Enzyme Modulators

Omeprazole is a proton pump inhibitor (PPI) that inhibits the production of gastric acid in the stomach. This is due to Omeprazole binding through a stable disulphide bond to the H+/K+ ATPase enzyme found on parietal cells, and preventing hydrogen ion transport. Consequently, gastric acid secretion is supressed. As a PPI, Omerprazole can be used to treat disorders where gastric acid is over-secreted. Examples of these disorders are gastroesophageal reflux disease (GERD) and peptic ulcer disease. Omeprazole is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Specific inhibitor of 8-oxoguanine glycosylase OGG1 with IC50 in submicromolar range. The compound inhibits binding of OGG1 to its substrate 8-oxoguanine, a guanine analog generated in the presence of reactive oxygen species (ROS). It was shown that TH5487 decreases inflammation level by inhibiting the base excision DNA repair in mice and altering the OGG1 chromatin dynamics. The compound also has implications in cancer biology since OGG1 inhibitors sensitise tumours to chemotherapy.

Wee1 inhibitor with an IC50 of 5.2 nM

Immune suppressant; prevents pro-inflammatory cytokine release

Inhibitor of immunophilin FKBP12 and mTOR signalling with immunosuppressant activity. Zotarolimus inhibits proliferation of endothelial cells and smooth muscle cells and is employed in vascular interventional therapies.

Selective and reversible inhibitor of the multicatalytic 26S proteasome. The inhibition of protein breakdown affects several metabolic pathways and leads to cell death. The compound is effective in treating multiple myeloma because it prevents the binding of myeloma cells to bone marrow stroma and inhibits osteoclast differentiation.

Inositol monophosphatase (IMPase) inhibitor

N-ω-Propyl-L-arginine is a selective inhibitor of neuronal nitric oxide synthase (nNOS). This enzyme is involved in the production of nitric oxide, which plays important roles in various physiological and pathological processes in the body. N-ω-Propyl-L-arginine selectively inhibits nNOS, preventing the conversion of L-arginine to nitric oxide. This makes it a useful tool for studying the role of nNOS in various Life Sciences fields, such as neuroscience and cardiovascular research. It can also be used as an enzyme modulator or ligand in drug discovery studies targeting nNOS. N-ω-Propyl-L-arginine is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of B-Raf kinase mutant

Indomethacin is a nonsteroidal anti-inflammatory drug that inhibits the production of prostaglandin PGE2. It is used to treat pain, fever, and inflammation. Indomethacin's mechanism of action is not well understood, but it may be due to interference with the ability of PMNs to bind to the surface of bacteria or to release reactive oxygen species. The drug has been shown to reduce mitochondrial membrane potential in mammalian cells, leading to apoptosis. This effect on mitochondria may also contribute to Indomethacin's anti-inflammatory effects. Indomethacin is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Please enquire for more information about Polmacoxib including the price, delivery time and more detailed product information at the technical inquiry form on this page

Parecoxib is a COX-2 inhibitor and belongs to the group of pharmacological agents. It is a prodrug of valdecoxib that is used for the treatment of osteoarthritis and rheumatoid arthritis, as well as other conditions where the reduction in pain and inflammation are desired. Parecoxib sodium salt is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

(Z)-Mycophenolic acid is an immunosuppressive agent derived from the fermentation of fungi, primarily from the Penicillium species. It functions by inhibiting inosine monophosphate dehydrogenase (IMPDH), an enzyme crucial for de novo purine synthesis. This selective blockade of IMPDH specifically affects lymphocyte proliferation due to their heavy reliance on this pathway for DNA synthesis, thereby exerting its immunosuppressive effects. (Z)-Mycophenolic acid is primarily utilized in the field of transplantation medicine to prevent organ rejection in patients receiving transplants. Its ability to suppress T and B lymphocyte proliferation makes it an invaluable component of immunosuppressive regimens. Additionally, it is being explored for its potential applications in treating autoimmune diseases, given its targeted mode of action and relatively specific effects on immune cells. The mechanistic understanding of (Z)-Mycophenolic acid provides insightful avenues for further research into immune regulation and therapeutic interventions.

