Enzyme inhibitors

Catalog	Product Name / CAS / Description	Structure
BBF-05370	Δ-2-Doramectin Monosaccharide Inquiry
BBF-05404	Thelephoric acid (479-64-1) Inquiry
	Thelephoric acid is a terphenylquinone pigment found in several fungi, such as Omphalotus subilludens and Polyozellus multiplex. It is derived from atromentin, and its precusor can be from cyclovariegatin. Thelephoric acid has been shown to inhibit prolyl endopeptidase, an enzyme that plays a role in processing proteins (specifically, amyloid precursor protein) in Alzheimer's disease.
BBF-05447	Polyporic acid (548-59-4) Inquiry
	Polyporic acid is an intermediate in the biosynthesis of allantofuranone first isolated from a mycelial culture of the fungus species Hapalopilus nidulans. It inhibits the enzyme dihydroorotate dehydrogenase and has some antifungal and antibacterial activity.
BBF-05511	Physciosporin (64662-25-5) Inquiry
	Physciosporin (PHY) is an effective secondary metabolite found in lichens and isolated from Pseudocyphellaria coriacea. It inhibits the motility of lung cancer cells.
BBF-05522	Mertensene (66389-40-0) Inquiry
	Mertensene, a halogenated monoterpene isolated from the red alga Pterocladiella capillacea (S.G. Gmelin) Santelices and Hommersand, induces G2/M Cell Cycle Arrest and Caspase Dependent Apoptosis of Human Colon Adenocarcinoma HT29 Cell Line through the Modulation of ERK-1/-2, AKT and NF-κB Signaling. It has antimicrobial and anti-algal properties, and it has insecticidal effect.
BBF-05524	Virensic acid (668-14-4) Inquiry
	It is a lichen acid with enzyme inhibitory potential.
BBF-05534	Hypostictic acid (68729-11-3) Inquiry
	It has moderate inhibitory activity against the growth of Mycobacterium tuberculosis.
BBF-05537	2-O-Methylsekikaic acid (69563-42-4) Inquiry
	It is an inhibitor of Prostaglandin synthase with anti-oxidant activity and anti-radical power.
BBF-05538	2,4'-Di-O-methylnorsekikaic acid (69563-43-5) Inquiry
	It is an inhibitor of Prostaglandin synthase.
BBF-05539	4'-O-Methylpaludosic acid (69563-44-6) Inquiry
	It is an inhibitor of Prostaglandin synthase.
BBF-05561	Deschlorothricin (72656-14-5) Inquiry
	It is isolated from Streptomyces antibioticus. It shows DNA-binding properties and inhibits cholesterol biosynthesis.
BBF-05567	Acetyl oleanolic acid chloride (7372-21-6) Inquiry
	It has inhibitory activity against S. pneumoniae, and this activity is stronger than Oleanolic acid.
BBF-05591	Lirioresinol-B dimethyl ether (80780-43-4) Inquiry
	It is extracted from the seeds of Magnolia fargesii CHENG (Magnoliaceae). It inhibits NF-κB and COX-2 and activates IκBα expression in CCl4-induced hepatic fibrosis. It has anti-inflammatory and anti-cancer activities against HepG2 cells as well as in BALB/C male mice.
BBF-05663	Anhydrofulvic acid (95730-85-1) Inquiry
	In acidic condition, Anhydrofulvic acid inhibits mitochondrial respiration of Candida utilis using both succinate and cytochrome C as respiratory substrates, but not using NADH. Anhydrofulvic acid has antifungal activity.
BBF-05692	Neoxaline (909900-78-3) Inquiry
	Neoxaline is an alkaloid fungal metabolite originally isolated from Aspergillus japonicus. It inhibits the proliferation of Jurkat cells and induces cell cycle arrest at the G(2)/M phase.
BBF-05693	Psoromic acid (7299-11-8) Inquiry
	Psoromic acid is a selective inhibitor of Rab geranylgeranyl transferase and P. falciparum fatty acid synthesis (FAS) II enzymes.
BBF-05736	Polyoxorim (22976-86-9) Inquiry
	Polyoxorim is a member of the class of polyoxins that is isolated from the soil organism Streptomyces cacaoi var. asoensis. Polyoxorim exhibits fungicidal properties and may be used on rice, industrial grounds, golf courses and parks. It has a role as an EC 2.4.1.16 (chitin synthase) inhibitor and an antifungal agrochemical. It is a polyoxin and an antibiotic fungicide.
BBF-05780	Bivalirudin (128270-60-0) Inquiry
	Bivalirudin is a specific and reversible direct thrombin inhibitor (DTI). It is a synthetic congener of the naturally occurring drug hirudin. It is a DTI that overcomes many limitations seen with indirect thrombin inhibitors, such as heparin. It is a short, synthetic peptide that is potent, highly specific, and a reversible inhibitor of thrombin. It inhibits both circulating and clot-bound thrombin, while also inhibiting thrombin-mediated platelet activation and aggregation. It has a quick onset of action and a short half-life. It does not bind to plasma proteins (other than thrombin) or to red blood cells. Therefore, it has a predictable antithrombotic response. It does not require a binding cofactor such as antithrombin and does not activate platelets.
BBF-05812	Ibrexafungerp Citrate (1965291-08-0) Inquiry
	Ibrexafungerp Citrate, an intravenous and orally bioavailable semisynthetic derivative of enfumafungin, is a triterpene antifungal agent indicated for the treatment of adult and postmenarchal pediatric females with vulvovaginal candidiasis (VVC). It is a glucan synthase inhibitor.
BBF-05813	Ibrexafungerp (1207753-03-4) Inquiry
	Ibrexafungerp, an intravenous and orally bioavailable semisynthetic derivative of enfumafungin, is a triterpene antifungal agent indicated for the treatment of adult and postmenarchal pediatric females with vulvovaginal candidiasis (VVC). It is a glucan synthase inhibitor.

