Modulateurs d'enzymes

N-alpha-Benzoyl-L-argininamide is a synthetic compound that is used as an enzyme inhibitor. It binds to the active site of proteases, thereby inhibiting their activity. This drug has been shown to inhibit the activities of phosphodiesterase and phosphatase enzymes in vitro. N-alpha-Benzoyl-L-argininamide also inhibits the proteolytic degradation of hippuric acid and casein in vitro. The binding affinity for this drug is due to its structural similarity with substrates such as glutamate and rhizosphere exudates.

Pemetrexed is an antifolate drug that is used to treat mesothelioma and non-small cell lung cancer. It is used during chemotherapy and sometimes used in conjunction with cisplatin. This drug disrupts folate-dependent metabolic activities essential for cell replication. In vitro studies have shown that Pemetrexed inhibits thymidylate synthase. Pemetrexed disodium 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.

Inhibitor of myosin?II?specific ATPase which blocks the myosin heads in an actin-detached state, disrupts contractility of myosin-actin filaments and stabilizes super-relaxed state of muscle fibres. It inhibits skeletal muscle myosin, non-muscle myosin II and heart muscle myosin.

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 8-oxoguanine DNA glycosylase OGG1 with IC50 of 0.059 μM and excellent specificity over other DNA repair enzymes. OGG1 and its substrate 8-oxoguanine are involved in mutagenesis, genotoxicity, inflammation and cancer. The compound can cause accumulation of 8-oxoguanine in DNA in vitro and is a potent tool for the study of OGG1 biology.

Dual COX/5-LO inhibitor; anti-inflammatory; analgesic

Inhibitor of LRRK2 kinase

Inhibits MET, VEGFR1, VEGFR2; VEGFR3 receptor tyrosine kinases; antineoplastic

Linagliptin is a dipeptidyl peptidase-4 inhibitor drug that is used to manage hyperglycaemia in patients with type 2 diabetes. This drug works by inhibiting the enzyme dipeptidyl peptidase-4 and allows for the breakdown of GLP-1 and glucose dependent insulinotropic polypeptide. As a result of this, breakdown of glycogen is reduced and release of insulin is increased. Linagliptin 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.

Masitinib is an orally bioavailable inhibitor of c-Kit, PDGFR and FGFR3 tyrosine. It is an antineoplastic which has been studied for applications in a range of human diseases including Alzheimers and cancer and is currently used to treat mast cell tumours in animals. As part of a screening study, Masitinib was shown to be highly effective in blocking SARs-CoV-2 replication.

ERKtide Substrate Peptide.

Inhibitor of activin receptor-like kinases (ALK4, ALK5 and ALK7), members of TGFβ type I receptor family. Blocks activin- and TGFβ-mediated signaling and phosphorylation of Smad2 downstream. Suppresses tumor-promoting and tumor-suppressing effects of TGFβ. Promotes differentiation of human embryonic stem cells (hESCs), whilst sustaining mouse ESCs in the undifferentiated state.

Competitive inhibitor of ceramide-glycosyltransferase used for substrate reduction therapy in lysosomal storage disorders. It inhibits glucosylceramide synthase, which catalyses the initial step in glycosphingolipid biosynthetic pathway. This compound delays the onset of symptoms in type 1 Gaucher disease, Sandhoff disease and Tay-Sachs disease. It also reduces brain abnormalities in mucolipidosis type IV.

Neuronal selective nitric oxide synthase inhibitor

Tirofiban is a platelet aggregation inhibitor drug that is used for the prevention of thrombotic events in acute coronary syndrome. This drug is an antagonist of fibrinogen and inhibits it from binding to the glycoprotein IIb/IIIa receptor. As a result of this, Tirofiban blocks the blood from clotting during a cardiovascular event. Tirofiban 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.

Inhibitor of HMG-CoA reductase

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.

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.

Sunitinib is a tyrosine kinase inhibitor drug. It is a drug that is used as a treatment for renal cell carcinoma, gastrointestinal stromal tumor, and other solid tumors. This drug inhibits tyrosine kinases such as VEGFRs, this prevents tumour growth and pathologic angiogenesis. Sunitinib 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.

Sorafenib is a drug that belongs to the class of multikinase inhibitors. It inhibits a number of kinases, including the Mcl-1 protein, which is involved in apoptosis along with blocking picolinic acid (PA), an endogenous metabolite involved in apoptosis signal transduction. Sorafenib also binds to epidermal growth factor receptor (EGFR) on the surface of cancer cells, inhibiting the production of proteins that are required for angiogenesis, thus blocking the formation of new blood vessels. Sorafenib may also inhibit P-glycoprotein (Pgp) activity. Overall, these cytotoxic effects give Sorafenib anti-tumor properties, inhibiting angiogenesis and cellular transformation, which are the two main processes of tumor growth and metastasis. Sorafenib tosylate has been shown to be effective against a range of solid tumors such as breast, prostate and lung cancers and is also used for the treatment of metastatic colorectal cancer and renal cell carcinoma. A combination therapy group found that sorafenib was more effective when used with interferon alfa-2b for the treatment of advanced renal cell carcinoma. Sorafenib also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes.