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.