Inhibitor of DNA replication; inhibitor of theophylline and caffeine metabolism

Nitazoxanide acts as a noncompetitive inhibitor of the pyruvate: ferredoxin/flavodoxin oxidoreductases of various microorganism with Ki values between 2 and 10 μM. Nitazoxanide is clinically relevant for its broad-spectrum action to reduce the growth of bacteria, various parasites, and especially for its efficacy against the pathogen Helicobacter pylori. Nitazoxanide also has been shown to be effective in treating inflammatory bowel disease and acute enteritis caused by bacteria. In 2021, nitazoxanide was tested for the treatment of COVID-19 patients with mild symptoms due to its broad antiviral action. Nitazoxanide is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Topoisomerase I inhibitor

Inhibitor of phosphodiesterase 7

Analog of cAMP; activates cAMP receptors

Inhibitor of MEK kinase; anti-neoplastic

Angiotensin-converting enzyme inhibitor; antioxidant

Idelalisib is a pharmaceutical drug that functions as a PI3Kδ inhibitor, developed through synthetic chemical processes. Its mode of action involves selectively targeting and inhibiting phosphatidylinositol 3-kinase delta (PI3Kδ), a lipid kinase that plays a crucial role in the signaling pathways responsible for cell proliferation, survival, and differentiation. By inhibiting this enzyme, Idelalisib effectively impedes pathways that are often hyperactivated in certain hematologic malignancies, thereby exerting antitumor effects. Idelalisib is primarily utilized in the treatment of specific types of blood cancers, including chronic lymphocytic leukemia (CLL), follicular B-cell non-Hodgkin lymphoma (FL), and small lymphocytic lymphoma (SLL). Its application is particularly beneficial for patients who have relapsed after previous therapies or are considered unfit for standard chemoimmunotherapy. By disrupting the signaling cascade essential for the survival and proliferation of malignant B cells, Idelalisib induces apoptosis and reduces tumor growth, presenting a targeted therapeutic approach in the oncology field.

Pazopanib is an antineoplastic agent that is used to treat advanced renal cell cancer and advanced soft tissues sarcoma. This drug is a multitargeted tyrosine kinase inhibitor against vascular endothelial growth factor receptor 1, 2, 3 and c-kit. As a result, it increases tumor apoptosis and decreases tumor blood flow. Pazopanib is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Serine protease inhibitor

Capecitabine is a chemotherapeutic agent that is used in the treatment of various cancers such as gastrointestinal, breast and pancreatic. This drug is a nucleotide metabolic inhibitor and inhibits DNA synthesis and slows the growth of tumor tissue. It is a prodrug of Fluorouracil. Capecitabine is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Voglibose is a competitive inhibitor of α-glucosidase used for the control of blood sugar levels in patients with type 2 diabetes mellitus. The compound binds reversibly to intestinal carbohydrate-active digestive enzymes with α-glucosidase activity, inhibits breakdown of complex sugars and consequently delays the absorption of glucose into blood. Voglibose is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of TAOK1 and TAOK2 kinases

Inhibitor of FGFR kinase

A15 also known as alpha2-Antiplasmin is a serine/protease inhibitor which inactivates plasmin in the blood. To inhibit plasmin in the blood alpha2-Antiplasmin forms a protease serpin complex with plasmin due to interactions of kringle 1 or 3 of plasmin and the lysine residues of alpha2-Antiplasmin's C-terminus. Although synthesised in the Liver A15 is also present within the neurons of the human brain and its expression has been found to be enhanced in Aβ plaques of Alzheimer's disease and during myocardial infarction. A high concentration of alpha2-Antiplasmin in the blood may also contribute to an increased risk of Ischemic strokes. Alternatively its expression appears to be diminished in patients with cirrhosis and acute liver failure. A further function of A15 is its ability to regulate fibrinolysis through crosslinking to fibrin.

Inhibits Wnt signaling pathway by targeting porcupine, a membrane-bound O-acyltransferase involved in the palmitoylation and secretion of Wnt. Anti-cancer properties of LGK 974 have been demonstrated in various tumor models of breast cancer, head and neck squamous cell carcinoma and glioblastoma. Blocks LPS-mediated inflammatory response in epithelial and endothelial cells.

