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>Dual PI3K/mTOR inhibitor</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>Nateglinide is used to treat type 2 diabetes mellitus as an oral hypoglycemic, insulinotropic agent. It is a blocker of ATP-dependent potassium channels and works by increasing the body's production of insulin, which lowers blood glucose levels. Nateglinide has been shown to be effective in reducing postprandial blood glucose levels in patients with type 2 diabetes who have not responded well to other treatments. The effects of nateglinide are reversible.</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>Alarelin is a form of a hypothalamic peptide that is used to treat endometriosis and induce ovulation. It works by stimulating the release of follicle stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary gland.</p>

<p>Clopidogrel is a potent inhibitor of the platelet aggregation. It reduces blood clotting by inhibiting the ADP receptor on the surface of platelets, thereby inhibiting the aggregation and adhesion of platelets. Clopidogrel has been shown to be effective in preventing thrombosis, myocardial infarction (heart attack), and stroke. Clopidogrel inhibits the activity of cytochrome P450 3A4 (CYP3A4) and p2Y 12 receptors. Clopidogrel has been shown to have synergic effects with nonsteroidal anti-inflammatory drugs (NSAIDs). The polymorphic nature of Clopidogrel can be monitored using a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for quantification in biological samples such as human serum and plasma.</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>Inhibitor of VEGF receptor tyrosine kinases and non-receptor tyrosine kinases</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>Antagonist of OX1 orexin receptor</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>GYY4137 sodium, dichloromethane-free, is a slow-releasing hydrogen sulfide (H₂S) donor used in research. It is synthesized as a stable compound to deliver controlled and sustained release of hydrogen sulfide, a critical signaling molecule, in biological systems. Its mode of action involves hydrolysis, gradually liberating H₂S, thus mimicking endogenous production more closely compared to fast-releasing sulfide salts.</p>

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

<p>Apraclonidine is an alpha adrenoreceptor agonist that is used in the treatment of raised intraocular pressure. This drug’s mechanism of action is not fully understood however, animal and human studies suggested that Apraclonidine reduces aqueous humor production and increases uveoscleral outflow.</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>Pimavanserin is an atypical antipsychotic drug that is used for the treatment of symptoms associated with Parkinson’s disease. Although this drug’s mechanism of action is not fully understood, it is said to act via inverse agonist at serotonin 5-HT2A receptors to aid with the symptoms.</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>Inhibitor of ERK1 and ERK2 serine/threonine kinases</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>RET receptor tyroine kinase inhibitor</p>

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

<p>Potent inhibitor of the interaction between defective cullin neddylation protein DCN1 and NEDD8-conjugating enzyme UBC12 with IC50 of 11 nM. WS 383 blocks the DCN1-UBC12 interaction in a reversible manner, selectively inhibits Cul3/1 neddylation and induces accumulation of p21, p27, and NRF2 proteins.</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>Inhibitor of transcriptional coactivator PGC-1a; anti-diabetic agent</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>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>Inhibits VEGFR1, VEGFR2, VEGFR3, c-kit and PDGFR tyrosine kinases</p>

<p>AZD 1152 is an Aurora kinase inhibitor, which is a type of small-molecule therapeutic agent. It is derived from the pharmaceutical research conducted by AstraZeneca. Its primary mode of action involves the selective inhibition of Aurora B kinase, an enzyme crucial for the regulation of mitosis. By interfering with this enzyme, AZD 1152 disrupts the normal progression of cell division, leading to the inhibition of proliferation and induction of apoptosis in rapidly dividing cells.</p>

<p>Prostaglandin D2 receptor antagonist</p>

<p>Androgen receptor antagonist; anti-cancer agent</p>

<p>Serotonin uptake inhibitor; anti-depressant</p>

<p>Albuterol is a selective beta-2 adrenergic receptor agonist drug that is used to prevent and treat wheezing, shortness of breath, and other breathing difficulties caused by asthma. It relaxes the muscles in the airways, making them more open. Albuterol also has an anti-inflammatory effect.</p>

<p>Interleukin-13 human is a recombinant cytokine, which is derived from the expression of the human IL-13 gene in suitable host systems, such as E. coli or mammalian cells. This cytokine belongs to the interleukin family and plays a pivotal role in the immune response by modulating inflammatory pathways. The mode of action of interleukin-13 involves binding to specific cell surface receptors, IL-13Rα1 and IL-13Rα2, which facilitates the activation of various intracellular signaling cascades, including the JAK/STAT pathway. This promotes the differentiation and proliferation of certain immune cells, influencing the production of IgE and contributing to the regulation of inflammatory responses.</p>

<p>O6-Benzylguanine is a guanine analog that is an antineoplastic agent. It works by acting as a suicide inhibitor of the enzyme O6-alkylguanine-DNA alkyltransferase. This results to an interruption of DNA repair so that damage can occur to local tumor targets.</p>

