Ethylisopropylamiloride (5-(N-ethyl-N-isopropyl)-Amiloride, EIPA) is a potent inhibitor of several Sodium-hydrogen exchangers (NHE) isoforms, inhibiting NHE1, NHE2, NHE3, and NHE5, that potentially can be used in cancer treatment. Ethylisopropylamiloride was also demonstrated to inhibit a wide variety of cation channels such as KATP channels) peptide-gated Na+ channels and shrinkage-activated Na+ channels. EIPA is commonly used at a concentration of 5-10 μM to inhibit cellular HNE activity.

2,4-Diacetylphloroglucinol (DAPG) is a secondary metabolite of the P. Fluorescens strain CHAo which inhibits bacteria, fungi, and plants and suppresses pathogens. 2,4-Diacetylphlo roglucinol also displays antiviral activity against DNA and RNA viruses with envelopes. 2,4-Diacetylphloroglucinol exhibited a broad-spectrum of anti-leukemic, anti-lung, and anti-breast cancer properties. The anticancer and antimetastatic activities of DAPG were mediated by the inhibition of ROS, NF-κB, Bcl-2, MMP-2, VEGF and primary inflammatory mediators such as TNF-α, IL-6, IL-1β and NO. The DAPG induced apoptosis in cancer cells by intrinsic and extrinsic pathways via the release of cytochrome-C, upregulation of Bax and the activation of caspases and also, exhibited anti-inflammatory activity by the inhibition of LPS-inflammed cell proliferation of macrophage (Raw 264.7), monocytic cells (THP-1) and peripheral blood mononuclear cells (PBMCs). Results further confirmed that the DAPG inhibited the primary inflammatory mediators in cancer cells and inflammed immune cells through the down regulation of NF-κB.

Brassinolide ((22R,23R,24S)-2a,3a,22,23-tetrahydroxy- 24-methyl-B-homo-7-oxa-5a-cholestan-6-one) is a plant growth hormone that has been implicated in Auxin Signaling. In vitro and field experiments have shown that application of Brassinolide and Brassinolide analogs produces protection against phytopathogens and stress conditions, as well as higher production of biomass, which resulted in an increase in the quality and yield of different crops, such as legumes, cereals, and fruits. Since Brassinolide and its congeners are natural products, and abundant in the vegetable kingdom, they are not excluded from the usual diet of all living organisms, and therefore do not constitute an 'unnatural' additive. These facts make this family of compounds a potential environmental friendly helper to agricultural production. In preclinical experiments, Brassinolide shows marked cytotoxicity to cancer cells via Wnt pathway inhibition. Brassinolide induced a concentration-dependent increase in the apoptotic rate and marked accumulation in the G2/M phase of cell cycle. PC-3 cells treated with brassinolide showed characteristic apoptotic alterations: shrinking cellular figure, decreasing cell surface microvilli, cytoplasmic vacuoles, chromatin condensation. Oral administration of Brassinolide decreased the levels of blood glucose. The levels of blood glucose displayed significant differences after treatment with a different dose of brassinolide. Brassinolide can still reduce the blood glucose levels without toxicity effect even at a lower dose.

Fibronectin tetrapeptide (RGDS peptide) is a key component of the cell attachment domain of fibronectin fibrinogen α, and von Willebrand factor, that interacts with αVβ1 and αVβ3 integrins. The Fibronectin tetrapeptide sequence was found initially to promote the attachment of rat kidney fibroblasts (NRK cells) to fibronectin and synthetic fibronectin peptides coupled to protein-coated plastic. Further investigation indicated that the free Fibronectin tetrapeptide peptide inhibited the attachment of NRK cells to fibronectin-coated substrates. The RGDS sequence has been shown to occur in several other proteins, such as the λ receptor on E. coli and the Sindbis coat protein. RGDS is also a target sequence for spirochete adherence of the syphilis bacterium Treponema pallidum. RGDS has been shown to block fibrinogen-induced aggregation of intact erythrocytes and specific binding of fibrinogen to erythrocyte membranes. The effect of RGDS on transforming growth factor ß1 (TGFß1) mRNA expression and secretion in cultured human mesangial cells have been investigated. RGDS has been utilized in a study of integrin-mediated signal transduction in cultured cells from the sponge Suberites domuncula. RGDS has been demonstrated to mitigate the binding of Mycobacterium tuberculosis to murine alveolar macrophages

Indolactam V is a tumor promoter and a nanomolar agonist of protein kinase C. The compound was shown to induce differentiation of stem cells into pancreatic progenitors through activation of PKC signaling.

