Go_6983_DataSheet_MedChemExpress

Inhibitors, Agonists, Screening Libraries

https://www.wendangku.net/doc/4613271427.html, Data Sheet

BIOLOGICAL ACTIVITY:

Go 6983 is a pan–PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC 50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM,respectively.

IC50 & Target: IC50: 7 nM (PKCα), 7 nM (PKCβ), 6 nM (PKCγ), 10 nM (PKCδ), 60 nM (PKCζ)

In Vitro: Go 6983 inhibits PKCμ with IC 50 of 20 μM, and the pther PKC isoenzymes can be suppressed by Go 6983 with IC 50 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 100nM) despite inhibiting PMN superoxide release by 99%[3].

PROTOCOL (Extracted from published papers and Only for reference)

Kinase Assay:[1]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 MgCl 2, 10 μg PS, 100 nM TPA, 5 μL of a Sf158 cell extract as a source of recombinant PKCμor 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.

Product Name:

Go 6983Cat. No.:

HY-13689CAS No.:

133053-19-7Molecular Formula:

C 26H 26N 4O 3Molecular Weight:

442.51Target:

PKC; PKC Pathway:

TGF–beta/Smad; Epigenetics Solubility:

DMSO: ≥ 34 mg/mL

Caution: Product has not been fully validated for medical applications. For research use only.

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