-01-13
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