Dimorpholinethiuram disulfide is a thiuram derivative which was initially used in the vulcanization of rubber. Later it was shown that dimorpholinethiuram disulfide is an inhibitor of monoglycerol lipase and pyruvate dehydrogenase kinase (PDK). The compound suppresses proliferation of A549 lung cancer cell line in vitro and reduces tumor volume of A549 xenografts in mice.

5-O-Caffeoylshikimic acid is a characteristic phenolic compound mainly found in the Palmae family. 5-O-Caffeoylshikimic acid was isolated from such plants as Vaccinium corymbosum, Livistona chinensis to name a few. The drug demonstrated the antiproliferative activity against different cancer cell lines. 5-O-Caffeoylshikimic acid could promote cancer cell apoptosis and block cancer cell adhesion, invasion and migration by inhibiting transforming growth factor beta 1 (TGF-beta1) signaling pathway.

7-Oxocholesterol (7-Ketocholesterol) is a major oxidation product of cholesterol (oxysterol) found in human atherosclerotic plaque and is more atherogenic than cholesterol in some animal studies. Oxysterols (oxygenated forms of cholesterol) are present at low levels in the circulation and accumulate is plasma and tissues in some pathologies. In atherosclerotic lesions, 7-oxygenated oxysterols, predominantly 7-ketocholesterol, accumulate and have been implicated in the pathology of the disease. There is some in vivo and in vitro evidence that sterol 27-hydroxylase acts on 7-ketocholesterol to initiate its degradation to more polar, water-soluble products. Recent studies indicate an alternative mechanism, in which 7-ketocholesterol is reduced to 7 beta-hydroxycholesterol by 11 beta-hydroxysteroid dehydrogenase type 1. 7-Ketocholesterol can inhibit cholesterol 7 alpha-hydroxylase, the rate-limiting step in bile acid biosynthesis, as well as strongly inhibiting HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis. It has even been suggested that 7-ketocholesterol is formed enzymically as an endogenous regulator of cholesterol biosynthesis. However, when tested as a pharmacological cholesterol-lowering agent, inhibition of HMG-CoA reductase was rapidly overcome and the 7-ketocholesterol metabolised. In vitro, 7-ketocholesterol has wide-ranging and potent effects, most of which have the potential to contribute to atherosclerosis. For example, 7-ketocholesterol can be cytotoxic and can induce apoptosis in vascular cells. These effects, either individually or more likely, in combination, all implicate 7-ketocholesterol in the initiation and development of atherosclerosis, but further work is needed to establish whether or not its role is a direct causal one. 7-Ketocholesterol is the second most abundant oxysterol found in human atherosclerotic plaque, after the enzymically formed 27-hydroxycholesterol (cholest-5-ene-3beta,27-diol). 7-Ketocholesterol differs from cholesterol by a ketone functional group present at the 7-position. It is produced from cholesterol via the epimeric cholesterol 7-hydroperoxides (cholest-5-ene-3beta-ol-7-hydroperoxide) which decompose to the epimeric 7-hydroxycholesterols (cholest-5-ene-3beta,7-diol) and 7-ketocholesterol. 7-Ketocholesterol is a major dietary oxysterol. It has also been widely suggested that 7-ketocholesterol present in atherosclerotic tissue may be derived from the diet. Certainly, 7-ketocholesterol is a major oxysterol found in cholesterol-rich processed foodstuffs. Dietary 7-ketocholesterol is rapidly metabolised by the liver to 7beta-hydroxycholesterol (cholest-5-ene-3beta,7beta-diol), unusual bile acids and perhaps even cholesterol itself. Its conversion to 7beta-hydroxycholesterol is well documented.

ST-638 (alpha-cyano-3-ethoxy-4-hydroxy-5-phenyl-methylcinnamamide) is a protein tyrosine kinase inhibitor that also inhibits HGF-induced MAP kinase activation in hepatocytes. ST638 has also shown to inhibit PC-PLD (phospholipase D) activity in human neutrophils and suppresses tyrosine phosphorylation induced by tumor necrosis factor-α and phorbol myristate acetate in neutrophils and by angiotensin II in cardiac fibroblasts.

1,4-naphthoquinone is a chemical studied as a potential inhibitor of monoamine oxidase and DNA topoisomerase activities as well as acetyltransferase activity. 1,4-Naphthoquinone is a potent inhibitor of human cancer cell growth and angiogenesis.