Enzyme inhibitors

Enzyme inhibitors

Catalog Product Name / CAS / Description Structure

γ-Mangostin (31271-07-5)


gamma-Mangostin isolated from the fruit of Garcinia cambogia is an HIV protease inhibitor. gamma-Mangostin is cytotoxic to HL-60, SMMC-7721, A549, MCF-7, and SW480 cancer cells and BEAS-2B non-cancerous pulmonary epithelial cells in vitro (IC50s = 7.39, 6.57, 10.07, 5.33, 8.4, and 7.43 μM, respectively).


Chelerythrine is a cell-permeable inhibitor of protein kinase C (IC50 = 660 nM) with a wide range of biological activities.


Artemisinin (63968-64-9)


Artemisinin is a natural product originally isolated from plants of the genus Artemisia. It effectively kills malarial parasites of the genus Plasmodium. It is usually used in combination therapy for the treatment of malaria. Artemisinin is also used against a wide range of trematodes, including Schistosoma. Artemisinin is an inhibitor of human NOS2 (iNOS) with anticancer activity.


Embelin (550-24-3)


Embelin, a quinone isolated from the Japanese Ardisia herb, is an inhibitor of X-linked inhibitor of apoptosis (XIAP) with IC50 of 4.1 uM.


Naringenin (67604-48-2)


Naringenin is an estrogen receptor binding inhibitor produced by Streptomyces graminofaciens BA 14348.


Sulopenem (120788-07-0)


Sulopenem is a penem antibiotic and a β-lactamase inhibitor produced by Penicillium. Sulopenem showed potent antibacterial activity against gram-positive and gram-negative bacteria except Pseudomonas aeruginosa and Xanthomonas maltophilia.


Mevastatin (73573-88-3)


It is produced by the strain of Penicillum brevicompactum. It has weak anti-fungal activity and can inhibit the key enzyme (3-hydroxy-3-methyl glutaryl coenzyme A(HMGCoA) reductase) in the cholesterol biosynthesis pathway. It has been shown to lower cholesterol in animals and humans. It led the discovery of statins, lipid-lowering drugs. It is now used as a biochemical reagent.


Thailanstatin A (1426953-21-0)


Thailanstatin A is a splicesosome inhibitor that acts via suppressing RNA-polymerase II. It is effective against cancers, and can be used as a payload for ADCs.


Cyclo (-Leu-Pro) is a cyclic dipeptide containing leucine and proline.


K252A (99533-80-9)


K252a, an analog of staurosporine, has been found to be a protein kinase inhibitor and exhibit antitumor activity at some extent.


Bafilomycin A1 (88899-55-2)


It is produced by the strain of Streptomyces griseus ssp. sulphurus TU 1022 and Str. griseus TU 2437. Bafilomycin A1 is a vacuolar H+-ATPase inhibitor with IC50 of 0.44 nM. It can inhibit the growth of gram-positive bacteria, negative bacteria, fungi, yeast and protozoa, and has the effects of insect killing, nematode killing and immunosuppression.


Ixazomib Citrate (1239908-20-3)


The citrate salt form of Ixazomib which is a proteasome inhibitor. It is undergoing a rollover Phase II trial against multiple myeloma, amyloidosis and lymphoma in sorts of countries. IC50 = 3.4 nM.


Marizomib (437742-34-2)


Marizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity. Marizomib irreversibly binds to and inhibits the 20S catalytic core subunit of the proteasome by covalently modifying its active site threonine residues.


Plitidepsin (137219-37-5)


Plitidepsin is a cyclic depsipeptide isolated from the marine tunicate Aplidium albicans. Plitidepsin shows potent anticancer activity against a large variety of cultured human cancer cells, inducing apoptosis by triggering mitochondrial cytochrome c release, initiating the Fas/DC95, JNK pathway and activating caspase 3 activation. This agent also inhibits elongation factor 1-a, thereby interfering with protein synthesis, and induces G1 arrest and G2 blockade, thereby inhibiting tumor cell growth.


