GO 6976 Chemical Properties

Melting point:

>221°C (dec.)

Boiling point:

652.3±55.0 °C(Predicted)

Density 

1.41±0.1 g/cm3(Predicted)

storage temp. 

Sealed in dry,2-8°C

solubility 

Acetonitrile (Very Slightly, Heated), DMSO (Slightly), Methanol (Very Slightly)

form 

Off-white solid

pka

14.39±0.20(Predicted)

color 

White to Off-White

Safety Information

Safety Statements 

22-24/25

HS Code 

2933998090

GO 6976 Usage And Synthesis

Uses

Go 6976 is a potent FLT3 inihibtor which is been shown to initiate cytotoxicity involving acute leukemia. Also known as a PKC inhibitor, which results into apoptosis and tumor destruction. Cancer therapeutic agent.

Definition

ChEBI: Goe 6976 is an organic heterohexacyclic compound and an indolocarbazole. It has a role as an EC 2.7.11.13 (protein kinase C) inhibitor.

Biological Activity

Potent protein kinase C (PKC) inhibitor (IC 50 = 7.9 nM). In vitro, discriminates between Ca 2+ -dependent and -independent isoforms of PKC; selectively inhibits PKC α and PKC β 1 (IC 50 values are 2.3 and 6.2 nM respectively) but does not inhibit the activity of PKC δ , - ε , or - ζ (IC 50 > 3 μ M). Also inhibits TrkA, TrkB, JAK2 and JAK3 tyrosine kinases (IC 50 values are 5, 30, 130 and 370 nM respectively).

storage

-20°C (desiccate)

References

[1]. gschwendt, m., et al., inhibition of protein kinase c mu by various inhibitors. differentiation from protein kinase c isoenzymes. febs lett, 1996. 392(2): p. 77-80.
[2]. qatsha, k.a., et al., go 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. proc natl acad sci u s a, 1993. 90(10): p. 4674-8.
[3]. joksovic, p.m., et al., mechanisms of inhibition of t-type calcium current in the reticular thalamic neurons by 1-octanol: implication of the protein kinase c pathway. mol pharmacol, 2010. 77(1): p. 87-94.
[4]. taube, e., et al., a novel treatment strategy for egfr mutant nsclc with t790m-mediated acquired resistance. int j cancer, 2012. 131(4): p. 970-9.
[5]. yoshida, a., et al., go6976, a flt3 kinase inhibitor, exerts potent cytotoxic activity against acute leukemia via inhibition of survivin and mcl-1. biochem pharmacol, 2014. 90(1): p. 16-24.

GO 6976(136194-77-9)Related Product Information

• Indole-5-carboxaldehyde
• N-Ethyl-3-carbazolecarboxaldehyde
• 4-AMINOMETHYLINDOLE
• 1-(1-METHYL-1H-INDOL-4-YL)METHYLAMINE 97
• N-(2-CYANOETHYL)PYRROLE
• Indole-4-carboxaldehyde
• 3-Formyl-9H-carbazole
• GO 6976
• 1-Methylindoline-5-carboxaldehyde 97%
• C-(9-ETHYL-9H-CARBAZOL-3-YL)-METHYLAMINE
• 3-METHYLCARBAZOLE
• 1H-INDOLE-5-CARBOXAMIDE, 97%
• 1-ethyl-1H-indole-5-carbaldehyde
• 11,12-Dihydroindolo[2,3-a]carbazole
• (1-METHYL-1H-INDOL-5-YL)METHYLAMINE
• 1-METHYL-1H-INDOLE-4-CARBALDEHYDE
• C-(1H-INDOL-5-YL)-METHYLAMINE
• K-252C