Modulateurs d'enzymes

During extraction of lecithin from egg yolk, peptide by-products can be isolated and purified by gel filtration. Within the by-products this has led to the discovery of biologically active value-added products. The egg yolk gel filtration (EFGF) fractions were analysed for their antioxidant and angiotensin converting enzyme (ACE) inhibitory activities. EYGF-33 predominantly contained 3 peptides - KLSDW, YPSPV, and MPVHTDAD). YPSPV in EYGF-33 was found to have minimal antioxidant activity. However, YPSPV showed notably high angiotensin converting enzyme (ACE) inhibitory activity, it exceeded the positive control captopril.

Benazepril is a nonsteroidal anti-inflammatory drug that can be used to treat hypertension, heart failure and renal failure. It is an angiotensin-converting enzyme (ACE) inhibitor that blocks the conversion of angiotensin I to angiotensin II. This inhibition prevents the vasoconstrictive effects of this peptide, which are mediated through activation of the renin-angiotensin system. Benazepril HCl 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.

Dipeptidyl peptidase-4 inhibitor; anti-diabetic agent

Inhibits type III tyrosine kinases (PDGFRα, PDGFRβ, FLT3)

Spirapril hydrochloride is an antihypertensive agent, which is a synthetic pharmaceutical compound designed to treat high blood pressure. The compound is derived from laboratory synthesis aimed at modulating the renin-angiotensin-aldosterone system. Its mode of action involves the inhibition of angiotensin-converting enzyme (ACE), which is crucial for the conversion of angiotensin I to the vasoconstrictor peptide angiotensin II. Angiotensin II is responsible for the constriction of blood vessels and an increase in blood pressure. By inhibiting this enzyme, Spirapril hydrochloride effectively reduces vascular resistance and lowers blood pressure. The primary application of Spirapril hydrochloride is in the management and treatment of hypertension, providing a means to control elevated blood pressure and reduce the risk of associated cardiovascular events. Additionally, it may be used adjunctively in treating certain heart conditions, improving cardiac function by decreasing preload and afterload on the heart. Its efficacy in hypertension management positions it as a critical agent in therapeutic regimens aiming at minimizing the long-term risks associated with chronic high blood pressure.

Pomalidomide is an immunomodulatory agent that inhibits transcriptional regulation by interacting with the pomalidomide-binding protein, which prevents its interaction with RNA polymerase II and thereby prevents DNA transcription. The study with U266 cells demonstrated that pomalidomide targets CRBN, part of an E3 ligase complex, and inhibits its autoubiquinitation and supresses a critical gene (IRF4, interferon regulatory factor 4) for myeloma cell growth with concentrations up to 10 μM. In vitro assays have shown that pomalidomide has inhibitory effects on cell signaling pathways, such as the NF-κB pathway. Pomalidomide also decreases the production of proinflammatory cytokines, such as TNFα and IL-1β, by inhibiting their synthesis or their release from activated monocytes. Recently, the promoting effect of pomalidomide, as its analog lenalidomide, on erythropoiesis (production of red blood cells) has been investigated, demonstrating positive results for its use as a potential new therapy agent for β-hemoglobinopathies. Pomalidomide 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 cathepsin K inhibitor; reduces bone resorption

A selective VHL inhibitor that stabilizes the hydroxylated form of HIF-α, resulting in upregulation of downstream target genes and proteins. Provides a tool for studying hypoxic signaling pathway.

mTOR kinase inhibitor; rapamycin analog; immunosuppressant

A potent ATP-competitive inhibitor of tropomyosin-related kinases (TRK1, TRK2 and TRK3), members of the receptor tyrosine kinase family of neurotrophin receptors. Tumors with oncogenic TRK fusions are sensitive to larotrectinib, leading to reduced proliferation and tumor growth in patients with soft tissue sarcoma, triple-negative breast cancer and lung cancer.

Inhibitor of histone deacetylases

A glycogen synthase kinase 3β- (GSK3β-) / crosstide fragment representing the phosphorylation site on GSK3β-. GSK3β- is a serine/threonine kinase which regulates glycogen synthase activity and is a key mediator of vertebrate development, tumourigenesis and cell differentiation. GSK3β- is phosphorylated by activated AKT/protein kinase B on serine 9- promoting its inactivation.

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.

Inhibitor of leucine-rich repeat kinase LRRK2Â

Inhibitor of vacuolar-type proton pump

Inhibitor of TOP1 topoisomerase; anti-cancer

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.

Oxaprozin is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of osteoarthritis and rheumatoid arthritis. This drug relieves swelling and inflammation by inhibiting the enzyme cyclooxygenase which in turn inhibits prostaglandin synthesis. Oxaprozin 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.