Zileuton is an inhibitor of the 5-lipoxygenase enzyme, thus preventing the leukotrienes LTE4, LDT4, LTB4 and LTC4 from being formed. This in turn reduces inflammation, bronchoconstriction and mucus secretion in the airways. As a result, Zileuton can be used in the treatment and management of asthma and allergic rhinitis. Studies have shown that Zileuton has the potential to reverse dementia-related brain damage. Zileuton is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Antirheumatic; immunosuppressant; neuroprotective; neuroregenerative

Inhibitor of AKR1C3 (type 5 17β-hydroxysteroid dehydrogenase)

Inhibitor of VEGFR; antineoplastic

Moclobemide is a monoamine oxidase inhibitor that is used to treat major depressive disorder and dipolar disorder. This drug’s mechanism of action involves the reversible inhibition of the enzyme MAO-A. The inhibition of this enzyme results in a decreased metabolism and destruction of neurotransmitters thus relieving the symptoms of depression and bipolar disorder. Moclobemide is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

A novel survivin suppressant with an IC50 of 0.54 nM for the negative regulation of the survivin promoter.

Multi-kinase inhibitor; inhibits epoxide hydrolase; antineoplastic

This product is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

JAK3 enzyme inhibitor

Ibandronate is a bisphosphate used in the treatment of osteoporosis in postmenopausal women. This drug slows down the activity of osteoclasts resulting in a slower process of bone breakdown. This drug also inhibits farnesyl diphosphate and induces apoptosis of hematopoietic tumor cells. Ibandronate sodium salt monohydrate is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibits c-MET tyrosine kinases

Amino acids 359-409 of human glycogen synthase kinase 3 β (GSKβ), a multifunctional serine/threonine kinase widely expressed in most mammalian cells. GSKβ is highly active under basal conditions and acts downstream of phosphoinositide 3-kinase (PI3K) signalling. PI3K activation results in Akt phosphorylation and the subsequent phosphorylation of GSKβ at serine-9 and its inactivation. GSKβ in turn activates the production of pro-inflammatory cytokines including IL-1β, IL-6, IL-12, IL-17, TNFalpha and IFNγ, and supresses the production of IL-10, IL-1Ra, and IFNβ by immune cells. Under resting conditions, GSKβ is constitutively active due to tyrosine-216 phosphorylation, and it phosphorylates and inhibits a diverse group of pro-oncogenic substrates, such as: β-catenin- cyclin D1- c-Jun- c-Myc and CREB. GSKβ is also involved in Wnt signalling pathways.Aberrant expression of GSKβ has been shown to promote cell growth in some cancers and to suppress it in others. GSKβ inhibition leads to the accumulation of β-catenin in the nucleus, enhancing the progression of many cancers. However the inhibition of GSKβ also induces apoptosis in various types of cancers, such as pancreatic, colorectal and bladder cancer. Inhibition of GSKβ can also have neuroprotective effects on dopaminergic neurons such as in Parkinson's disease.

Inhibits non-receptor tyrosine kinase BTK; antineoplastic

Inhibits multiple receptor tyrosine kinases (RTKs), including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl. Sitravatinib inhibits proliferation of sarcoma cells and reduced tumor growth in vivo. Promotes immune response in tumor microenvironment and enhances sensitivity to immune checkpoint inhibitors. This compound is undergoing several clinical trials as a potential anti-cancer therapeutic agent.

A selective inhibitor of PI3Kα. Inhibits cancer cell proliferation by blocking the G0/G1 phase of the cell cycle. Anti-tumor effect of BYL 719 has been demonstrated in models of tumors with PI3KCA mutation and amplification in vivo. BYL 719 also suppresses tumor growth in pre-clinical models of osteosarcoma.

Inhibits isocitrate dehydrogenase 1 (IDH-1) harbouring a gain of function mutation at R132, which causes impaired cellular differentiation via epigenetic modulation. By inhibiting mutant IDH1, synthesis of oncometabolite 2-hydroxyglutarate is reduced. This compound therefore has therapeutic potential in solid and haematological malignancies, such as acute myeloid leukemia (AML).

Inhibitor of acetylcholinesterase

Inhibitor of cytochrome P450; inhibitor of prostaglandin synthesis

Epalrestat is a carboxylic acid derivative that is used for the treatment of diabetic neuropathy. This drug is an aldose reductase inhibitor and aims to reduce the accumulation of intracellular sorbitol. Studies in rats have shown this drug to improve morphological abnormalities of nerves. Epalrestat is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

A potent inhibitor of EGFR with sensitizing and T790M resistance mutations, selective over the wild-type form of the receptor. Causes tumour regression in EGFR mutant T790M transgenic and xenograft models in vivo.

Inhibitor of metalloendopeptidase neprilysin