Wortmannin is a fungal metabolite that so far has been shown to act as a selective inhibitor of phosphoinositide 3-kinase. Wortmannin inhibits cancer cell growth and has shown activity against mouse and human tumor xenografts in mice. Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.

Canthin-6-one is a natural product isolated from various plant genera and from fungi with potential antitumor activity. It induces cell death, cell cycle arrest and differentiation in human myeloid leukemia cells. Canthin-6-one is main compound isolated from Zanthoxylum chiloperone var angustifolium with broad spectrum antifungal, leishmanicidal and trypanocidal activities. Canthin-6-one exhibited trypanocidal activity in vivo in the mouse model of acute or chronic infection. Canthin-6-one exhibited a broad spectrum of activities against Aspergillus fumigatus, A. niger, A. terreus, Candida albicans, C. tropicalis, C. glabrata, Cryptococcus neoformans, Geotrichum candidum, Saccharomyces cerevisiae, Trichosporon beigelii, Trichosporon cutaneum and Trichophyton mentagrophytes var. interdigitale with MICs values between 5.3 and 46 umol/L.

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.

AG-14361 binds to the catalytic domain of PARP-1 and is a potent, selective inhibitor. AG-14361 is a selective inhibitor of PARP-1 with Ki50 value <5 nM. AG-14361 is the first high-potency PARP-1 inhibitor with the specificity and in vivo activity to enhance chemotherapy and radiation therapy of human cancer.

COPPER(II) 4-OXOPENT-2-EN-2-OLATE (Copper(II) acetylacetonate [Cu(acac)2]) is a soluble copper catalyst that has been widely employed in many types of reactions. It is a powerful reagent in organic synthesis. Anticancer properties of Copper(II) acetylacetonate complex was found by treating different cancer cell lines. The TUNEL assay showed a strong positivity in the C6 cells treated with Cu(acac)2 and this indicates that the Cu compounds initiated cell death by DNA fragmentation.

Calphostin C (UCN-1028C), isolated compound from Cladosporium cladosporioides, is a cell permeable, potent and highly selective inhibitor of protein kinase C (IC50=0.05 uM). Calphostin C has been shown to compete at the DAG binding site and inhibit DGK (DAG kinase, DAGK). Calphostin inhibition of PKC is light dependent. At higher concentrations it inhibits myosin light chain kinase, PKA (cAMP-dependent protein kinase), protein kinase G, c-Src (pp60v-src protein TyK) (tyrosine kinase) and DGK. This compound also inhibits PC-PLD1 and -PLD2 (Phospholipase D1 and D2, PLD1 and PLD2). Calphostin C has been observed to induce apoptotic DNA fragmentation and cell death. This compound has demonstrated the ability to inhibit cardiac L-type Ca2+ channels. It has demonstrated the ability to Inhibit cardiac L-type calcium channel protein inhibitors. Calphostin C is an inhibitor of MYLK, PKA and PKD.

BAG-956 is a dual PDK1 and class I PI 3-kinase inhibitor (IC50 values are 245, 56, 446, 35 and 117 nM for PDK1 and PI3K p110 -α, -β, -δ, and -γ respectively). BAG-956 has been shown to inhibit cellular AKT phosphorylation at Thr308. BAG-956 also blocks cell proliferation and causes arrest in the G1 phase of the cell cycle. BAG-956 has been shown to slow tumor progression in mouse xenograft models.

Cholanic acid is the archetypal C24 bile acid skeleton from which all other C24 bile acids can be derived. Of the two common isomers: 5alpha and 5Beta, the last isomer is the most biologically relevant. 5-Beta Cholanic Acid has been studied as a modulator of the gamma-secretase complex as it pertains to Alzheimer's disease; it has also been identified as an inhibitor of the Ephrin type-A receptor 2 that is involved in cancer cell signaling and angiogenesis.

(-)-Catechin gallate is a polyphenol, which occurs naturally in various plants, including green tea leaves. The compound was shown to have anti-cancer activity in vitro, with breast cancer, lung cancer, and colon cancer cells. It is supposed that the drug may act by inhibiting Bcl family of proteins. It has been reported to inhibit HIV-1 replication by targeting several steps in HIV-1 life cycle. (-)-Catechin gallate (in combination with other catechins) caused the hypocholesterolemic effect in rats.

AM-114, a derivative of boronic chalcone, is a potent small-molecule inhibitor of the proteasome that inhibits the chymotrypsin-like activity of the 20S proteasome, with a value of 50% inhibition concentration IC50 of approximately 1 uM, resulting in a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells without significantly disrupting the interaction of p53 and murine double minute 2 (mdm2) proteins. AM 114 also exerts anti-cancer activity against cancer cells, which potently inhibits the growth of human colon cancer HCT116 cells with values of IC50 of 1.5 uM and 0.6 uM in MTT and colony formation assays respectively.