Safingol, the synthetic L-threo-stereoisomer of endogenous (D-erythro-) sphinganine, is an inhibitor of protein kinase C and sphingosine kinase in vitro, and in some cell types has been implicated in ceramide generation and induction of apoptosis. Safingol inhibits enzymatic activity and 3H-phorbol dibutyrate binding of purified rat brain PKC (IC50 = 37.5 uM and 31uM, respectively). Inhibits human PKCα, the major overexpressed isoenzyme in MCF-7 DOXR cells (IC50 = 40 uM). Safingol enhances the cytotoxic effect of the chemotherapeutic agent Mitomycin C (MMC) in gastric cancer cells by promoting drug-induced apoptosis. Safingol is an inhibitor of SphK (Sphingosine kinase). Safingol has been shown to act synergistically with other chemotherapeutic agents and may potentiate chemotherapy drug-induced apoptosis in vitro and in vivo.

Ro 32-0432 hydrochloride is an orally available cell-permeable selective inhibitor of PKC enzymes. Moreover, Ro 32-0432 inhibits G protein-coupled receptor kinase 5 activity. Ro 32-0432 prevents T cell-driven chronic inflammatory responses in several rat models. Ro 32-0432 inhibits an antigen-driven T-cell-mediated arthritis in vivo. Treatment of rats with Ro 32-0432 in ischemic stroke decreases the ischemic infarction area, neurological symptoms and associated endothelin B receptor upregulation. Ro 32-0432 attenuates the propagation of nicotine dependence and reduce withdrawal signs possibly by G protein-coupled receptor kinase 5 activation-linked mechanisms.

5-eicosenoic acid (C20:1omega15), a cis-unsaturated free fatty acid, plays a significant role in PKC-epsilon activation and potentiation of nicotinic ACh receptor responses.

Myricitrin is a naturally occurring polyphenol hydroxy flavonoid. Myricitrin has a variety of beneficial properties, such as antiviral, antimicrobial, antinociceptive, and anticarcinogenic activities. In particular, myricitrin possesses stronger oxidative resistance and free radical scavenging activity than other flavonol rhamnosides or quercetin. Myricitrin showed antipsychotic-like effects in animal models at doses that did not induce catalepsy or alter locomotor activity, suggesting that myricitrin may be a potential drug treatment for the positive symptoms of schizophrenia.

Safingol, the synthetic L-threo-stereoisomer of endogenous (D-erythro-) sphinganine, is an inhibitor of protein kinase C and sphingosine kinase in vitro, and in some cell types has been implicated in ceramide generation and induction of apoptosis. Safingol inhibits enzymatic activity and 3H-phorbol dibutyrate binding of purified rat brain PKC (IC50 = 37.5 uM and 31uM, respectively). Inhibits human PKCα, the major overexpressed isoenzyme in MCF-7 DOXR cells (IC50 = 40 uM). Safingol enhances the cytotoxic effect of the chemotherapeutic agent Mitomycin C (MMC) in gastric cancer cells by promoting drug-induced apoptosis. Safingol is an inhibitor of SphK (Sphingosine kinase). Safingol has been shown to act synergistically with other chemotherapeutic agents and may potentiate chemotherapy drug-induced apoptosis in vitro and in vivo.