Modulateurs d'enzymes

Carmofur is an antineoplastic agent that is used to treat various cancers such as breast and colorectal cancer. This drug is a derivative of fluorouracil. Carmofur is an inhibitor of the human acid ceramidase, a lysosomal amidase involved in the development of cancer cells. Carmofur 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.

HMG-CoA reductase inhibitor

Inhibitor of Abl and Src kinases; anti-proliferative; antineoplasticÂ

Toceranib phosphate is a receptor tyrosine kinase inhibitor. Toceranib phosphate has been shown to be effective in the treatment of skin cancer and other types of cancer, including lung cancer and breast cancer. It is approved in the US as a treatment for canine mastocytoma (mast cell tumours).  Toceranib phosphate 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.

LRRKtide (also called moesin) is a peptide substrate for leucine-rich repeat kinase 2 (LRRK2). The sequence of LRRKtide has been derived from the ERM proteins: Ezrin (amino acids 561-573), radixin (amino acids 558-570) and moesin (amino acids 539-553). These proteins influence cytoskeletal dynamics by anchoring the cytoskeleton to the plasma membrane. LRRK2 phosphorylates LRRKtide at its Thr558 site. This peptide contains the phosphorylated threonine residue.LRRK2 is a large, ubiquitous protein of unknown function. LRRK2 has GTPase and kinase activity, and is located in multiple areas of the cell, associated with intracellular membranes and vesicular structures- suggesting LRRK2 may be involved in several cellular pathways. LRRK2 is also found in most organs and mutations in LRRK2 have been identified in Parkinson's disease.The threonine residue at position 9 of this peptide has been phosphorylated.

Potently inhibits PARP-1 and PARP-2 enzymes, orally bioavailable and crosses blood-brain barrier. Sensitises cancer cells to DNA-damaging chemotherapy and radiotherapy. Combination therapies investigated in clinical trials for solid and blood malignancies.

Selective, potent, competitive and reversible inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) with IC50 of 2.3 nM and more than 10000-fold selectivity over the related 11β-HSD-2 isoform. BMS 823778 inhibits conversion of cortisone in cortisol and has applications in the treatment of diabetes type 2 since it can influence the occurrence of insulin resistance.

Atorvastatin is an HMG-CoA reductase inhibitor which is used to lower lipid levels and to reduce the risk of cardiovascular disease. This drug belongs to the class of medicines called statins. It lowers abnormal levels of cholesterol and lipids to reduce the risk of cardiovascular disease by inhibiting the enzyme HMG-CoA. Atorvastatin 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.

mTOR serine/threonine kinase inhibitor

Selective c-Met kinase inhibitor

Cerivastatin is a drug that belongs to the class of drugs called statins. This drug is used to reduce the risk of cardiovascular events and lower lipid levels. Cerivastatin is an HMG-CoA reductase inhibitor and allows for a decrease in cholesterol in hepatic cells. Cerivastatin is cardioprotective and anti-atherosclerotic. Cerivastatin sodium 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.

Leflunomide is a pyrimidine synthesis inhibitor drug that is used to treat rheumatoid arthritis. Although its mechanism of action is not fully determined, this drug has shown to interfere with cell cycle progression by inhibiting dihydroorotate dehydrogenase and has shown antiproliferative activity. As a result of this, it interferes with the expansion of activated autoimmune lymphocytes. Additionally, Leflunomide is a tyrosine kinase inhibitor. Leflunomide 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 EIF2AK3/PERK kinases

Specific inhibitor of glycogen synthase kinase 3 (GSK-3) with IC50 in low nanomolar range. Studies showed that BIO maintains self-renewal in embryonic stem cells (ESCs) as well as increases activity of β-catenin. In neonatal cardiomyocytes, BIO promotes cell cycle by stimulating cell entry into S phase as well as cytokinesis. In germline stem cells from female mice (FGSCs), BIO promoted proliferation and maintenance of FGSCs by activating β-catenin and up-regulating E-cadherin.

Perindopril t-butylamine salt inhibits the angiotensin converting enzyme (ACE) to prevent the conversion of angiotensin I to angiotensin II. When used in drug formulations, it has been shown to decrease blood pressure in patients with congestive heart failure. Perindopril also has an effect on the renin-angiotensin system, which regulates blood pressure and fluid homeostasis by promoting vasoconstriction and increasing salt and water retention. Perindopril t-butylamine 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.

Sildenafil is a pharmaceutical compound, which is a synthetic product derived from chemical processes. It functions as a selective inhibitor of the enzyme phosphodiesterase type 5 (PDE5). By inhibiting PDE5, sildenafil increases cyclic guanosine monophosphate (cGMP) levels within the smooth muscle cells of the corpus cavernosum. This leads to smooth muscle relaxation and vasodilation, allowing increased blood flow and facilitating penile erection in the presence of sexual stimulation. Primarily, sildenafil is used in the treatment of erectile dysfunction (ED) and is also prescribed for pulmonary arterial hypertension under different brand names. The compound's efficacy in treating ED arises from its ability to enhance the natural erectile response to sexual arousal by modulating the nitric oxide-cGMP pathway, crucial for vascular regulation. Published studies have demonstrated its effectiveness and safety profile, making it a widely utilized therapeutic option in clinical settings. The pharmacokineteics of sildenafil underscore its relevance by ensuring rapid absorption and a preferable half-life, which defines its dosage regimen and therapeutic window.

Brain-penetrant inhibitor of anaplastic lymphoma kinase (ALK) and proto-oncogene kinase ROS1. It is a reversible ATP-competitor, interacting with P-loop (L1122, G1123, V1130) and K1150 residue of ALK tyrosine kinase. It has major implications in the treatment of non-small cell lung cancer (NSCLC). The compound is used for resensitization of drug resistant, ALK-mutated cancers to crizotinib chemotherapy and was shown to trigger the regression of EML40ALK-driven brain metastases.

Inhibitor of beta-lactamase enzymes

Inhibitor of COX-2 and PDE4 enzymes; NSAID of coxib class

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.