Cerulenin ((2R,3S)-2,3-epoxy-4-oxo-7,10-trans, trans-dodecadienoylamide) is an antifungal antibiotic isolated from Cephalosporium caerulens, that inhibits eukaryotic lipid and sterol synthesis and blocks lipid modification of proteins. Cerulenin is a potent inhibitor of fatty acid synthase (FAS). It inhibits all known types of FASs: both multifunctional enzyme complexes (Type I) (from yeast, rat liver, mammalian cells, and certain bacteria) and unassociated enzymes (Type II) (from most bacteria, and higher plants). Cerulenin blocks the synthesis of polyketides in a wide variety of organisms, including actinomycetes, fungi, and higher plants. In addition, cerulenin is suggested to inhibit the condensation step in polyketide synthesis as well as fatty acid synthesis. Cerulenin has a wide range of antimicrobial activity, the drug significantly inhibits the growth of yeast-like fungi, such as Candida, Saccharomyces, and Cryptococcus. Cerulenin is commercially available as a biochemical reagent for widespread use in the field of obesity, cancer biology, posttranslational protein modification system, drug discovery research and so on.

PD-166866 is a member of a new structural class of tyrosine kinase inhibitors, the 6-aryl-pyrido[2,3-d]pyrimidines. PD 166866 is an inhibitor of FGFR1. PD166866 might be used in the control of fibrotic proliferative diseases, as well as in other tumor pathologies. PD166866 inhibits proliferation and triggers anoikis in FGFR1-amplified breast cancer cell lines. Mechanistic study reveals that PD166866 induces autophagy through repressing Akt/mTOR signaling pathway.

Verrucarin A (VC-A) is a Type D macrocyclic mycotoxin which inhibits cell proliferation and induces apoptosis in cancer cells. Strong antiproliferative and apoptosis-inducing activity of verrucarin A for pancreatic ductal adenocarcinoma and prostate cancer cells through cell cycle arrest and inhibition of the prosurvival (antiapoptotic) AKT/NF-κB/mTOR signaling.has being demonstrated. Verrucarin A, a protein synthesis inhibitor, also induces growth inhibition and apoptosis in breast cancer cell lines MDA-MB-231 and T47D.

Psoralidin (1) was first isolated from seeds of Psoralea corylifolia Linn. It was found to be an active ingredient of many Indian and Chinese traditional herbal medicines. Psoralidin exhibits a variety of biological activities like antineoplastic, antioxidant, antibacterial, antidepressant activities. Psoralidin inhibits protein tyrosine phosphatase 1B activity. Psoralidin may act as a estrogen receptor agonist. In addition psoralidin showed potent and noncompetitive inhibition against UDP- glucuronosyltransferase (UGT) or cytochrome p450 (CYP450) enzymes.

Tunicamycin VII is nucleotide sugar analogs produced by several Streptomyces species. In eukaryotes, Tunicamycin VII inhibit UDP-N-acetylglucosamine-dolichol phosphate GlcNAc-1-P transferase (GPT) that catalyzes the first step in protein glycosylation. In bacteria they inhibit UDP-N-acetylmuramoyl-pentapeptide: undecaprenol phosphate MurNAc-pentapeptide-1-P transtransferase (MraY) that catalyzes an early stage in peptidoglycan cell wall assembly. Tunicamycins are substrate analog of GPT and MraY, such that the alphabeta-1'',11'-linked GlcNAc residue of the tunicamycins mimics the transferred GlcNAc-1-phosphate. Tunicamycin VII impairs ALK phosphorylation and disrupts pro-survival signaling and cell viability in various neuroblastoma cell lines. 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.

6-(4-chlorophenyl)imidazo(2,1-b)(1,3)thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl)oxime (CITCO) is a novel potent and selective agonist for the human orphan nuclear receptor CAR (constitutive androstane receptor). CITCO displayed an EC50 of 49 nM in a CAR FRET assay and showed 50-fold selectivity for CAR over PXR. CITCO displayed no activity against a panel of 15 other nuclear receptors at a concentration of 10 µM. In hepatocytes CITCO induced CAR nuclear translocation and induced the CAR target gene CYP2B6. The cell proliferation of several ovarian cell lines expressing CAR significantly increased when CITCO was combined with anticancer agents compared with any anticancer agent alone. The up-regulation of MDR1 and UGT1A1 by anticancer agents was further enhanced in the presence of CITCO. Combination of CITCO with any anticancer agents significantly enhanced CAR-mediated transcription compared with any anticancer agents alone and CAR down-regulation completely inhibited the transcription in the presence of CITCO and/or anticancer agents. Inhibition of CAR pathway could be a novel therapeutic approach for the augmentation of sensitivity to anticancer agents, or to overcome resistance, in the treatment of ovarian cancer. CITCO has being shown to inhibit growth and expansion of brain tumour stem cells. CITCO induced a dose-dependent decrease in growth and expansion of CD133(+) BTSCs as gliospheres in culture. Cell cycle arrest and apoptosis in BTSCs were induced by CITCO, but not in normal astrocytes. Growth of s.c BTSC xenograft in nude mice was also inhibited by CITCO. CITCO inhibits the growth and expansion of BTSCs, suggesting the use of CAR agonists for the treatment of brain tumour.

BMS-754807 is an orally bioavailable, potent and reversible small molecule inhibitor of the IGF-1R/IR family kinases with Ki <2 nmol/L. BMS-754807 could effectively inhibit the growth of many human tumor types from in vitro perspective, such as mesenchymal, hematopoietic and epithelial tumor cell lines with an IC50 value of 5–365 nmol/L. BMS-754807 F-18 is the first small molecule radioligand that showed promise for imaging IGF-1R in tumor/ cancer. The results indicate that BMS-754807 F-18 can be a potential PET imaging agent for in vivo monitoring IGF-1R.

Bisbenzimide ethoxide is a fluorescent nucleic acid stain useful for DNA labeling in fluorescence microscopy and flow cytometry. It appears to bind to AT-rich regions containing at least four such basepairs. Bisbenzimide ethoxide seems to bind relatively poorly to nucleotide sequences containing the alternating step TpA. Bisbenzimide ethoxide induced apoptosis in the HL-60 cells in a time- and dose-dependent manner. Endogenous nuclear topoisomerase I activity in HL-60 cells was inhibited by treatment with Bisbenzimide ethoxide.

Sylvatesmin is a furofuran lignin isolated from Forsythia suspense, Osmanthus fragrans and other plants. It protected LDL from lipid peroxidation and demonstrated free radical scavenging activity. Molecular modeling showed that sylvatesmin exhibited the highest inhibition of aldose reductase. In nutritive hyperlipidemia mice fed with high-cholesterol in vivo, the serum levels of blood TG and LDL-C were remarkably down-regulated by sylvatesmin. In vitro, sylvatesmin exhibited anti-inflammatory and anti-cancer activity.

Margaric acid (Heptadecanoic acid, C17) is a fatty acid of exogenous (primarily ruminant) origin. Many "odd" length long chain amino acids are derived from the consumption of dairy fats (milk and meat). Heptadecanoic acid constitutes 0.61% of milk fat and 0.83% of ruminant meat fat. The content of heptadecanoic acid in the subcutaneous adipose tissue of humans appears to be a good biological marker of long-term milk fat intake in free-living individuals in populations with high consumption of dairy products. Margaric acid is a metabolite in glutamate and lipid metabolism in vivo. Blood-brain barrier permeable. Orally active. Possibly involved in anti-tumor activity.