Temozolomide acid is the inactive metabolite of temozolomide. However, it was demonstrated to have small anti-cancer activity in vitro.

The synthetic small molecule TGX-221 is a potent, selective and cell membrane permeable inhibitor of PI3K p110 beta catalytic subunit, which is critical for cell growth, proliferation and tumorigenesis of PTEN-deficient tumor cells including prostate cancers. Therefore, PI3K p110 beta inhibitors have a great promise as novel chemotherapeutic agents to treat PTEN deficient cancer cells. In vivo, TGX-221 significantly improved blood flow in FeCl3-induced arterial thrombosis as well as increased tail and renal bleeding times in mice.

Dihydrorotenone (DHR) is a potent mitochondrial inhibitor and natural pesticide widely used in farming industry. Mechanistic investigations suggested that Dihydrorotenone bound to and inhibited the complex I in the electron transport chain, thus inhibiting mitochondrial function and decreasing ATP production. Inhibition of mitochondrial function and disruption of the energy supply lead to insect death. Although Dihydrorotenone is non-toxic in rats, it induces Parkinsonian syndrome in the long-term treated mice, which suggesting Dihydrorotenone is toxic to neural cells.

AMG-458 is a potent c-Met inhibitor. AMG-458 was found to significantly inhibit tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight. AMG-458 was advanced into preclinical safety studies in cancer in USA.

Tunicamycin V is nucleotide sugar analogs, with a modified fatty acid side-chain, produced by several Streptomyces species. In eukaryotes, Tunicamycin V inhibit transfer of N-acetylglucosamine to a lipid intermediate. A few studies suggest that tunicamycin may work as a therapeutic drug to cancer cells as it has been shown to sensitize human colon and prostate cancer cells to TRAIL-induced apoptosis.

β-Amanitin is an extremely toxic constituent of the mushroom, Amanita phalloides, that inhibits Rpb (eukaryotic RNA polymerase II) and eukaryotic RNA polymerase III. This toxin is synthesized as a proprotein, on ribosomes, 34 to 35 amino acids in length and then cleaved at specific proline residues by an enzyme belonging to the prolyl oligopeptidase (POP) subfamily. β-Amanitin shows remarkable binding affinity for eukaryotic RNA polymerase II, slightly binds to RNA polymerase III, and shows no activity on RNA polymerase I; it has been used to determine which types of RNA polymerase are present in a given sample. The toxin works by binding to the bridging helix of RNA polymerase II inhibiting the translocation of RNA and DNA needed to empty the site for the next round of synthesis; thereby slowing the rate of transcription by over 1000 fold.

Gitoxigenin is a 16β-substituted digitoxigenin which may act as a Na+/K+-ATPase inhibitor. Cardiac glycosides (CGs), inhibitors of Na+/K+-ATPase (NKA), used clinically to treat heart failure, have garnered recent attention as potential anti-cancer and anti-viral agents. A high-throughput phenotypic screen designed to identify modulators of promyelocytic leukemia protein (PML) nuclear body (NB) formation revealed the CG gitoxigenin as a potent activator of PML.

Digitoxigenin is a cardenolide and aglycone constituent of digitoxin, an extract from the foxglove plant, D. purpurea. It elicits cardiac contraction and cardiotonic effects by inhibiting the Na+/K+ ATPase via binding at the digitalis receptor site with nanomolar potency. Digitoxigenin is highly cytotoxic, inhibiting Na+/K+ ATPase-dependent protein synthesis, and has been examined for use as an antitumor compound.

GNE-493 is a potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitor for the treatment of cancer.

GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor. GNE-477 exhibited stasis in a PC3 tumor growth inhibition study.