Rottlerin is a principal phenolic compound of the Kamala plant Mallotus philippinensis. It is a widely-used selective inhibitor of PKCδ (protein kinase Cδ) (IC50=3-6 μM). It also inhibits PKCα, PKCβ, PKCγ, PKCε, PKCη, PKCζ and eEF2K (CaMK III) (IC50 = 5.3 μM). In HT1080 human fibrosarcoma cells, rottlerin induces apoptosis and autophagy via a PKCδ-independent pathway. When tested on HERG (human Ether-á-go-go) channels, rottlerin increased both step and tail HERG current by leftward shifting the voltage and dependence of HERG activation and slowing channel deactivation. Rottlerin is an inhibitor of Chk2, MAPKAPK-2, Pim-3, PKCλ, PKCθ, Plk, PRAK, SRPK1 and an activator of AMPK and HERG. There have been a number of studies published with evidence against the role of Rotterlin as a specific PKCδ inhibitor.
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See how others have used Rottlerin. Click on the entry to view the PubMed entry .
PMID: # 25827954
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PMID: # 20674954
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Perissi, V. et al. 2008. TBL1 and TBLR1 phosphorylation on regulated gene promoters overcomes dual CtBP and NCoR/SMRT transcriptional repression checkpoints Molecular Cell. 29: 755-766.
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Tapia, JA. et al. 2006. Rottlerin inhibits stimulated enzymatic secretion and several intracellular signaling transduction pathways in pancreatic acinar cells by a non-PKC-delta-dependent mechanism. Biochim. Biophys. Acta. 1763: 25-38.
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