Berubicin (677017-23-1)


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.


Diprotin A (90614-48-5)


It is produced by the strain of Bacillus cereus BMF 657-RF1. It can inhibit Dipeptidyl amino peptidase IV and immune enhancement effect.


Atpenin A5 (119509-24-9)


Atpenin A5 is an inhibitor of SDHB, SDHC and SDHD. It is an antifungal antibiotic produced by Penicillium sp. and an ubiquinone-binding site inhibitor of succinate dehydrogenase with IC50s of 12 nM for nematode and IC50s of 3.7 nM for mammalian mitochondria. Atpenin A5 is the most effective inhibitor against complex II from all the atpenins and has been shown to protect against cardiac-reperfusion injury in rat studies through the stimulation of mitochondrial KATP channels.


Miltefosine (58066-85-6)


Miltefosine inhibits PI3K/Akt activity with ED50 of 17.2 μM and 8.1 μM in carcinoma cell lines A431 and HeLa, first oral drug for Visceral leishmaniasis, effective against both promastigotes and amastigotes.


Temsirolimus (162635-04-3)


Temsirolimus is an mTOR inhibitor produced by Streptomyces. Temsirolimus potently inhibits mTOR kinase activity with IC50 of 1.76 μM, similar to that of rapamycin with IC50 of 1.74 μM.


Sulbactam is an irreversible inhibitor of β-lactamase. It binds to the enzyme and does not allow it to degrade the antibiotic.

BOC Sciences has been committed to providing customers with high quality enzyme inhibitors.

Enzyme inhibitors are a class of substances that can specific binding to certain groups of enzymes and decrease their activity. By reducing or completely losing enzymes activity related to certain diseases in the organism, enzyme inhibitors can be used as related drugs to obtain curative effects.

Classification of Enzyme Inhibitors

Currently, as many as hundreds of enzyme inhibitors have been discovered.

  • According to chemical properties
  • Enzyme inhibitors can be divided into inorganic compounds (such as heavy metal salts, chlorides, fluorides, phosphates, etc.) and organic compounds (such as isobutyric acid, urea derivatives, paraformaldehyde, etc.).

  • According to inhibitor type
  • Enzyme inhibitors can be divided into oxidoreductase inhibitors, transferase inhibitors, hydrolase inhibitors, lyase inhibitors, isomerase inhibitors and synthetase inhibitors.

  • According to the disease being treated
  • Enzyme inhibitors include anti-tumor enzyme inhibitors, anti-HIV enzyme inhibitors, anti-inflammatory enzyme inhibitors, anti-thrombotic enzyme inhibitors and so on.

  • According to the mechanism of action with enzymes
  • Enzyme inhibitors can be divided into irreversible and reversible.

Source of Enzyme Inhibitors

Enzyme inhibitors are mainly derived from plants, microorganisms and chemical synthesis. The primary metabolites and secondary metabolites of microorganisms are able to produce enzyme inhibitors. Actinomycetes are the group of microorganisms that produce the most enzyme inhibitors. Bacteria and fungi are also crucial microbial sources of enzyme inhibitors. In addition to the traditional screening and isolation of medicinal bacteria, researchers have focused their attention on a variety of new microbial groups, such as marine microbes and extreme microbes. Plants are the main source of new drugs for enzyme inhibitors.

Application of Enzyme Inhibitors

Enzyme inhibitors are vital to organisms. In animals and plants, there are biological macromolecular enzyme inhibitors related to human biological regulation. In industrial production, the quality of fermented products can be improved by inhibiting metabolic regulation enzymes. Enzyme inhibitors are widely used in agricultural production, medicine and military fields. Certain enzyme inhibitors could be taken as serve as herbicides or insecticides. Enzyme inhibitors could also be available for clinical applications. Lots of drugs and poisons related to diseases are enzyme inhibitors.

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