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. Reversible inhibitors bind non-covalently and can dissociate from the enzyme, allowing the enzyme to regain activity once the inhibitor is removed. They are further classified into competitive, uncompetitive, and non-competitive inhibitors.

How do enzyme inhibitors work?

Irreversible inhibitors

Irreversible inhibitors covalently bind to the enzyme, permanently inactivating it. This binding usually occurs at the active site or a critical residue essential for enzyme activity. Irreversible inhibitors reduce the total number of active enzyme molecules, thereby decreasing Vmax. Km may remain unchanged if the remaining active enzymes function normally. Aspirin irreversibly inhibits cyclooxygenase-1 (COX-1) by acetylating a serine residue in the active site.

Competitive inhibitors

Competitive inhibitors resemble the substrate and compete for binding to the active site of the enzyme. By occupying the active site, they prevent the substrate from binding. This type of inhibition increases the apparent Km (the substrate concentration at which the reaction rate is half of Vmax) without affecting Vmax (the maximum reaction rate). The inhibition can be overcome by increasing substrate concentration. For example, methotrexate competes with dihydrofolate for the active site of dihydrofolate reductase.

Uncompetitive inhibitors

Uncompetitive inhibitors bind only to the enzyme-substrate complex, preventing the conversion of the substrate to the product. This binding typically occurs at a site distinct from the active site.  Uncompetitive inhibition decreases both Km and Vmax, as the inhibitor only binds to the enzyme-substrate complex and not to the free enzyme. Lithium inhibits inositol monophosphatase in a manner consistent with uncompetitive inhibition.

Non-competitive inhibitors

Non-competitive inhibitors bind to an enzyme at a site other than the active site (allosteric site). This binding induces a conformational change in the enzyme that reduces its catalytic efficiency, regardless of substrate concentration. Non-competitive inhibition decreases Vmax without affecting Km. The inhibitor can bind to both the free enzyme and the enzyme-substrate complex. For example, cyanide inhibits cytochrome c oxidase by binding to a site other than the active site, blocking electron transport.

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.

What do enzyme inhibitors do?

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.

Regulation of metabolic pathways

Enzyme inhibitors are crucial in the regulation of metabolic pathways. Cells use natural inhibitors to modulate enzyme activity, ensuring that metabolic processes occur at appropriate rates and in response to changing cellular conditions.

Therapeutic agents

Many drugs are designed as enzyme inhibitors to treat diseases. By inhibiting specific enzymes, these drugs can modulate biochemical pathways and alleviate symptoms or cure diseases. Penicillin inhibits transpeptidase, an enzyme involved in bacterial cell wall synthesis. Protease inhibitors used in HIV therapy inhibit viral proteases necessary for virus replication. Inhibitors like imatinib target specific tyrosine kinases involved in cancer cell proliferation.

Industrial applications

Enzyme inhibitors are used in various industrial processes to control enzyme activity. For example, inhibitors are added to food products to prevent enzymatic browning and spoilage.