SC 236 is a selective COX-2 inhibitor with anti-cancer and anti-inflammatory properties. SC 236 exhibited an unacceptably long plasma half-life and this limited its development.

MRT 67307 dihydrochloride is a novel inhibitor of IKK-epsilon/TBK1. Negative regulation on the canonical IKKs may be critical in preventing the overproduction of the inflammatory mediators that lead to inflammatory and autoimmune diseases. In addition, it was demonstrated that MRT 67307 inhibits series of MARKs and salt inducible kinases (SIKs). SIKs prevent the formation of regulatory macrophages and their inhibition induces increasing in some markers of regulatory macrophages, such as IL-10 and other anti-inflammatory molecules. It is an inhibitor for ULK1and ULK2. ULK1, a serine/threonine protein kinase, is essential for the initial stages of autophagy. Cancer cells are thought to take advantage of autophagy to help them to cope with the stress of tumorigenesis; thus targeting autophagy is an attractive therapeutic approach.

Nornidulin is a depsidone produced by several fungal species with potent and selective antibacterial activity. Nornidulin inhibited aromatase with IC50 value of 4.6 uM. Nornidulin suppresses nitric oxide production in RAW 264.7 cells.

Mitraphylline is the major pentacyclic oxindolic alkaloid presented in Uncaria tomentosa. It has traditionally been used to treat disorders including arthritis, heart disease, cancer, and other inflammatory diseases. It is also present in the leaves of the tree Mitragyna speciosa, commonly known as kratom, herb which is traditionally used to treat withdrawal symptoms associated with opiate addiction. However, the specific role and the mechanism of action of mitraphylline is not clear. Current research is focusing on mitraphylline as a new promising anticancer and anti-inflammatory agent. Its antiproliferative and cytotoxic effects and in vivo efficacy to induce apoptosis has been studied in human breast cancer, sarcoma, bladder cancer as well as lymphoblastic leukaemia cell lines. As a new candidate for inflammatory disease therapies mitraphylline has been studied in vitro in LPS-activated human primary neutrophils and Its activity against cytokines involved in inflammation process was tested in a murine model in vivo. In mice mitraphylline inhibited around 50% of the release of interleukins 1α, 1β, 17, and TNF-α. It also reduced about 40% of the production of interleukin 4 (IL-4). Mitraphylline was stable in simulated gastric fluid but unstable in simulated intestinal fluid (13.6 % degradation) and was metabolized by human liver microsomes with half-live of 50 min.

GW-9508 is a small-molecule agonist of the fatty acid receptors GPR40 and GPR120. GW-9508 exerts wide-range activity in animal models: anti-depressant, anti-inflammatory, anti-diabetic and analgetic actions.

Escin Ia and isoescin Ia have been traditionally used clinically as the chief active ingredients of escin, a major triterpene saponin isolated from horse chestnut (Aesculus hippocastanum) seeds for the treatment of chronic venous insufficiency, hemorrhoids, inflammation and edema. The interconversion of escin Ia and isoescin Ia when given alone indicates that administration of one isomer leads to exposure to the other.

Isoorientin is a common C-glycosyl flavone in the human diet. It has been isolated from several plant species, including Phyllostachys pubescens, Crataegus monogyna and Crataegus pentagyna, Patrinia villosa Juss, Drosophyllum lusitanicum, buckwheat, Arum palaestinum, and Rumex and Swertia. Isoorientin possesses significant anti-nociceptive and anti-inflammatory activities. Significantly protected PC12 nerve cells from 6-OHDA-induced apoptotic neurotoxicity and reduced the proliferation of HepG2 cells. Isoorientin showed anti-RSV (respiratory syncytial virus) activity.

BAY 61-3606 is a potent inhibitor of spleen tyrosine kinase (Syk) which is playing essential roles in receptors for Fc portion of immunoglobulins and B cell receptor complex signaling in various inflammatory cells. In addition, BAY61-3606 could inhibit the inhibitor of nuclear factor kappa B kinase (IKK-alpha) kinase activity. The compound is able to inhibit neoplastic phenotype of leukemia cells as well as of colon and breast cancer cells in vitro. BAY 61-3606 also exrets antiinflammatory and antiallergic properties in animal models.

Skimmin is one of the major pharmacologically active compounds found in the traditional Chinese medicinal herb Hydrangea paniculata and H. macrophylla. Skimmin is a glycosylated coumarin and precursor in the biosynthesis of umbelliferone. Skimmin has been identified as a potential anti-inflammatory compound which may be of use in diabetic neuropathies such as membranous glomerulonephritis. It was also identified as a potent anti-amoebic compound found in the root bark of Adina cordifolia, a plant used in East Indian folk medicine.

Evodiamine, a naturally occurring indole alkaloid, is one of the main bioactive ingredients of Evodia Rutaecara, the dried unripe fruit of which is also known as Wu zhu yu (Wu Zhu Yu, interchangeably) or Evodia Fruit. Evodia Fruit used in Traditional Chinese Medicine for the purposes of warmth, intestinal comfort (specifically; to alleviate abdominal pain, acid regurgitation, nausea and diarrhea), dysmenorrheal, and fighting inflammation and infections. With respect to the pharmacological actions of evodiamine, more attention has been paid to beneficial effects in insults involving cancer, obesity, nociception, inflammation, cardiovascular diseases, Alzheimer's disease, infectious diseases and thermo-regulative effects. Evodiamine has evolved a superior ability to bind various proteins including TRPV1, the aryl hydrocarbon receptor (AhR), and topoisomerases I and II. There are currently no human studies on evodia rutaecarpa berries or evodiamine.