Enzyme Modulators

<p>(S)-Mephenytoin is a substrate of cytochrome P450 enzyme CYP2C19 (a hydroxylase). It is an effective anticonvulsant that improves control of seizures in patients. According to studies, the drug exhibits a genetic polymorphism in CYP2C19 that results in reduced metabolism in some individuals.</p>

<p>Analeptic</p>

<p>BRAF kinase inhibitor; antineoplastic</p>

<p>Kifunensine is a small molecule inhibitor that was designed and synthesized to inhibit plant and animal α-mannosidase I. It is a potent and specific inhibitor with IC50 in nanomolar range. It inhibits the enzyme isoforms in Golgi apparatus (GMI) and endoplasmatic reticulum (ERMI). The compound prevents mannose trimming on glycoproteins and shifts the glycoform content from complex to oligomannose type. Used for the production of recombinant therapeutic glycoproteins with mannose rich N-linked glycans.</p>

<p>A small molecule inhibitor with high selectivity for CDK8 over CDK19. Increases IL-10 production in stimulated human and murine macrophages and dendritic cells. Modulatory action on inflammatory responses has therapeutic potential.</p>

<p>A brain-penetrant inhibitor of leucin-rich repeat kinase 2 (LRRK2) with IC50 = 0.76 nM and anti-parkinsonian activity. Gain-of-function mutations in LRRK2 gene lead to increased familial and idiopathic risk of developing the disease. The inhibitors of the kinase activity have therapeutic potential against Parkinson’s disease.</p>

<p>Inhibitor of caspases; broad spectrum</p>

<p>Inhibitor of c-Met kinase</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.<br>Sorafenib 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>Seratrodast is a thromboxane receptor antagonist that is used to treat asthma. However, this drug does not affect thrombus formation as other thromboxane synthase inhibitors do such as ozagrel.</p>

<p>Lumiracoxib is a COX-2 selective non-steroidal anti-inflammatory drug that is used for the treatment of osteoarthritis. This drug inhibits prostaglandin synthesis via inhibition of COX-2.</p>

<p>Receptor tyrosine kinase inhibitor; anti-angiogenesis; anti-oncogenesis</p>

<p>Afatinib is a small molecule that inhibits the activity of cellular kinases that are involved in the progression of cancer. It is an Irreversible inhibitor of three members of the ErbB family. This molecule binds covalently to cysteine 797 residue in HER2 and blocks downstream cellular signalling which inhibits cellular growth and promotes apoptosis. It has been researched for the treatment of non-small cell lung cancer (NSCLC), breast cancer, pancreatic cancer and colorectal cancer.</p>

<p>Camostat is a serine protease inhibitor that is used for the treatment of chronic pancreatitis. This drug has shown to reduce inflammation and pain. Studies have shown that Camostat has also inhibited the entry of SARS-CoV-2 in lung cells by inhibiting the priming process of S-protein, necessary for the viral entry into host cells.</p>

<p>LOXO-305 is a small molecule inhibitor, which is a synthesized chemical compound designed to selectively target specific enzymes or pathways. Its source is rooted in medicinal chemistry and pharmacological research aimed at elucidating pathways involved in oncogenesis.</p>

<p>R-(-)-Arundic acid is a chiral compound, which is a derivative of arundic acid specifically designed for enantiomeric purity. It is sourced through synthetic organic chemistry processes, allowing for precise control over its stereochemistry. The mode of action of R-(-)-Arundic acid involves the inhibition of astrocyte activation by modulating the synthesis of certain cytokines and inflammatory mediators. This mechanism provides a neuroprotective effect, making it a valuable tool in the study of neurodegenerative diseases and brain injuries.</p>

<p>Anastrozole is a non-steroidal drug that belongs to the class of aromatase inhibitors. It inhibits the production of estrogen by blocking the conversion of androgens to estrogens in peripheral tissues. The drug has been shown to be effective in treating breast cancer in postmenopausal women. In vitro assays have shown that Anastrozole can inhibit tumor growth as well as induce apoptosis in human serum cells, which suggests that it may be effective against a variety of cancers.</p>

<p>VEGFR2 a tyrosine kinase receptor inhibitor; antineoplastic</p>

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

<p>BRK tyrosine kinase (PTK6) inhibitor; anti-proliferative in breast cancer cells</p>