Enzyme Modulators

<p>Inhibits proto-oncogene Pim kinases (Pim-1, Pim-2 and Pim-3); antineoplastic</p>

<p>Inhibitor of guanylyl cyclase</p>

<p>Omeprazole is a proton pump inhibitor (PPI) that inhibits the production of gastric acid in the stomach. This is due to Omeprazole binding through a stable disulphide bond to the H+/K+ ATPase enzyme found on parietal cells, and preventing hydrogen ion transport. Consequently, gastric acid secretion is supressed. As a PPI, Omerprazole can be used to treat disorders where gastric acid is over-secreted. Examples of these disorders are gastroesophageal reflux disease (GERD) and peptic ulcer disease.</p>

<p>LW-II-41-27 is a novel Eph receptor tyrosine kinase inhibitor used for cancer treatment.</p>

<p>NADPH oxidase inhibitor; anti-inflammatory</p>

<p>Specific inhibitor of the phosphoinositide 3-kinase (PI3K) alpha subunit with IC50 of 32 nM. In heart muscle it negatively regulates hypertrophic growth, causes increase in late sodium current and leads to arrhythmias. In tumours it inhibits the p110α subunit of PI3K and blocks growth factor signalling resulting in reduced tumour growth.</p>

<p>Inhibitor of COX-1 and COX-2 cyclooxygenases</p>

<p>Lapatinib is an antineoplastic agent used to treat breast and lung cancer. This drug is also a tyrosine kinase inhibitor and inhibits human epidermal growth factor receptor type 2 (HER2/ERBB2) and epidermal growth factor receptor (HER1/EGFR/ERBB1). Lapatinib has shown to inhibit ERBB-driven tumor cell growth in vitro and in various animal models.</p>

<p>An irreversible GSK-3β inhibitor that reduces phosphorylation of tau proteins, protects from neuronal loss and has cognitive and behavioural benefits in murine models. Studied for its potential as a therapeutic agent in Alzheimer’s disease and other neurodegenerative diseases. Tideglusib was also shown to inhibit the main protease Mpro from the SARS-CoV-2 virus with IC50 of 1.55 μM.</p>

<p>Inhibitor of human neutrophil elastase</p>

<p>Inhibitor of dihydroorotate dehydrogenase; anti-inflammatory; immunomodulatory</p>

<p>Inhibitor of CK2 protein kinase; anti-proliferative</p>

<p>A selective and potent inhibitor of phosphodiesterase 2 (PDE2). Raises cAMP and cGMP levels in neurons, improves social recognition and object memory in murine animals. Reverses anxiolytic effects induced by oxidative stress in mice by blocking cGMP-PKG signaling.</p>

<p>Vildagliptin is an antihyperglycemic agent that is used for the management of type 2 diabetes mellitus. This drug is a dipeptidyl peptidase 4 inhibitor and prevents the degradation of glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). This leads to improved glycemic control.</p>

<p>MK 886 is a leukotriene antagonist that has been studied for use in treating atherosclerosis. This drug inhibits the 5-lipoxygenase activating protein thus inhibiting 5-lipoxygenase.</p>

<p>Inhibitor of ERK1 and ERK2 serine/threonine kinases</p>

<p>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.</p>

<p>Selective inhibitor of the Src kinase family with subnanomolar IC50 values and good selectivity over c-Abl, PDGFRα and c-Kit kinases. The compound is effective in inhibiting growth in drug resistant cancer cell lines. In a recent study, it inhibited the growth of HER2-positive breast cancer cell lines which were resistant to pan-HER family kinase inhibitors such as lapatinib.</p>

<p>RET receptor tyroine kinase inhibitor</p>

<p>Rigosertib sodium is an experimental chemotherapeutic agent that is a derivative of benzyl styryl sulfone. It is synthesized chemically and functions primarily by inhibiting key signaling pathways involved in cancer cell proliferation. Specifically, Rigosertib targets the RAS signaling pathway along with the phosphatidylinositol-3-kinase/AKT and polo-like kinase 1 (Plk1) pathways, impeding the progression of the cell cycle and inducing apoptosis in malignant cells.</p>

<p>Inhibitor of cyclin-dependent kinases CDK4 and CDK6</p>

<p>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.</p>

<p>Sulindac is a non-steroidal anti-inflammatory drug that has anti-inflammatory and analgesic properties. It is used to relieve the pain of osteoarthritis and rheumatoid arthritis by reducing inflammation and inhibiting the production of prostaglandins, which are chemicals that cause inflammation.</p>

<p>Inhibits VEGFR1, VEGFR2, VEGFR3, c-kit and PDGFR tyrosine kinases</p>

<p>Inhibitor of leucine-rich repeat kinase LRRK2Â</p>

<p>Inhibitor of carbonic anhydrase; muscle relaxant</p>

<p>Lovastatin is an HMG-CoA reductase inhibitor that is used to lower LDL cholesterol levels and to aid in the management of cardiovascular diseases. Animal studies have demonstrated that this drug has vasculoprotective properties.</p>

<p>Inhibitor of LRRK2 kinase</p>

<p>Inhibitor of factor Xa</p>

<p>Inhibitor of panPI3K/mTOR</p>

<p>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.</p>

<p>Arbutin or alpha-arbutin is a natural product. It is a hydroquinone glucoside with antioxidant properties. It is widely used in cosmetics as depigmenting agent, acting as an inhibitor of tyrosinase in melanocytes. Arbutin acts by supressing the enzymes that stimulate these melanocytes without killing or fully inhibiting them. As a consequence, melanin production is decreased to avoid hyperpigmentation that might be caused by an excess of UV radiation or a higher activity of tyrosinases.</p>

<p>Nintedanib is an anti-inflammatory and anti-cancer drug. It is used for treatment of idiopathic pulmonary fibrosis. Nintedanib is a prodrug that is rapidly converted to the active form nintedanib, which inhibits angiogenesis by interfering with the activation of vascular endothelial growth factor receptor 1 (VEGFR1). <br>Nintedanib 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>5-Fluorouracil is a cytotoxic drug that inhibits the synthesis of DNA. It is used in combination therapy to treat cancer and is a pyrimidine analog. This drug inhibits the formation of thymidylate synthase from uracil. As a result, this leads to DNA and RNA synthesis inhibition and cell death.</p>

<p>A novel non-covalent inhibitor of the PLpro protease from SARS-CoV-2 and SARS-CoV viruses. GRL 0617 inhibits the proteolytic processing of the viral polypeptide. As PLpro also acts as a protease in pathways involved in innate immunity, there are indications that it can promote immunity against the virus.</p>

<p>Dipeptidyl peptidase 4 (DPP4) inhibitor</p>

<p>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.</p>

<p>mTOR serine/threonine kinase inhibitor</p>

<p>Potent and selective GSK3-β inhibitor, with IC50 value of 48 nM. Increases Nanog expression and regulates self-renewal in murine embryonic stem cells (ESCs). Induces reprograming of induced pluripotent stem cells (iPSCs) to derive cells from specific lineages.</p>

<p>Inhibitor of pan-class I PI3K family of lipid kinases; antineoplastic</p>

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

<p>Inhibitor of VEGF receptors</p>

<p>Inhibits interaction between small GTPase Rab27a and its effector JFC1 (synaptotagmin-like protein1, Slp1). These proteins regulate neutrophil exocytosis, decrease neutrophil infiltration in liver and kidneys and reduce extracellular ROS production by NAPDH oxidase. Thus, nexinhibib20 suppresses systemic inflammation.</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>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.</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>Dual IGF-1R and InsR kinase inhibitor; antineoplastic</p>