Enzyme inhibitors

Mebendazole is a benzimidazole anthelmintic and Tubulin-disrupting drug. It has antitumour activity in vitro and in vivo and inhibits growth and induces apoptosis. It is highly effective on various gastrointestinal nematodes in animals, has good effects on some tapeworms, and also effective on Trichinella spiralis. It is used for nematode diseases of horses, sheep, poultry and wild animals, nematodes and tapeworms of dogs and cats.

It is a type II topoisomerase inhibitor with IC50 of 2.0 μM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively. Mitoxantrone dihydrochloride is an antiviral, antibacterial, antiprotozoal, immunomodulating and antineoplastic anthraquinone derivative.

A semi-synthetic product produced by hydrolysing the disaccharide unit of ivermectin. It is a potent inhibitor of nematode larval development, but is devoid of paralytic activity. The aglycone is used as a sensitive probe for the detection of some types of ivermectin resistance. An impurity of Ivermectin.

A semi-synthetic product produced by selective hydrolysis of the terminal saccharide unit. It is a potent inhibitor of nematode larval development, but is devoid of paralytic activity. It is a sensitive probe for the detection of some types of ivermectin resistance. An impurity of Ivermectin.

Cercosporamide, a natural antifungal phytotoxin produced by Cercosporidium sp. MST-FP1899, has been found to be a selective Mnk inhibitor and shows probable antileukemic effects.

A rare fungal metabolite produced by selected penicillium species. It is a pollen growth inhibitor.

It is a fungal metabolite originally isolated from Nemania sp. UM10M. It is a major component of the cytochalasin complex. It inhibits tumour cell growth in vitro and inhibits the growth of chloroquine-sensitive and -resistant strains of P. falciparum.

It is a fungal metabolite originally isolated from Nemania sp. UM10M. It is a major component of the cytochalasin complex. It inhibits tumour cell growth in vitro. It is active against the chloroquine-sensitive and -resistant strains of P. falciparum.

Luteoreticulin is a rare nitrophenyl pyranone closely related to aureothin, neoaureothin and its unusual photoisomers Antibiotics SNF4435C and D. It is a potent antitumor agent produced by Streptomyces luteoreticuli with pronounced immunosuppressive. It also has nematocide activity.

An alkaloid topoisomerase I (topo I) inhibitor with anticancer properties. It is isolated from camptotheca acuminata, a deciduous tree or nothapodytes foetida.

An isocoumarin metabolite produced by selected species of streptomyces. It is a potent inhibitor of cyclic nucleotide phosphodiesterase. It also causes dose-dependent inhibition of lung metastasis in the B16F10 melanoma model.

It is a ring expanded isomer of apoptolidin originally isolated from Nocardiopsis sp. It demonstrates 10-fold reduced F1FO-ATP synthase inhibitory activity compared to apoptolidin (IC50s = 17 and 0.7 µM, respectively).

It has been shown to increase intracellular glutathione levels in cystinotic cells, thus restoring the altered redox state of the cells. It is an antioxidant and inhibitor of DMBA-induced tumors.

Elasnin is isolated from certain strains of Streptomyces. Elasnin is a reversible inhibitor of elastase with IC50 values of 1.3 and 30 µg/ml for human granulocyte and pancreatic enzymes, respectively. It inhibits human leukocyte elastase, porcine pancreatic elastase, and chymotrypsin with Ki values of 93, 69 and 224 µM, respectively.

It is an antitumor drug and a PP1 and PP2A inhibitor. It is a modified product of the natural antitumor drug cantharidin. It reduces its urinary system toxicity but not its antitumor efficacy after is demethylated. It induces cell apoptosis and acts as an antineoplastic.

The dominant analogue of complex of spiroketals isolated from streptomyces sp. It is an inhibitor of the mitogenic activity of EGF and a G1 phase cell cycle inhibitor. It selectively inhibits isoleucyl-trna synthetase. It has anti-proliferation effect on human cell lines KB and K562, and has potent antifungal activity.

Berubicin has potential antineoplastic activity. Berubicin intercalates into DNA and interrupts topoisomerase II activity, resulting in the inhibition of DNA replication and repair, and RNA and protein synthesis.

N-acetyl trans-4-hydroxyproline is an atypical inflammation inhibitor, which can be used to treat osteoarthritis and other diseases that affect connective tissue.

Hydroxypurine is an alkaloid isolated from L. lanatus. It is an inhibitor of ganglion transmission.

Epibenzomalvin E is a new substance P inhibitor from Penicillium.