Nonsteroidal anti-inflammatory (NSAID)

Pralidoxime is a cholinesterase reactivator that is used for the treatment of organophosphate poisoning. When organophosphate binds to the esteratic site of acetylcholinesterase, it results in a reversible inactivation of the enzyme. However, by rupturing the phosphate-ester link that has been formed between the organophosphate and acetylcholinesterase, pralidoxime is able to reactivate the cholinesterase enzyme. Pralidoxime chloride 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 PDE4 enzyme; anti-inflammatory

Inhibitor of B-RAF kinase

Thromboxane A2 synthetase inhibitor

Malotilate is a pharmacological agent that is used to treat symptoms of hepatitis, bowel disease, and collagen diseases. This drug reduces collagen synthesis and cell migration activity of fibroblasts in vitro. It also has been shown to facilitate liver regeneration in rats. Malotilate 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 tyrosinase in melanocytes: skin whitener

Phosphorylated EGFR peptide substrate.

Ubenimex is a protease inhibitor drug that is being studied for the treatment of acute myelocytic leukemia. This drug is an aminopeptidase N, B and leukotriene A4 hydrolase inhibitor. It is also used in the treatment of hypercholesterolaemia. Ubenimex 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.

Apremilast is the commercial name of a phosphodiesterase-4 (PDE4) inhibitor developed to treat chronic inflammatory disorders. Similarly to thalidomide, the apremilast molecule carries a phthalimide ring, but it lacks however the glutarimide ring needed to bind to cereblon, specifically targeted by thalidomide. As a drug, apremilast is indicated for the treatment of psoriasis and psoriatic arthritis. Apremilast 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.

Imatinib is a tyrosine kinase inhibitor that is used in the treatment of various leukemias and gastrointestinal stromal tumors. This drug inhibits the BCR-ABL tyrosine kinase. It is suggested that Imatinib also inhibits other tyrosine kinases such as PDGF, SCF and c-Kit. Imatinib base 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 II and DNA helicase inhibitor

PI3K enzyme inhibitor

PI3K enzyme inhibitor; antineoplastic

Ile-Pro-Pro (IPP) has the ability to inhibit angiotensin-converting enzyme and stimulate the production of nitric oxide. It could be used to improve hypertension thus reducing the risk of cardiovascular diseases.

VEGFR tyrosine kinase inhibitor

Inhibitor of pan-class I PI3K family of lipid kinases; antineoplastic

A tyrosine kinase inhibitor with potent activity against EGFR, STAT3, JAK3/STAT, JAK3/AP-1 and JAK3/MAPK. Suppresses IL-2 signaling pathway, inhibits T-cell growth and activation of JAK3, AP-1, STAT, MAPK. Has anti-proliferative and anti-invasive effect on cancer cells.

Phosphodiesterase PDE4 inhibitor

Bortezomib is a 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 t-cell lymphomas and multiple myeloma because it prevents the binding of myeloma cells to bone marrow stroma and inhibits osteoclast differentiation. Bortezomib 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.

Lovastatin is an HMG-CoA reductase inhibitor that is used to lower LDL cholesterol levels and to aid in the management of cardiovascular diseases. Animal studies have demonstrated that this drug has vasculoprotective properties. Lovastatin 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.

Sulindac is a non-steroidal anti-inflammatory drug that has anti-inflammatory and analgesic properties. It is used to relieve the pain of osteoarthritis and rheumatoid arthritis by reducing inflammation and inhibiting the production of prostaglandins, which are chemicals that cause inflammation. Sulindac 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 PARP1 and PARP2 enzymes

Imiquimod is a toll-like receptor 7 agonist drug that is used for the treatment of genital warts, basal cell carcinoma and condyloma acuminata. This drug works by relieving and controlling wart production. Studies in mice have shown that this drug may induce cytokines such as interleukins. Imiquimod helps to increase apoptosis of diseased tissues and an infiltration of lymphocytes into tumor lesions. Imiquimod 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 5-lipoxygenase activating protein_x000D_

A potent and selective c-Met inhibitor. Anti-tumour activity demonstrated in xenograft models in vivo. Forms a thioether conjugate by reacting with thiol groups in proteins. Non-small-cell lung carcinoma (NSCLC) tumour cells that overexpress c-MET have increased sensitivity to AMG458.

Inhibits cyclin-dependent kinase 4 and 6 (CDK4 and CDK6); antineoplastic

Inhibitor of vacuolar ATP-ases

Inhibitor of p38 MAPK kinase

Diacerein is a slow-onset anthraquinone IL-1 inhibitor that is used in the treatment of joint diseases such as osteoarthritis. This drug is also being studied for the treatment of insulin resistance and diabetes mellitus. Diacerein works to decrease inflammation and cartilage destruction by reducing the level of interleukin-1. Diacerein 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.

Anti-inflammtory drug

Potent and selective inhibitor of the glycogen synthase kinase GSK-3. Promotes cell renewal in embryonic stem cells by modulating Notch, MAPK and TGF-β signalling pathways, which are involved in pluripotency. It also affects the Wnt/β-catenin pathway and alters expression of genes coding for proteins, epigenetic regulatory elements and non-coding RNAs. The combination of CHIR 99021 and basic fibroblast growth factor (bFGF) allows long-term self-renewal in adult mouse retinal progenitor cells.