Description
Go-6983 (133053-19-7) potent and pan-specific, ATP-competitive protein kinase C inhibitor. PKC isotype IC50s= 7, 7, 6, 10 and 60 nM for PKC α, β, γ, δ, ζ respectively.1 Suppresses stress induced HSP27 disassociation.2 Maintains rat embryonic stem cell pluripotency.3 Attenuates myocardial ischemia/reperfusion injury.4
Uses
Go 6983, is a protein kinase C (PKC) inhibitor.Potent PKC Inhibitor
Definition
ChEBI: 3-[1-[3-(dimethylamino)propyl]-5-methoxy-3-indolyl]-4-(1H-indol-3-yl)pyrrole-2,5-dione is a member of indoles and a member of maleimides.
Biological Activity
Broad spectrum protein kinase C (PKC) inhibitor (IC 50 values are 7, 7, 6, 10, 60 and 20000 nM for PKC α , PKC β , PKC γ , PKC δ , PKC ζ and PKC μ respectively). Displays cardioprotective properties; reduces polymorphonuclear leukocyte adherence and infiltration following myocardial ischemia/reperfusion injury.
Biochem/physiol Actions
Protein kinase C (PKC) inhibitor that selectively inhibits several PKC isozymes (IC50 = 7 nM for PKCα and PKCβ; 6 nM for PKCγ; 10 nM for PKCδ; and 60 nM for PKCζ), but does not inhibit PKCμ (IC50 = 20 mM).
References
1) Gschwendt et al. (1996), Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase C isoenzymes; FEBS Lett., 392 77
2) Kato et al. (2001), Protein kinase inhibitors can suppress stress-induced dissociation of Hsp27; Cell Stress Chaperones, 6 16
3) Rajendran et al. (2013), Inhibition of protein kinase C signaling maintains rat embryonic stem cell pluripotency; J. Biol. Chem., 288 24351
4) Young et al. (2005), Go 6983: a fast acting protein kinase C inhibitor that attenuates myocardial ischemia/reperfusion injury; Cardiovasc, Drug Rev., 23 255
