Enzyme Modulators

<p>Moexipril is an angiotensin converting enzyme inhibitor that is used for the treatment of hypertension. This drug is a prodrug for moexiprilat and works by relaxing the blood vessels causing them to widen and lowering blood pressure. Moexipril has been shown to be effective in treating metabolic disorders such as congestive heart failure.</p>

<p>NMDA receptor antagonist</p>

<p>Pazopanib is an antineoplastic agent that is used to treat advanced renal cell cancer and advanced soft tissues sarcoma. This drug is a multitargeted tyrosine kinase inhibitor against vascular endothelial growth factor receptor 1, 2, 3 and c-kit. As a result, it increases tumor apoptosis and decreases tumor blood flow.</p>

<p>Inhibitor of MEK kinase</p>

<p>Sunitinib is a receptor tyrosine kinase inhibitor and a chemotherapeutic agent used for the treatment of renal cell carcinoma. This drug can also be used to treat gastrointestinal tumors that are resistant to imatinib. Sunitinib inhibits VEGFR1, VEGFR2, VEGFR3, PDGFR and KIT tyrosine kinases.</p>

<p>Inhibitor of EGFR receptor</p>

<p>Inhibitor of TAOK1 and TAOK2 kinases</p>

<p>Dexrazoxane is a cytoprotective drug that is used in chemotherapy to provide cardio-protection against anthracycline toxicity. It is an antimitotic agent with immunosuppressive properties. Dexrazoxane works by binding to iron in the cell, preventing it from being released. Dexrazoxane is also a catalytic inhibitor of topoisomerase II.</p>

<p>Inhibitor of protein kinase CK1</p>

<p>Inhibitor of poly (ADP-ribose) polymerase enzyme; antineoplastic</p>

<p>Carbimazole is an imidazole antithyroid agent that is used to treat hyperthyroidism. It reduces the production of diiodotyrosine and thyroxine, as well as the uptake and concentration of inorganic iodine by the thyroid. Once it has been converted to methimazole, the thyroid peroxidase enzyme is inhibited from coupling and iodinating the tyrosine residues on thyroglobulin therefore lowering the production of the thyroid hormones T3 and T4.</p>

<p>Inhibitor of PDE4 enzyme; anti-inflammatory</p>

<p>Milrinone has an application for use in the treatment of heart failure. It has been shown to increase cardiac output and decrease left ventricular end diastolic pressure (LVEDP). Milrinone also increases the amount of oxygen delivered to the tissues by increasing cardiac contractility. <br>Milrinone 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>HMG-CoA reductase inhibitor</p>

<p>Inhibits proteosomes of class peptide epoxyketone; antineoplastic</p>

<p>Abiraterone is an anti-cancer drug that has been shown to be effective in treating prostate cancer. It works by blocking the production of testosterone by inhibiting androgen synthesis. Abiraterone does this by inhibiting CYP17A1, which converts cholesterol into pregnenolone, and then into progesterone and testosterone. Furthermore, it binds to the enzyme steroid 5-alpha reductase, which converts testosterone into dihydrotestosterone (DHT). Abiraterone is usually a last resort for patients who have stopped responding to other lines of hormone therapies, which is known as second-line therapy.</p>

<p>Nitazoxanide acts as a noncompetitive inhibitor of the pyruvate: ferredoxin/flavodoxin oxidoreductases of various microorganism with Ki values between 2 and 10 μM. Nitazoxanide is clinically relevant for its broad-spectrum action to reduce the growth of bacteria, various parasites, and especially for its efficacy against the pathogen Helicobacter pylori. Nitazoxanide also has been shown to be effective in treating inflammatory bowel disease and acute enteritis caused by bacteria. In 2021, nitazoxanide was tested for the treatment of COVID-19 patients with mild symptoms due to its broad antiviral action.</p>

<p>Selective inhibitor of the mutated RET variant RETV804M, which is the anticipated drug-resistant RET mutant that can occur in tumours treated with kinase inhibitors. The compound has a biochemical IC50 of 0.02 µM and selectivity for purified RETV804M over purified RET and KDR of 3.7 and 110, respectively. The efficacy of the compound was shown also in cell cultures with IC50 of 4.4 µM, and cell assay selectivity for RETV804M over RET and KDR of 0.89 and 2.3, respectively.</p>

<p>High affinity inhibitor of glycogen synthase kinase GSK-3 with Ki of 0.6 nM. A 1070722 showed favourable characteristics for the penetration across blood brain barrier. A 1070722 was also shown to reduce the phosphorylation of microtubule-associated protein Tau.</p>

<p>Used for treatment of idiopathic pulmonary fibrosis</p>

<p>Inhibitor of IGF1 receptor</p>

<p>Inhibitor of BRAG2-mediated activation of Arf GTP-ase. In vitro experiments showed that Bragsin2 inhibits the Arf GTP-ase activation that is mediated by a nucleotide exchange factor BRAG2 in a membrane-dependent manner. Bragsin2 interacts with the PH domain of BRAG2 protein as well as membrane, which prevents the activation of lipidated Arf. Bragsin2 affects the trans-Golgi network and was shown to affect the tumour sphere in breast cancer cell lines.</p>

