Modulateurs d'enzymes

<p>Inhibits multiple protein kinases, such as PKC and FLT3</p>

<p>Inhibitor of VEGF receptors</p>

<p>Dabigatran is an anticoagulant that is used for the treatment of atrial fibrillation and prevention of venous thromboembolic events. It is a drug that acts as an inhibitor of the enzyme thrombin. Dabigatran inhibits platelet activation and aggregation, which reduces the risk of stroke or other vascular events. Dabigatran is a prodrug and does not have any activity in its active form.</p>

<p>Anti-rheumatic; immunosuppressant; neuroprotective; neuroregenerative</p>

<p>Inhibitor of glutaminase; glutamine analogue</p>

<p>Inhibitor of VEGFR; antineoplastic</p>

<p>PD 168393 is a potent and selective irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It is synthesized through advanced chemical processes, designed to specifically target and covalently modify the ATP-binding site of EGFR. The mode of action involves the irreversible binding to the cysteine residue in the ATP-binding pocket, leading to the inhibition of EGFR autophosphorylation and subsequent downstream signaling pathways.</p>

<p>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.</p>

<p>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.</p>

<p>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.<br>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&amp;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.</p>

<p>Potent and irreversible inhibitor of phosphoinositide-3-kinase (PtdIns-3-kinase) with IC50 of 0.1 nM. PX 866 inhibited cell motility and growth of 3D spheroids of glioblastoma, breast, prostate and colon cancer cell lines at low nanomolar concentrations. PX 866 also exhibited anti-tumoral activity in vivo in xenograft models for ovarian and lung cancer.</p>

<p>Amlexanox is an antiallergic and anti-inflammatory drug that has been shown to be effective in treating rhinitis and allergic asthma in clinical studies. It prevents the slow-reacting substance of anaphylaxis (SRS-A) from being released chemically as a mediator and may have antagonistic effects on interleukin-3.</p>

<p>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.</p>

<p>Sulbactam is a synthetic antibacterial agent that inhibits bacterial cell wall synthesis. Sulbactam is a potent inhibitor of bacterial DNA-dependent RNA polymerase. The combination of sulbactam and polymyxin B has been shown to have synergistic inhibitory effects on Gram-negative bacteria and is used as an intravenous antibiotic for the treatment of infections caused by Gram-negative bacteria.</p>

<p>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.</p>

<p>Inhibits histone deacetylase (HDAC)</p>

<p>Inhibitor of BCR-ABL1 kinase</p>

<p>Teniposide is a cytotoxic drug that is used in the treatment of refractory childhood acute lymphoblastic leukemia. It has antitumour activity. It is a type II topoisomerase inhibitor. This drug inhibits DNA synthesis by forming a complex with topoisomerase II and DNA.</p>

<p>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.</p>

<p>Inhibitor of ALK1, ALK2, ALK3 and ALK6 kinases and bone morphogenetic protein (BMP) pathway. LDN 1931189 is a dorsomorphin derivative that inhibits BMP-mediated activation of Smad, Akt and p38 signalling. LDN 193189 promotes differentiation of human pluripotent cells into PAX6+ anterior neural ectoderm. In combination with basic fibroblast growth factor (FGF2), LDN 193189 promotes differentiation of mouse pluripotent stem cells into inner ear sensory epithelium.</p>