Modulateurs d'enzymes

<p>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&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>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&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>Flavoxate is a muscarinic antagonist and spasmolytic drug that is used for the relief of conditions associatied with a lack of muscle control in the bladder such as urine urgency. This drug acts as a direct antagonist on acetylcholine receptors. This action reduces the tonus of smooth muscles in the bladder.</p>

<p>A tyrosine kinase inhibitor with potent activity against EGFR, STAT3, JAK3/STAT, JAK3/AP-1 and JAK3/MAPK. Suppresses IL-2 signaling pathway, inhibits T-cell growth and activation of JAK3, AP-1, STAT, MAPK. Has anti-proliferative and anti-invasive effect on cancer cells.</p>

<p>Serine protease inhibitor</p>

<p>Nociceptin/orphanin FQ peptide receptor antagonist</p>

<p>Inhibits Akt translocation by targeting the pleckstrin homology (PH) domain. Inhibits hepatitis C virus NS5B RNA-dependent RNA polymerase (IC50 = 79 µM). Attenuates cannabinoid agonist-mediated proliferation of neural stem/precursor cells.</p>

<p>Multi-kinase inhibitor; inhibits epoxide hydrolase; antineoplastic</p>

<p>SU 3327, originally introduced as a thiadiazole JNK inhibitor (De et al. 2009) has recently been identified as having antibiotic activity against a broad range of bacteria including drug-resistant gram positive and negative strains (Strokes et al. 2020). This molecule has been given the fictional name ‘Halicin’ inspired by the AI approach used to discover its novel biological activity.</p>

<p>Angiotensin-converting enzyme inhibitor; antioxidant</p>

<p>MG 132 is a modified tripeptide that acts as proteasomal inhibitor. In 2006, MG 132 has been experimentally tested in in vitro cell-based and in vivo models for to assess its use in the medical treatment of Parkinson's disease.</p>

<p>1-NM-PP1, also known as 1NM-PP1, is an inhibitor of the Src kinase. Studies have shown that 1-NM-PP1 inhibits analog-sensitive kinases (as-kinases) characterised by a small amino acid as gatekeeper of the ATP binding site. Tested to prevent parasitic infections, 1-NM-PP1 inhibited the Toxoplasma gondii life cycle when used at a higher concentration than 500 nM.</p>

<p>5-HT6 serotonin receptor antagonist; anti-convulsant</p>

<p>Farnesyltransferase inhibitor</p>

<p>Apatinib, also known as rivoceranib, is an inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR2) tyrosine kinase. Apatinib targets VEGFR2 with its action and has proven to have strong anti-tumor effects in human cancers. In studies in mice, apatinib acted as an Inhibitor of VEGFR2 and played an antiangiogenic effect. Apatinib has been suggested for the treatment of ischemia-induced proliferative retinopathy and neovascular age-related macular degeneration.</p>

<p>Inhibits acetylcholinesterase (AChE); antispasmodic agent</p>

<p>Inhibits human and mouse diacylglycerol O-acyltransferase 1 (DGAT-1) with IC50 values of 9 and 22 nM, respectively. Selective for DGAT-1 over DGAT-2 (IC50 = 53 µM), acyl coenzyme A transferase (IC50 = 296 µM) and other acyltransferases. Reduces plasma and liver triglycerides, FFA, chylomicron secretion and increases HDL cholesterol in vivo.</p>

<p>Inhibitor of protein kinases; induces apoptosis; anti-cancer</p>

<p>Aldose reductase AKR1B10 inhibitor; hepatotoxic</p>

<p>Cyclosporin B is an antifungal and immunosuppressive cyclic peptide, which is derived from the fungus *Tolypocladium inflatum*. The compound is a member of the cyclosporin family, characterized by cyclic polypeptides with a unique arrangement of amino acids that enable its biological activity. Though its precise mode of action is not completely delineated, it is observed to influence cell growth and viability by potentially disrupting cellular communication or signal transduction pathways.</p>