<p>SD 0006 is a small-molecule inhibitor, which is synthesized through specialized chemical processes. It functions by selectively inhibiting the cyclooxygenase-2 (COX-2) enzyme, which plays a significant role in the inflammatory pathway. This inhibition reduces the production of pro-inflammatory prostaglandins, ultimately leading to a decrease in inflammation.</p>

<p>mTOR kinase inhibitor; rapamycin analog; immunosuppressant</p>

<p>Perindopril t-butylamine salt inhibits the angiotensin converting enzyme (ACE) to prevent the conversion of angiotensin I to angiotensin II. When used in drug formulations, it has been shown to decrease blood pressure in patients with congestive heart failure. Perindopril also has an effect on the renin-angiotensin system, which regulates blood pressure and fluid homeostasis by promoting vasoconstriction and increasing salt and water retention.<br>Perindopril t-butylamine salt 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>Inhibitor of PI3K kinase isoforms α, δ, and γ</p>

<p>Thromboxane A2 synthetase inhibitor</p>

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

<p>Vitamin B3; antioxidant; favours cell repair</p>

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

<p>ATP-competitive inhibitor of Met and VEGFR2</p>

<p>Inhibitor of histone deacetylases</p>

<p>Inhibitor of mutant B-rafV600E protein that results in decreased proliferation of cancer cells with this mutation. Treatment of metastatic melanoma in patients harboring the V600E mutation, had improved disease outcome. This antitumor activity is enhanced when combined with MEK inhibitor trametinib.</p>

<p>GSK-126 is a potent inhibitor of histone lysine methyl transferase 2, which is encoded by the enhancer of zeste homolog 2 gene (EZH2). The EZH2 protein regulates cell cycle as it represses the Polycomb-Repressive Complex 2 (PRC2), allowing cells to divide actively. GSK-126 inhibits the EZH2 by targeting the catalytic domain (SET) of the enzyme and therefore blocks the PCR2 repression mechanism, resulting in cell proliferation arrest. The compound has shown therapeutic potential for a variety of cancers.</p>

<p>Pan-ALK receptor tyrosine kinase inhibitor</p>

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

<p>Nilotinib is tyrosine kinase inhibitor drug that is used to treat chronic myeloid leukemia (CML). It inhibits the activity of the BCR-ABL protein kinase, which is involved in the development of CML. Additionally, it inhibits PDGF and c-kit for the potential treatment of various leukemias.</p>

<p>Inhibits cyclin-dependent kinase 4 and 6 (CDK4 and CDK6); antineoplastic</p>

<p>A reversible and selective inhibitor of thrombin that rapidly binds to the catalytic site directly. Inhibits both soluble and bound forms of thrombin. Used for prophylaxis and treatment of heparin-induced thrombocytopenia type II.</p>

<p>Inhibitor of SHIP2 phosphatase</p>

<p>Aminoglutethimide is an adrenocortical steroid synthesis inhibitor that is used for the treatment of Cushing’s syndrome. This drug is an aromatase inhibitor that blocks the production of adrenal steroids. Also, this drug blocks the conversion of androgens to estrogens. Aminoglutethimide has been studied for the treatment of cancers such as breast and prostate.</p>

<p>A novel survivin suppressant with an IC50 of 0.54 nM for the negative regulation of the survivin promoter.</p>

<p>Irreversible ErbB receptor tyrosine kinase inhibitor</p>

<p>Lysine-specific demethylase 1 ( LSD1) antagonist</p>

<p>Tadalafil analogue; PDE 5 inhibitor</p>

<p>Activator of soluble guanylyl cyclase (sGC) which stimulates cGMP production and is effective in cells under oxidative stress. Ataciguat stimulates the heme-free form of the sGC enzyme via the sGC N-terminus of β1-subunit. Ataciguat can promote vasorelaxation and hypotension by restoring or potentiating the nitric oxide (NO) signalling pathway.</p>

<p>Ranolazine is a group P2 drug that reverses the pathogenic mechanism of myocardial infarction. It is used to treat chronic angina. It decreases myocardial wall tension and improves coronary blood flow. It inhibits the ryanodine receptor, which is responsible for regulating the release of intracellular calcium in cardiac and skeletal muscle cells. Furthermore, it is also effective at preventing atrial fibrillation and has been studied as monotherapy as well as in combination with other medications used to treat irregular heartbeat.</p>

<p>Inhibitor of CPT1 and CPT2 enzymes; inhibitor of mTORC1 kinase; anti-fungal</p>

<p>Potent inhibitor of c-Met catalytic activity. Selective over other tyrosine and serine-threonine kinases (600-fold selectivity). Ability to block constitutive or HGF-stimulated phosphorylation of c-Met demonstrated in vitro. JNJ 38877605 reduces radiation-induced invasion, apoptosis and proliferation of cancer cells in vitro.</p>

<p>Inhibitor of B-Raf kinase mutant</p>