Ligas Organometálicas

<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>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>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>CFTR modulator</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>Tolterodine is a muscarinic antagonist drug that is used for the treatment of an overactive bladder and its conditions associated with that such as urine urgency and incontinence. This drug act as an antagonist at muscarinic receptors which results in inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.</p>

<p>Inhibitor of PI3K kinase isoforms α, δ, and γ</p>

<p>Inverse agonist of 5-HT2A serotonin receptor; anti-psychotic</p>

<p>Inhibitor of HMG-CoA reductase</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>Carboplatin is an antineoplastic alkylating agent that is used in the treatment of ovarian cancer. This drug attaches alkyl groups to nucleotides leading to the formation of monoadducts. Carboplatin’s main mechanism of action is preventing DNA strands from separating for synthesis and transcription.</p>

<p>Gastric proton pump inhibitor</p>

<p>Inhibitor of HIF1-α transcription factor and repressor of HIF1-α-regulated genes in adult and embryonic stem cell models as well as in tumoral cell lines. FM19G11 inhibits the expression of undifferentiating factors Oct4, Sox2, Nanog, and Tgf-α at transcriptional and protein level. FM 19G11 affects also epigenetic events by reducing histone acetylation and leading to repression of p300, a HIF-transcription activation co-factor.</p>

<p>Inhibitor of AKR1C3 (type 5 17β-hydroxysteroid dehydrogenase)</p>

<p>Inhibitor of ecto-ATPase which blocks the hydrolysis of nucleoside diphosphates and triphosphates in extracellular space. The compound inhibits NTPDase1, NTPDase 3, NTPDase 8 and NPP1and prolongs the effect of ATP on purinergic P2 receptors in environment with physiological concentrations of nucleotides. The compound has variable effectiveness as ecto-ATP inhibitor in mouse, rat, human and guineia pig tissues.</p>

<p>Agonist of estrogen-related receptors ERRβ and ERRγ. In primary mouse myotubes, GSK 4716 activated ERRβ/γ transcriptional activity and increased expression of mitochondrial genes.</p>

<p>Used to treat psoriasis; teratogenic</p>

<p>Inhibitor of 3β-hydroxysteroid dehydrogenase in steroid biosynthesis</p>

<p>Phosphodiesterase 5 inhibitor; anti-impotence drug</p>

<p>Inhibitor of 8-oxoguanine DNA glycosylase OGG1 with IC50 of 0.059 μM and excellent specificity over other DNA repair enzymes. OGG1 and its substrate 8-oxoguanine are involved in mutagenesis, genotoxicity, inflammation and cancer. The compound can cause accumulation of 8-oxoguanine in DNA in vitro and is a potent tool for the study of OGG1 biology.</p>

<p>Pheniramine is an antihistamine drug that is used to treat allergic rhinitis and pruritus. This drug is a histamine receptor antagonist and competes with histamine for the H1 receptor. Pheniramine aims to reduce edema, itching and redness. This drug also produces sedation by acting on the central nervous system.</p>

<p>Lomustine is an alkylating agent that is used as chemotherapy for treating metastatic brain tumors and relapsed Hodgkin’s disease in combination with radiation treatments. This drug causes alkylation and cross-linking of DNA, thus inducing cytotoxicity. Furthermore, this drug inhibits DNA synthesis.</p>

<p>Prasugrel is a thienopyridine prodrug that inhibits the enzyme ADP-dependent P2Y purinergic receptor. Prasugrel inhibits platelet aggregation and the formation of blood clots by blocking the conversion of ADP to ATP on the surface of platelets, thus preventing the release of serotonin from platelets. The reaction products formed by prasugrel are similar to those formed by clopidogrel and include hydrogen sulfate ions and a thiol-containing metabolite. It has also been shown to have potent cytotoxic activity against melanoma cells and anti-inflammatory properties. <br>Prasugrel 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>Tulobuterol is a drug used as a bronchodilator for the treatment and management of asthma and COPD. This drug is a long acting beta-2 adrenergic receptor agonist.</p>

<p>Omeprazole is a proton pump inhibitor (PPI) that inhibits the production of gastric acid in the stomach. This is due to Omeprazole binding through a stable disulphide bond to the H+/K+ ATPase enzyme found on parietal cells, and preventing hydrogen ion transport. Consequently, gastric acid secretion is supressed. As a PPI, Omerprazole can be used to treat disorders where gastric acid is over-secreted. Examples of these disorders are gastroesophageal reflux disease (GERD) and peptic ulcer disease.</p>

<p>Agonist of μ opioid receptor; irritable bowel disease treatment</p>

<p>Bruton's tyrosine kinase antagonist; reduces Fcγ receptor signaling</p>

<p>Rabeprazole is a proton pump inhibitor drug that is used to treat symptoms of GERD, heal gastrointestinal ulcers and eradicate Helicobacter pylori. This antiulcer drug suppresses gastric acid by inhibiting the gastric H+/K+ ATPase at the parietal cell.</p>