<p>Inhibitor of NPM-ALK kinase</p>

<p>Inhibitor of acetylcholinesterase</p>

<p>Angiotensin-converting enzyme inhibitor; anti-hypertensive</p>

<p>Inhibitor of Abl and Src kinases; anti-proliferative; antineoplasticÂ</p>

<p>PI3K enzyme inhibitor</p>

<p>Inhibitor of DNA replication; inhibitor of theophylline and caffeine metabolism</p>

<p>Selective inhibitor histone methyltransferases SUV420H1 and SUV420H2 (IC50 values = 25 nM and 144 nM, respectively). Reduces histone H4K20me2 and H4K20me3 expression whilst increasing H4K20me1 global expression. Inhibits formation of p53-binding protein 1 (53BP1) foci upon ionizing radiation and reduces NHEJ-mediated DNA-break repair.</p>

<p>Inhibitor of CKD1, CDK2, and CDK4 serine/threonine kinases</p>

<p>Inhibitor of phosphodiesterase 7</p>

<p>Inhibitor of γ-secretase and Notch signalling</p>

<p>Ligand of plasminogen; used for bleeding control</p>

<p>An active product of vitamin A metabolism. Activates RXR and RAR receptor isoforms with high binding affinity. Induces differentiation of neural stem cells into neurons.</p>

<p>Anti-folate inhibitor of thymidylate synthase</p>

<p>Sumoylation inhibitor; reported to inhibit histone acetylation transferase</p>

<p>Topoisomerase I inhibitor</p>

<p>Small molecule antagonist of heparan sulfate that binds to glycosaminoglycans electrostatically. Surfen neutralised anti-coagulant activity of unfractionated and low molecular weight heparins, inhibited enzymatic sulfation and degradation reactions. Surfen also blocked signalling and cell adhesion to fibronectin that was triggered by heparan sulphate.</p>

<p>Binds to FK506 binding proteins (FKBPs) to form a complex that inhibits mammalian targets of rapamycin (mTOR). Blocks p70 S6 kinase activation by interleukin-2 and thereby inhibits proliferation of T cells. Induces differentiation of human pluripotent stem cells (hPSCs) to mesendoderm and blood progenitor cells.</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 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>JAK2 inhibitor with potential antineoplastic activity</p>

<p>Inhibitor of HMG-CoA reductase</p>

<p>Inhibitor of Bruton's tyrosine kinase (BTK)</p>

<p>Tolcapone is a catechol-O-methyltransferase (COMT) inhibitor that is used as adjunct therapy to manage symptoms of Parkinson’s disease. Although its precise mechanism is unknown, it is thought to be an inhibitor of COMT and allows for a greater reduction in the symptoms of Parkinson’s.</p>

<p>Inhibitor of EGFR (ErbB1) and HER2 (ErbB2) receptor tyrosine kinases. Used for sensitization of HER2-overexpressing cancer cells to radiation as well as chemotherapy to tamoxifen- and trastuzumab-resistant cell lines. The compound blocks signalling via Akt and mitogen-activated protein kinase (MAPK) pathways leading to reduced cell survival. In trastuzumab resistant cancer cells, it inhibits HER2 phosphorylation, prevents receptor ubiquitination and causes accumulation of inactive HER2 dimers on the cell surface.</p>

<p>Spirapril hydrochloride is an antihypertensive agent, which is a synthetic pharmaceutical compound designed to treat high blood pressure. The compound is derived from laboratory synthesis aimed at modulating the renin-angiotensin-aldosterone system. Its mode of action involves the inhibition of angiotensin-converting enzyme (ACE), which is crucial for the conversion of angiotensin I to the vasoconstrictor peptide angiotensin II. Angiotensin II is responsible for the constriction of blood vessels and an increase in blood pressure. By inhibiting this enzyme, Spirapril hydrochloride effectively reduces vascular resistance and lowers blood pressure.</p>

<p>Inhibits factor Xa; anti-thrombotic</p>

<p>TPPB is a small molecule inhibitor, which is synthetically derived for targeted biochemical studies. It functions by selectively modulating G-protein-coupled receptor (GPCR) signaling pathways through the inhibition of specific protein-protein interactions. This mode of action makes TPPB an insightful tool for dissecting the complex mechanisms by which G-proteins relay extracellular signals to intracellular responses.</p>

