Enzyme Modulators

<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>

<p>First generation PI 3-kinase inhibitor</p>

<p>Inactive enantiomer of the inhibitor of myosin II-ATPase</p>

<p>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.</p>

<p>Inhibitor of Janus kinase JAK-1</p>

<p>p38α MAP kinase inhibitor; JNK2α2 protein kinase inhibitor</p>

<p>Selective and potent inhibitor of lysine acetyltransferases KAT6A and KAT6B with IC50 values in low nanomolar range. The compound is a reversible competitor of acetyl coenzyme A domain of KAT6A/B enzymes. It inhibits MYST-catalysed histone acetylation and was shown to arrest lymphoma progression in mice models. The compound opened the door to a new class of cancer therapeutics that could potentially direct the cancer cells in senescence or permanent dormancy.</p>

<p>CAY10727 is a potent biochemical inhibitor, which is derived from synthetic sources with specific action targeting cyclooxygenase-2 (COX-2) enzymes. It functions by selectively blocking the enzymatic activity of COX-2, which plays a critical role in the biosynthesis of prostaglandins involved in inflammatory responses. This targeted inhibition allows the study of COX-2-related pathways without interference from COX-1, which is significant for maintaining gastrointestinal integrity.The use and applications of CAY10727 are primarily in research settings where understanding the pathways involved in inflammation, pain, and cancer progression are critical. This compound is utilized in various in vitro experiments to delineate the role of COX-2 in cellular and molecular contexts, enabling scientists to dissect complex signaling networks. Given its specificity, CAY10727 is instrumental in the development of new therapeutic approaches where selective COX-2 inhibition might offer benefits over non-selective inhibitors.</p>

<p>N-(5-Aminopentyl) methotrexate amide-LC-biotin is a specialized bioconjugate, derived through the conjugation of methotrexate, an established antifolate drug, with an LC-biotin moiety. This product is synthesized by covalently linking methotrexate, which is known for its role in cancer therapy through the inhibition of dihydrofolate reductase (DHFR), to a biotin moiety via a long-chain spacer. The resultant bioconjugate retains the therapeutic effects of methotrexate, particularly in its ability to interrupt nucleotide synthesis, thereby affecting cell division in rapidly proliferating cancer cells.The inclusion of biotin in the structure allows for facile attachment to avidin or streptavidin-labeled systems, facilitating targeted delivery and enhanced detection in molecular and cellular studies. The primary application of N-(5-Aminopentyl) methotrexate amide-LC-biotin lies in the realm of targeted drug delivery and advanced research into methotrexate metabolism. By leveraging the high affinity of biotin-streptavidin interactions, researchers can effectively study the biodistribution and cellular uptake of methotrexate, advancing cancer therapeutic strategies and providing insights into antifolate drug mechanisms at the molecular level.</p>

<p>Inhibitor of PARP1 and PARP2 enzymes</p>