"目录号: HY-13689

EpigeneticsTGF-beta/Smad-

Go 6983 是一种有效的的PKC抑制剂，能够作用于PKCα，PKCβ，PKCγ，PKCδ和PKCζ，IC50值分别为 7 nM，7 nM，6 nM，10 nM 和 60 nM。

PKC

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生物活性

Description

Go 6983 is a pan-PKC inhibitor against forPKCα,PKCβ,PKCγ,PKCδandPKCζwithIC50of 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 IC50of 20 μM, and the pther PKC isoenzymes can be suppressed by Go 6983 with IC50values 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].

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.