<p>Inhibitor of FLT3 kinase and acid sphingomyelinase</p>

<p>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.</p>

<p>Pemetrexed is a chemotherapy drug that belongs to the class of drugs called folate antimetabolites. It is used for the treatment of various cancers such as non-small cell lung cancer and pleural mesothelioma. Pemetrexed targets the enzymes thymidylate synthase, dihydrofolate reductase and glycinamide ribonucleotide formyltransferase. The drug works by inhibiting those enzymes so that the formation of DNA and RNA is prevented.</p>

<p>Dihydrocyclosporin A is an immunosuppressant, which is a cyclic undecapeptide derived from fungal metabolites, specifically from the soil fungus Tolypocladium inflatum. This compound functions through the inhibition of calcineurin, which is a crucial phosphatase involved in the activation of T-cells. By binding to the intracellular protein cyclophilin, Dihydrocyclosporin A forms a complex that inhibits calcineurin activity, subsequently blocking the transcription of interleukin-2 and other cytokines essential for T-cell proliferation.</p>

<p>Inhibits MET, VEGFR2, Ron, AXL, Tie-2, Flt-1, Flt-3 and Flt-4 tyrosine kinases</p>

<p>Tegafur is an antineoplastic agent that is used for the treatment of gastric and colorectal cancers in combination with other medications. This drug is a prodrug of 5-fluorouracil and has anticancer properties by inhibiting thymidylate synthase during DNA synthesis. Additionally, Tegafur causes disruptions of RNA functions.<br><br>Tegafur 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>Simvastatin Na is the salt form of Simvastatin. It acts as HMG-CoA reductase inhibitor and suppresses TNF-mediated NF-kappaB activation.</p>

<p>Multi-kinase inhibitor; inhibits epoxide hydrolase; antineoplastic</p>

<p>Inhibitor of Polo-like kinase 1</p>

<p>Potent and specific inhibitor of checkpoint kinase CHK2 with IC50 of 3 nM. CCT 241533 binds to the ATP pocket of CHK2 and shows minimal cross-reactivity against related kinases. CCT 241533 blocked the activity of CHK2 and impaired DNA repair in response to DNA damage in human tumoral cell lines. The compound did not potentiate genotoxicity of several genotoxic compounds but it did potentiate the cytotoxicity of a PARP inhibitor olaparib.</p>

<p>Inhibitor of vacuolar ATP-ases</p>

<p>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.</p>

<p>Tyrosine kinase inhibitor; affects EGFR receptor; pancreatic cancer treatment</p>

<p>Synthetic phosphodiesterase inhibitor</p>

<p>Inhibitor of ADAM10 metalloprotease</p>

<p>Inhibitor of ALK4, ALK5, and ALK7 receptors</p>

<p>Inhibitor of calpain and cathepsin B</p>

<p>Inhibitor of B-Raf mutant (V600E); anti-neoplastic</p>

<p>Cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor</p>

<p>Inositol monophosphatase (IMPase) inhibitor</p>

<p>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.</p>

<p>Methotrexate is a drug that suppresses the immune system by inhibiting the production of white blood cells. It is used in the treatment of a number of diseases, including some cancers and autoimmune diseases such as rheumatoid arthritis and psoriasis. Methotrexate is metabolized to its active form, methotrexate, by an enzyme called dihydrofolate reductase (DHFR). The DHFR inhibitor activity of methotrexate blocks the synthesis of folate-dependent enzymes and prevents DNA synthesis in rapidly dividing cells. Methotrexate has been used in combination with other drugs to treat cancer. Methotrexate has also been shown to have antifungal properties against opportunistic fungal infections.</p>

<p>Antagonist of Aurora A serine/threonine protein kinase; antineoplastic</p>

<p>TDZD 8 is a selective, non-ATP competitive inhibitor of the glycogen synthase kinase GSK3β. TDZD 8 inhibits GSK3β with IC50 of 2 μM and was reported to not significantly affect Cdk-1/cyclin B, casein kinase CK-II, protein kinase A and C (PKA, PKC) activities. TDZD 8 was also identified as an inhibitor of the main protease in coronaviruses. In an in vitro study, TDZD 8 was characterised as an aggregate-based inhibitor as the presence of Triton-X decreased the inhibitory potency to Mpro protease of the SARS-CoV-2 virus (IC50 without Triton-X: 2.15 μM).</p>

