Enzyme Modulators

<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>