Chemical Name:3'-[(8-Cinnamoyl-5,7-dihydroxy-2,2-dimethyl-2H-1-benzop
yran-6-yl)methyl]-2',4',6'-trihydroxy-5'-methylacetophe
none
Biological Activity:
Originally reported to inhibit PKC isoforms,
with selectivity for PKCδ
(Ki values are 30, 42, 40, 3-6, 100, and 100 μM for α, β, γ, δ, e, l
respectively). Also reported to inhibit CAM kinase III. However, recently shown
to inhibit a wide range of protein kinases, and most potently to inhibit PRAK
and MAPKAP-K2 (IC50 values are 1.9 and 5 μM
respectively). Also shown to act as a direct mitochondrial uncoupler.
Gschwendtet al
(1994) Rottlerin, a novel protein kinase inhibitor. Biochem.Biophys.Res.Comm. 199
93. Wayet al (2000) Identification of
PKC-isoform-specific biological actions using pharmacological approaches. TiPS 21
181. Davies et al (2000) Specificity and mechanism of action of
some commonly used protein kinase inhibitors. Biochem.J. 351 95. Zhang
et al (2007) Neuroprotective effect of protein kinase Cδ inhibitor rottlerin in cell culture
and animal models of Parkinson's disease. J.Pharmacol.Exp.Ther. 322 913.