Modulateurs d'enzymes

Abiraterone is an anti-cancer drug that has been shown to be effective in treating prostate cancer. It works by blocking the production of testosterone by inhibiting androgen synthesis. Abiraterone does this by inhibiting CYP17A1, which converts cholesterol into pregnenolone, and then into progesterone and testosterone. Furthermore, it binds to the enzyme steroid 5-alpha reductase, which converts testosterone into dihydrotestosterone (DHT). Abiraterone is usually a last resort for patients who have stopped responding to other lines of hormone therapies, which is known as second-line therapy. Abiraterone 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 MEK1/2 kinase enzymes; antineoplastic

1-NM-PP1, also known as 1NM-PP1, is an inhibitor of the Src kinase. Studies have shown that 1-NM-PP1 inhibits analog-sensitive kinases (as-kinases) characterised by a small amino acid as gatekeeper of the ATP binding site. Tested to prevent parasitic infections, 1-NM-PP1 inhibited the Toxoplasma gondii life cycle when used at a higher concentration than 500 nM.

Anti-folate inhibitor of thymidylate synthase

A selective and ATP-competitive inhibitor of mTOR kinase with an IC50 value of 0.8 nM. Inhibits growth of a range of tumor types in vivo and in vitro. Effective in preventing and treating endocrine-resistant breast cancer. Causes autophagy in H838 and A549 cells.

ERKtide Substrate Peptide.

Rosuvastatin is a synthetic lipid-lowering agent, which is a product of pharmaceutical manufacturing derived from extensive research in cardiovascular pharmacology. It functions as an HMG-CoA reductase inhibitor, effectively blocking the enzyme responsible for cholesterol biosynthesis in the liver. By inhibiting this enzyme, Rosuvastatin reduces the production of cholesterol, especially low-density lipoprotein (LDL) cholesterol, which is known to contribute to atherosclerosis. Its primary use is in the management of hypercholesterolemia and related conditions, aimed at reducing cardiovascular morbidity and mortality. Clinical studies have demonstrated its efficacy in not only lowering LDL cholesterol but also in raising high-density lipoprotein (HDL) cholesterol and reducing triglycerides. Furthermore, Rosuvastatin has applications in primary prevention among patients at risk for coronary artery disease, as well as in secondary prevention in those with established cardiovascular disease. Its pharmacokinetic properties, including a long half-life and minimal drug-drug interaction, make it a well-tolerated choice among statins. Continued research is expanding its clinical applications, examining benefits beyond lipid modulation.

A potent and selective agonist of CCR4 chemokine receptor with IC50 values ranging from 10 to 25 nM across different species. CCR4 is involved in activation and migration of Th2 lymphocytes to the lungs in response to allergens. Treating sensitised rats results in reduced inflammation of lung tissue.

Aurora kinase inhibitor

Inhibitor of monoamine oxidase

Inhibitor of Flk-1/KDR receptor tyrosine kinases, a vascular endothelial growth factor receptor (VEGF) receptor expressed on precursor and mature forms of endothelial cells. SU 5416 also inhibits other tyrosine kinases, including c-KIT and FLT-3. Has therapeutic potential as an anti-angiogenic agent for the treatment of cancer.

Inhibits coagulant factor VIIa; anti-thrombotic; antineoplastic

A potent and selective inhibitor of cyclin G-associated kinase (GAK) with Ki of 3.1 nM. The compound has more than 50-fold selectivity over the closest off-target kinase RIPK2, making it a potent tool for the study of GAK biology. SGC-GAK-1 was tested in vitro in human prostate carcinoma cell lines and showed strong growth inhibition in cell lines with androgen-dependent growth.

Tipifarnib is a farnesyltransferase inhibitor, which is a synthetic compound designed for experimental cancer treatment. It functions by targeting farnesyltransferase, an enzyme involved in the post-translational modification of proteins through the attachment of a farnesyl group to the protein's cysteine residue. This modification is crucial for the activity of several proteins, including those in the Ras signaling pathway, which is often dysregulated in cancer. By inhibiting farnesyltransferase, Tipifarnib prevents the proper functioning of these proteins, thereby disrupting key signaling pathways that are essential for cancer cell proliferation and survival. This makes it a molecule of significant interest in oncology research, particularly in cancers with mutations that lead to increased Ras activity. Tipifarnib has shown promise in the treatment of various malignancies, including particular types of leukemias and solid tumors. Its efficacy as a targeted therapy reflects its potential to selectively interfere with cancer growth while minimizing damage to normal cells. The ongoing research into its applications highlights its importance in the development of more effective, less toxic cancer treatments.

Caspase Modulator I is an antibody that binds to the caspase-1 receptor. This protein regulates apoptosis by binding to, and activating, the caspases. Caspase Modulator I can be used as a research tool for studying the molecular mechanisms of apoptosis. It may also be used in pharmacology as an inhibitor or activator of caspases.

Inhibitor of PIP5K1C

Inhibitor of human neutrophil elastase

Cetilistat is a drug that is used to treat obesity. This drug inhibits the enzyme pancreatic lipase and so it prevents triglycerides from being hydrolyzed into absorbable free fatty acids. Cetilistat 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.

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-56 predominantly contained 3 peptides - SDNRNQGY, KGLWE, and IQVPL. KGLWE in EYGF-56 was found to have very strong antioxidant activity. KGLWE showed minimal angiotensin converting enzyme (ACE) inhibitory activity.

Bruton's tyrosine kinase antagonist; reduces Fcγ receptor signaling

Farnesyltransferase inhibitor

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.

PI3K/mTOR kinase inhibitor; anti-neoplastic

Carbimazole is an imidazole antithyroid agent that is used to treat hyperthyroidism. It reduces the production of diiodotyrosine and thyroxine, as well as the uptake and concentration of inorganic iodine by the thyroid. Once it has been converted to methimazole, the thyroid peroxidase enzyme is inhibited from coupling and iodinating the tyrosine residues on thyroglobulin therefore lowering the production of the thyroid hormones T3 and T4. Carbimazole 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 MET, VEGFR2, Ron, AXL, Tie-2, Flt-1, Flt-3 and Flt-4 tyrosine kinases

Potent inhibitor of c-Met catalytic activity. Selective over other tyrosine and serine-threonine kinases (600-fold selectivity). Ability to block constitutive or HGF-stimulated phosphorylation of c-Met demonstrated in vitro. JNJ 38877605 reduces radiation-induced invasion, apoptosis and proliferation of cancer cells in vitro.

Inactive enantiomer of the inhibitor of myosin II-ATPase

MG 132 is a modified tripeptide that acts as proteasomal inhibitor. In 2006, MG 132 has been experimentally tested in in vitro cell-based and in vivo models for to assess its use in the medical treatment of Parkinson's disease.

Inhibitor of SHIP2 phosphatase

Lumiracoxib is a COX-2 selective non-steroidal anti-inflammatory drug that is used for the treatment of osteoarthritis. This drug inhibits prostaglandin synthesis via inhibition of COX-2. Lumiracoxib 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 prolyl 4-hydroxylase PHD