Go 6983

Names

[ Name ]:
Go 6983

[Synonym ]:
3-{1-[3-(Dimethylamino)propyl]-5-methoxy-1H-indol-3-yl}-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
3-[1-[3-(Dimethylamino)propyl]-5-methoxy-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
2-(1-(3-dimethylaminopropyl)-5-methoxyindol-3-yl)-3-(1H-indol-3-yl)maleimide
go 6983
1H-Pyrrole-2,5-dione, 3-[1-[3-(dimethylamino)propyl]-5-methoxy-1H-indol-3-yl]-4-(1H-indol-3-yl)-

Biological Activity

[Description]:

Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC

Signaling Pathways >> TGF-beta/Smad >> PKC

Research Areas >> Cancer

[Target]

PKCγ:6 nM (IC50)

PKCα:7 nM (IC50)

PKCβ:7 nM (IC50)

PKCδ:10 nM (IC50)

PKCζ:60 nM (IC50)

PKCμ:20000 nM (IC50)

[In Vitro]

Go 6983 inhibits PKCμ with IC50 of 20 μM, and the pther PKC isoenzymes can be suppressed by Go 6983 with IC50 values from 7 to 60 nM[1]. Go 6983 (100 nM) significantly reduces PMN adherence to the endothelium and infiltration into the myocardium compared with I/R + PMN hearts, and significantly inhibits superoxide release from PMNs by 90 +/- 2% in rat hearts[2]. Go 6983 (200 nM) has a reduced cardioprotective effect compared with the cardioprotective Go 6983 concentrations (50 and 100 nM) despite inhibiting PMN superoxide release by 99%[3].

[Kinase Assay]

Phosphorylation reactions are carried out in a total volume of 100 μL, containing buffer C (50 mM Tris-HCl, pH 7.5, 10 mM β-mercaptoethanol), 4 mM MgCl2, 10 μg PS, 100 nM TPA, 5 μL of a Sf158 cell extract as a source of recombinant PKCμ or of Sf9 cell extracts as a source of other recombinant PKC isoenzymes, 10 μg of syntide 2 as substrate, and 35 μM ATP containing 1 μCi [γ-32P]ATP. In some experiments, PS and TPA are omitted or various inhibitors at concentrations indicated in the text are added. After incubation for 10 min at 30°C, the reaction is terminated by transferring 50 μL of the assay mixture onto a 20 mm square piece of phosphocellulose paper, which is washed 3 times in deionized water and twice in acetone. The radioactivity on each paper is determined by liquid scintillation counting.

[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), 77-80.

[2]. Peterman EE, et al. G0 6983 exerts cardioprotective effects in myocardial ischemia/reperfusion. J Cardiovasc Pharmacol, 2004, 43(5), 645-656.

[3]. Young LH, et al. G0 6983: a fast acting protein kinase C inhibitor that attenuates myocardial ischemia/reperfusion injury. Cardiovasc Drug Rev, 2005, 23(3), 255-272.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
709.0±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₆H₂₆N₄O₃

[ Molecular Weight ]:
442.510

[ Flash Point ]:
382.6±32.9 °C

[ Exact Mass ]:
442.200500

[ PSA ]:
79.36000

[ LogP ]:
3.80

[ Appearance of Characters ]:
red

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.670

[ Storage condition ]:
−20°C

[ Water Solubility ]:
DMSO: 20 mg/mL, clear, red

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi

[ Risk Phrases ]:
36/37/38

[ Safety Phrases ]:
26-36

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

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