Rottlerin

Mitochondrial uncoupler that depolarizes the mitochondrial membrane potential, reduces cellular ATP levels, activates 5‘-AMP-activated protein kinase (AMPK) and affects mitochondrial production of reactive oxygen species (ROS). Potent activator of multiple Ca²⁺-sensitive K⁺ channels. Blocks several kinases and non-kinase proteins in vitro. Has been widely-used as a selective inhibitor of protein kinase Cδ (PKCδ) (IC₅₀=3-6µM). Although there is extensive published documentation to support the use of rottlerin as a selective PKCδ inhibitor, there has been some controversy in the literature over this claim. Some of this controversy may arise from the fact that rottlerin is a promiscuous inhibitor and therefore may not always display the same properties as would be expected from a classical 1:1 inhibitor. However, there are studies indicate that rottlerin has no direct effect on PKCδ and that it should not be used to determine the involvement of PKCδ in biological processes. Induces autophagy by inhibition of mTORC1 signaling.