Ligands organométalliques

<p>Inhibitor of the intracellular copper chaperones ATOX1 and CCS</p>

<p>Selective and potent inhibitor of lysine acetyltransferases KAT6A and KAT6B with IC50 values of 8 nM and 28 nM, respectively. The compound is a reversible competitor of acetyl coenzyme A domain of KAT6A/B enzymes. It inhibits MYST-catalysed histone acetylation and potentiates senescence in vitro and in zebrafish model of hepatocellular carcinoma. 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>Casein kinase (CK1ε and CK1Ύ) inhibitor</p>

<p>Neu5Ac[1Me,4789Ac]a(2-3)Gal[246Bz]-b-MP is a synthetic glycan, which is a complex carbohydrate molecule modeled after naturally occurring glycoconjugates. This product is derived through chemical synthesis in the laboratory, allowing precise control over its structure and functional groups. It consists of sialic acid (Neu5Ac) linked to galactose (Gal), with several protective acetyl (Ac) and benzyl (Bz) groups that confer stability during synthesis and ensure high specificity in its interactions.</p>

<p>Dopamine reuptake inhibitor</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>COX-2 inhibitor; anti-inflammatory</p>

<p>Diacerein is a slow-onset anthraquinone IL-1 inhibitor that is used in the treatment of joint diseases such as osteoarthritis. This drug is also being studied for the treatment of insulin resistance and diabetes mellitus. Diacerein works to decrease inflammation and cartilage destruction by reducing the level of interleukin-1.</p>

<p>Dapagliflozin is a sodium-glucose cotransporter subtype 2 (SGLT2) inhibitor that can be used in the treatment of diabetes mellitus type 2. It inhibits glucose reabsorption in the proximal tubule of the nephron and results in glycosuria, which helps to improve glycaemic control. Also, Dapagliflozin is used to lower the risk of sustained eGFR decline, end-stage renal disease, cardiovascular death, and hospitalization for heart failure in patients with chronic kidney disease who are at risk of progression.</p>

<p>Antagonist of H1 histamine receptors</p>

<p>Saha Chloroalkane T1 is a specialized chemical compound, typically categorized as a chloroalkane. It emerges from a synthetic process involving the chlorination of hydrocarbons, specifically alkanes, which serves as its primary source. The mode of action for chloroalkanes like Saha Chloroalkane T1 involves the stable incorporation of chlorine atoms, enhancing reactivity and providing versatility in chemical reactions.</p>

<p>Oxaprozin is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of osteoarthritis and rheumatoid arthritis. This drug relieves swelling and inflammation by inhibiting the enzyme cyclooxygenase which in turn inhibits prostaglandin synthesis.</p>

<p>Full antagonist to the estrogen beta receptor (ERβ) with 36-fold selectivity for the β over α receptor. ERβ is a tumour suppressor and PHTPP is a useful tool to study the biology of estrogen-dependent tumours.</p>

<p>Inhibitor of BET bromodomain; antineoplastic</p>

<p>Ibedenone is an analogue of ubiquinone that is used to treat visual impairment in patients with Leber’s Hereditary Optic Neuropathy. It is also known as an analogue of Coenzyme Q10. It has antioxidant properties. This drug increases ATP production that’s needed for mitochondrial function and reduces free radicals. It also protects the lipid membrane and mitochondria from oxidative damage.</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>Cetilistat is a drug that is used to treat obesity. This drug inhibits the enzyme pancreatic lipase and so it prevents triglycerides from being hydrolyzed into absorbable free fatty acids.</p>

<p>Inhibits binding of endogenous ligands to peroxisome proliferator-activated receptor gamma (PPARγ), blocking its activation and transcription. Unlike orthosteric antagonists GW 9662 and T 0070907, SR 16832 blocks both allosteric and orthosteric activation of PPARγ.</p>

<p>Gastric proton pump inhibitor</p>

<p>A cannabinoid receptor agonist, which binds more selectively to CB2 than CB1 receptors (1000-fold). GW833972A inhibits vagus nerve depolarization induced by tussive agents, such as hypertonic saline (EC50 = 6.5 μM), capsaicin (EC50 = 33.9 μM) or PGE2 (EC50 = 15.9 μM).</p>