Modulateurs d'enzymes

Celecoxib is a pyrazole derivative that acts as a selective COX-2 inhibitor. It has been shown to inhibit prostaglandin synthesis and promote apoptosis in human osteosarcoma cells. Celecoxib also inhibits tumor growth and inhibits angiogenesis in combination with paclitaxel, which is a chemotherapeutic agent. It is a nonsteroidal anti-inflammatory drug, thus a beneficial treatment in conditions such as rheumatoid arthritis, osteoarthritis, musculoskeletal pain, acute pain and juvenile rheumatoid arthritis. Furthermore it can be utilized in patients with familial adenomatous polyposis to reduce colon and rectal polyps. Celecoxib 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 COX1 cyclooxygenase

Lifirafenib is a targeted anticancer therapy, which is a small molecule inhibitor sourced through pharmaceutical development processes. Its mode of action involves the selective inhibition of the RAF kinase family, including B-RAF, which plays a critical role in the MAPK/ERK signaling pathway. By targeting these kinases, Lifirafenib effectively disrupts the aberrant signaling that contributes to tumor growth and survival in certain cancers with mutations such as BRAF V600E. Lifirafenib is primarily used in the treatment of cancers with identified aberrations in the RAS/RAF/MEK/ERK pathway, including certain forms of melanoma and thyroid and colorectal cancers. This drug holds therapeutic potential due to its ability to target specific genetic alterations, thereby providing a more personalized approach to cancer treatment. As with other targeted therapies, Lifirafenib is subject to ongoing clinical trials to better understand its efficacy, tolerability, and broader applications across various oncological indications.

MAP kinase kinase (MEK) inhibitor. Binds to MEK-1, preventing phosphorylation and activation by Raf or MEK kinase. PD 098059 enhances self-renewal in stem cells. Has anti-growth and anti-proliferative effects on AML cells. Anti-apoptotic effect on AML cells observed in synergy with Nutlin-3a.

Lenvatinib is a tyrosine kinase inhibitor that is used to treat cancers such as solid tumours. This drug inhibits the activity of VEGR receptors. It also inhibits other receptors such as fibroblast growth factor. Lenvatinib 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.

Inhibitor of stearoyl-CoA desaturase SCD1 with IC50 of 6.3 nM, as measured in the SCD1-expressing human microsomes.  A 939572 exhibited anticancer activity as it reduced cell proliferation and triggered cell killing in human non-small cell lung carcinoma cells. A 939572 inhibited tumour growth in an in vivo model for gastric carcinoma and reduced the oleic acid:stearic acid ratio in mouse liver and plasma.

Inhibitor of ecto-ATPase which blocks the hydrolysis of nucleoside diphosphates and triphosphates in extracellular space. The compound inhibits NTPDase1, NTPDase 3, NTPDase 8 and NPP1and prolongs the effect of ATP on purinergic P2 receptors in environment with physiological concentrations of nucleotides. The compound has variable effectiveness as ecto-ATP inhibitor in mouse, rat, human and guineia pig tissues.

A potent Met kinase inhibitor (IC50 = 3.9 nM). Also inhibits Axl, Ron, and Tyro-3 (IC50 = 1.1, 1.8 and 4.3 nM, respectively). Anti-proliferative in Met-driven tumors in vitro and in vivo. Induces polyploidy in breast cancer cells and thereby chemoresistance.

Inhibitor of EGFR, HER2 and HER4 tyrosine kinases

Simvastatin is a lipid-lowering agent that belongs to the group of statins. It is prescribed for the treatment of hypercholesterolemia, coronary heart diseases, and other conditions related to high cholesterol levels. Simvastatin inhibits the production of 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase, an enzyme involved in the synthesis of cholesterol. Simvastatin 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.

Rivastigmine is a cholinergic agent that is used in the treatment of dementia in Parkinson’s and Alzheimer’s disease. This drug is a carbamate derivative that binds to and inactivates cholinesterase such as acetylcholinesterase and butyrylcholinesterase. This leads to an increase concentration of acetylcholine at cholinergic synapse. Rivastigmine tartrate 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.

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.

VEGFR2 a tyrosine kinase receptor inhibitor; antineoplastic

Bestatin is a competitive protease inhibitor. It inhibits aminopeptidase N and is being studied for the use and treatment for acute myelocytic leukemia. Bestatin 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.

Etoricoxib is a cyclooxygenase-2 (COX-2) inhibitor, which is a type of nonsteroidal anti-inflammatory drug (NSAID). It works by blocking the enzyme COX-2 that is involved in the production of certain hormones called prostaglandins. These hormones are involved in the inflammation (swelling and heat) associated with conditions such as arthritis. By blocking the action of the COX-2 enzyme, Etoricoxib reduces the production of prostaglandins and thus, reduces the inflammation and pain. Etoricoxib 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.

Nilotinib is a kinase inhibitor that is used for the treatment of Chronic Myeloid Leukemia (CML). This drug is also used for the treatment of CML that is resistant to imatinib. Nilotinib inhibits the tyrosine kinase activity of the BCR-ABL protein. It also inhibits PDGFR and c-kit. Nilotinib HCl 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.

Vorinostat is a histone deacetylase inhibitor which interferes with gene transcription regulatory mechanisms. It is used to treat cutaneous manifestations in patients with progressive, persistent, or recurrent cutaneous T- cell lymphoma (CTCL) following prior systemic therapies. This drug inhibits the enzymatic activity of histone deacetylases HDAC1, HDAC2 and HDAC3 (Class I) and HDAC6 (Class II). Vorinostat 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-inflammatory; inducer of P450 II B family

PAC 1 is a small-molecule apoptosis inducer, derived from synthetic sources, with a unique mode of action targeting the apoptotic pathways in cancer cells. PAC 1 functions by selectively activating procaspase-3, an inactive precursor of the caspase enzymes, which play a crucial role in the execution phase of cell apoptosis. By facilitating the conversion of procaspase-3 to its active form, PAC 1 enhances the apoptotic response in cancer cells, promoting cell death and offering potential therapeutic advantages. In scientific research, PAC 1 is utilized extensively for its ability to sensitize cancer cells to apoptosis, making it a valuable tool in the development of cancer treatments. Its applications extend to studying apoptotic pathways and evaluating cancer cell responses to therapeutic agents. The specificity of PAC 1 for cancer cells over normal cells underscores its potential as a targeted therapeutic approach. Researchers are exploring its efficacy in combination with other chemotherapeutic agents to optimize cancer treatment regimens, aiming to reduce tumor resistance and improve patient outcomes.

Angiotensin-converting enzyme inhibitor