<p>BIBF 1202 is a potent inhibitor of phospholipase A2, prostaglandin synthase and cyclooxygenase-2. It inhibits the production of arachidonic acid from membrane phospholipids and is used in cancer research. BIBF 1202 has been shown to have anti-tumour activity in a number of animal models, including human liver cancer cells. This molecule has also been shown to inhibit the activation of nuclear factor kappa B (NF-κB), which is involved in carcinogenesis.</p>

<p>H-9 hydrochloride is a selective protein kinase inhibitor, which is synthetically derived. It primarily inhibits cyclic nucleotide-dependent protein kinases, including protein kinase A (PKA) and protein kinase G (PKG), along with myosin light chain kinase (MLCK). The mode of action involves competitive inhibition at the ATP binding site of these kinases, thereby impacting phosphorylation pathways crucial for multiple physiological functions. The selective inhibition by H-9 hydrochloride allows for detailed exploration of kinase-mediated signaling pathways in cellular biology. Moreover, it is extensively utilized in studies involving cell motility, smooth muscle contraction, and signal transduction. The relevance of H-9 hydrochloride in academic research lies in its ability to provide insights into kinase activity modulation and its ensuing effects on cellular dynamics. This compound serves as an invaluable tool for scientists aiming to elucidate the complex role of protein kinases in health and disease, enabling the development of innovative therapeutic strategies.</p>

<p>Rosuvastatin is a synthetic lipid-lowering agent, which is a product of pharmaceutical manufacturing derived from extensive research in cardiovascular pharmacology. It functions as an HMG-CoA reductase inhibitor, effectively blocking the enzyme responsible for cholesterol biosynthesis in the liver. By inhibiting this enzyme, Rosuvastatin reduces the production of cholesterol, especially low-density lipoprotein (LDL) cholesterol, which is known to contribute to atherosclerosis.</p>

<p>Odevixibat is a pharmacological agent that functions as an ileal bile acid transport inhibitor, which is synthesized through complex organic chemistry methods to create a specific molecular structure targeting bile acid transport mechanisms. It works by inhibiting the apical sodium-dependent bile acid transporter (ASBT) in the terminal ileum. This action reduces the reabsorption of bile acids from the small intestine back into the liver, thereby reducing overall bile acid levels in the body.</p>

<p>Cyclosporine U is a cyclic polypeptide immunosuppressant, which is a derivative of the natural product Cyclosporine A, produced by the fermentation process involving the filamentous fungus *Tolypocladium inflatum*. It primarily acts by inhibiting the activity of calcineurin, a phosphatase enzyme, which in turn blocks the transcription of interleukin-2 and other cytokines. This mechanism suppresses the activation of T-lymphocytes, a crucial component in the immune response.</p>

<p>Inhibitor of GSK3β kinase</p>

<p>Anti-parasitic; pyruvate ferredoxin oxidoreductase inhibitor</p>

<p>Inhibitor of EGFR, HER2 and HER4 tyrosine kinases</p>

<p>Glucokinase activator</p>

<p>Cyclosporin G is an immunosuppressive agent, which is derived from fungal sources with a specific mode of action that involves inhibiting calcineurin. The source of Cyclosporin G is primarily from the fermentation of the fungus *Tolypocladium inflatum*. Its mode of action involves binding to the cytosolic protein cyclophilin in T-lymphocytes, which subsequently inhibits the phosphatase activity of calcineurin. This inhibition prevents the dephosphorylation and nuclear translocation of the nuclear factor of activated T-cells (NFAT), thereby reducing the transcription of interleukin-2 and other cytokines critical for T-cell activation.</p>

<p>HMG-CoA reductase antagonist</p>

<p>p38 MAP kinase antagonist</p>

<p>Inhibitor of acetylcholinesterase</p>

<p>Inhibitor of CKD1, CDK2, and CDK4 serine/threonine kinases</p>