N-Bis(2-hydroxypropyl)nitrosamine is an agent with carcinogenic activity.

Thiodigalactoside (TDG) is an orally active and potent galectin (GAL) inhibitor with Kd values of 24 μM, 49 μM for GAL1 and GAL3, respectively. Thiodigalactoside, a non-metabolizable disaccharide, has anti-inflammatory and anti-cancer activity. Thiodigalactoside dramatically reduces body weight gain in diet-induced obese rats.

Gypenoside LXXV, isolated from Gynostemma pentaphyllum, is one of the deglycosylated shapes of ginsenoside Rb1. Gypenoside LXXV significantly reduces cancer cell viability and displays an anti-cancer effect.

GPRP acetate (Gly-Pro-Arg-Pro acetate) is a fibrin polymerization inhibitor that inhibits the interaction of fibrinogen with the platelet membrane glycoprotein IIb/IIIa complex (GPIIb/IIIa).

MLCK inhibitor peptide 18 is a myosin light chain kinase (MLCK) inhibitor with an IC50 of 50 nM, and inhibits CaM kinase II only at 4000-fold higher concentrations.

Isoxanthohumol is a prenylflavonoid from hops and beer. Isoxanthohumol exhibits an antiproliferative activity against several human cancer cell lines. Isoxanthohumol inhibits the development of lung metastatic foci in tumor-challenged animals. Isoxanthohumol shows an antiviral activity towards herpes viruses (HSV1 and HSV2) and bovine viral diarrhea virus (BVDV).

Desmethylxanthohumol is a prenylated hydroxychalcone isolated from hop cones (Humulus lupulus L.). Desmethylxanthohumol is a powerful apoptosis inducing agent. Desmethylxanthohumol has antiplasmodial, antiproliferative, and antioxidant bioactivities.

Xanthohumol D, isolated from hops, is an inhibitor of quinone reductase-2 (QR-2) with the IC50 value of 110 μM, and binds to the active site of QR-2. Xanthohumol D shows antiproliferative activity on human cancer cell lines in vitro.

GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects.

Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.