<p>Trkc active human is a bioengineered protein, which is a synthetic derivative of the TRKC (tropomyosin receptor kinase C) receptor. This product is derived from recombinant DNA technology, utilizing expression systems to produce a functionally active protein that mimics the natural receptor found in human cells. Its mode of action involves the specific binding and activation of neurotrophin-3 (NT-3), a critical signaling molecule in the nervous system.</p>

<p>Eliglustat is an oral medication used as a substrate reduction therapy for Gaucher disease type 1, which is an inherited lysosomal storage disorder. This product is a small-molecule inhibitor derived via chemical synthesis. Its primary mode of action involves the selective inhibition of glucosylceramide synthase, an enzyme responsible for the first committed step in glycosphingolipid biosynthesis. By reducing the production of glucosylceramide, eliglustat decreases the substrate accumulation that contributes to the pathophysiology of Gaucher disease.</p>

<p>Cisplatin, also known as cisplatinum, is a platinum-based anti-cancer agent that inhibits the EGFR, which is a receptor tyrosine kinase. It has been shown to have anti-cancer effects in melanoma cells and to inhibit tumor growth in mice. Cisplatin acts by interfering with the mechanism of DNA repairing. It loses one chloride ligand and binds to DNA to inhibit the synthesis, causing DNA damage, and thus inducing apoptosis in cancer cells. In certain studies, the use of cisplatin in combination with other metal chelators has shown improvement in the uptake of the anticancer drug. CisplatiN - Bio-X™ 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>Selective c-Met kinase inhibitor</p>

<p>Azocasein is a chromogenic substrate, which is derived from casein, with azo dye linkages. It functions by undergoing hydrolysis in the presence of proteolytic enzymes, resulting in the release of soluble azo dye fragments that can be quantified spectrophotometrically. This mode of action allows for the measurement of protease activity by evaluating the intensity of the color change, typically at an absorbance wavelength of around 350-440 nm.</p>

<p>Induces expression of Oct3/4 transcription factor</p>

<p>HS-1371 is a selective chemical inhibitor targeting specific enzymes, which is derived from synthetic organic compounds with a high affinity for its target proteins. It functions by selectively binding to the active site of the enzyme, inhibiting its activity and subsequently influencing downstream signaling pathways within the cell. This mode of action allows researchers to dissect complex biochemical pathways and assess the impact of enzyme inhibition on cellular functions.</p>

<p>Carbamazepine is an anticonvulsant that is used to treat epilepsy and nerve pain from trigeminal neuralgia. The mechanism of action for Carbamazepine is not well understood but it is theorized that carbamazepine reduces seizure activity by preventing sodium channel activation. This interaction reduces the frequency and duration of sodium channel opening, slowing down nerve impulses and helping to prevent seizures Studies on animals have shown that carbamazepine works by reducing polysynaptic nerve response and preventing post-tetanic potentiation.</p>

<p>Gefitinib is an inhibitor of the epidermal growth factor receptor (EGFR) protein. This inhibition is on the EGFR tyrosine kinase domain, where Gefitinib bindings to the ATP-binding site. As a a tyrosine kinase inhibitor, Gefitinib blocks tumor growth and has led to its use in slowing the progression of non-small cell lung cancer. Gefitinib also inhibits invasion and metastasis through inhibition of macrophage receptor interacting protein kinase 2 (RIPK2), rather than EGFR.</p>

<p>Temozolomide is an imidazotetrazine alkylating agent. It has anti-tumor activity against a broad spectrum of tumors, such as leukemias, lymphomas and solid tumors. Temozolomide induces G2/M arrest, preventing cells from entering mitosis and, therefore, apoptosis. As a drug resistance-modifying agent it is used for studying drug resistance mechanisms in glioblastoma cell lines.</p>

<p>BDP 37 is a type of boron-dipyrromethene (BODIPY) dye, which is a class of fluorescent compounds known for their stability and brightness. These dyes are synthetic, designed for optimal photophysical properties, and are synthesized through the condensation of pyrrole derivatives with boron difluoride. BDP 37 operates by absorbing light and emitting fluorescence, a process facilitated by its delocalized electron system, which results in a high quantum yield and exceptional photostability. This makes it particularly well-suited for applications requiring long exposure to light.</p>

<p>Platinum-based anti-tumor drug</p>

<p>Synthetic antineoplastic agent</p>

<p>Solifenacin is a muscarinic antagonist drug that is used to treat symptoms associated with an overactive bladder such as urine urgency and urinary incontinence. This drug has high affinity for M1, M2 and M3 receptors, with its highest being for M3 receptors. Antagonism of these receptors prevent contraction of smooth muscles in the bladder.</p>

<p>Aryl hydrocarbon receptor (AhR) agonist</p>