| Identification | Back Directory | [Name]
GO 6976 | [CAS]
136194-77-9 | [Synonyms]
G6976
GO 6976
GOE 6976
PD406976
Aids044729
Aids-044729
GO 6976 USP/EP/BP
InSolution? G? 6976
InSolution G 6976 - CAS 136194-77-9 - Calbiochem
5,6,7,13-Tetrahydro-13-methyl-5-oxo-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-12-propanenitrile
12-(2-CYANOETHYL)-6,7,12,13-TETRAHYDRO-13-METHYL-5-OXO-5H-INDOLO(2,3-A)PYRROLO(3,4-C)-CARBAZOLE
12-2(2-CYANOETHYL)-6,7,12,13-TETRAHYDRO-13-METHYL-5-OXO-5H-INDOLO[2,3-A]PYRROLO[3,4-C]CARBAZOLE
12H-Indolo[2,3-A]pyrrolo[3,4-C]carbazole-12-propanenitrile, 5,6,7,13-tetrahydro-13-methyl-5-oxo-
Go6976,5,6,7,13-Tetrahydro-13-Methyl-5-oxo-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-12-propanenitrile
Go 6976, 12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C24H18N4O | [MDL Number]
MFCD00236434 | [MOL File]
136194-77-9.mol | [Molecular Weight]
378.43 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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]
Store at -20°C,protect from light | [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. |
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