<p>Inhibits multiple receptor tyrosine kinases (RTKs), including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl. Sitravatinib inhibits proliferation of sarcoma cells and reduced tumor growth in vivo. Promotes immune response in tumor microenvironment and enhances sensitivity to immune checkpoint inhibitors. This compound is undergoing several clinical trials as a potential anti-cancer therapeutic agent.</p>

<p>ÎŽ opioid receptor agonist; anti-nociceptive; anti-depressant</p>

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

<p>Ranitidine is classified as a histamine antagonist that reduces gastric acid section by blocking the H2- receptor. It decreases the amount of acid in the stomach. It is used to treat conditions such as ulcers, Zollinger-Ellison syndrome and GERD.</p>

<p>Arbutin or alpha-arbutin is a natural product. It is a hydroquinone glucoside with antioxidant properties. It is widely used in cosmetics as depigmenting agent, acting as an inhibitor of tyrosinase in melanocytes. Arbutin acts by supressing the enzymes that stimulate these melanocytes without killing or fully inhibiting them. As a consequence, melanin production is decreased to avoid hyperpigmentation that might be caused by an excess of UV radiation or a higher activity of tyrosinases.</p>

<p>MET tyrosine kinase inhibitor; anti-proliferative; pro-apoptotic</p>

<p>Droperidol is a butyrophenone derivative, which is an antipsychotic agent and antiemetic medication, sourced from synthetic chemical processes. Its mode of action involves antagonism of dopamine D2 receptors in the central nervous system, particularly in the chemoreceptor trigger zone of the brain, and it also possesses some alpha-adrenergic blocking properties.</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>PMX 53 TFA is a synthetic cyclic peptide, which is derived from the advanced study of complement system interactors. This product, sourced from specialized peptide synthesis methodologies, functions through the inhibition of the C5a receptor, a key player in the immune response. By blocking this receptor, PMX 53 TFA modulates inflammatory pathways, effectively reducing overactive immune responses associated with various pathological conditions.</p>

<p>Tazarotene is an acetylenic retinoid that is used for the treatment of wrinkles, pigmentation of the skin and acne. Although, the mechanism of action for this drug is not yet fully understood, it is thought to bind to all three members of the retinoic acid receptor family. Studies have shown that this drug is associated with increased collagen production.</p>

<p>Potent and selective MAP/ERK kinase 1/2 inhibitor. Reduces growth of tumor cells with B-Raf and Ras mutations. Tumor regression observed after chronic treatment in in vivo xenograft models. Enhances anti-tumor effect in combination with irinotecan or docetaxel.</p>

<p>A potent inhibitor of CETP that inhibits transfer of cholesteryl esters and triglycerides. Raises HDL cholesterol levels whilst lowering LDL cholesterol. Reduces cardiovascular events in patients with atherosclerotic vascular disease that receive statin treatment.</p>

<p>Thioglycosyl Naphthalimide is a highly potent human O-GlcNAcase (hOGA) inhibitor with good selectivity against human β-N-acetylhexosaminidase B (HsHexB).</p>

<p>Prostaglandin E1 analog; agonist of EP2, EP3 and EP4 receptors</p>

<p>Fingolimod is a sphingosine 1-phosphate receptor modulator that is used in the treatment of relapsing-remitting form of multiple sclerosis. It is also being studies to manage lung complications in patients with COVID-19. This drug binds to various sphingosine 1-phospahte receptors and suppresses the exit of lymphocytes from lymph nodes.</p>

<p>NMDA glutamate receptor antagonist</p>

<p>Semaglutide is a peptide that is used as a pharmacological agent for the treatment of type 2 diabetes, and other diseases and is also used for long-term weight management in obesity. It is an analogue of glucagon-like peptide-1 (GLP-1) and acts as a GLP-1 receptor agonist and inhibitor of the enzyme DPP-4, which is responsible for the degradation of GLP-1. As a result, semaglutide increases levels of GLP-1, which stimulates insulin release from pancreatic beta cells. Semaglutide has been shown to reduce body weight, blood pressure and HbA1c levels in patients with type 2 diabetes, through its action to increase insulin production and inhibit the production of glucagon. Semaglutide acetate 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.Cymit Quimica provides this product solely for uses within the scope of any statute or law providing for an immunity, exemption, or exception to patent infringement (“Exempted Uses”), including but not limited to 35 U.S.C. § 271(e)(1) in the United States, the Bolar type exemption in Europe, and any corresponding exception to patent infringement in any other country. It is the sole responsibility of the purchaser or user of this product, and the purchaser or user of this product agrees to engage only in such Exempted Uses, and to comply with all applicable intellectual property laws and/or regulations. The purchaser of this product agrees to indemnify Cymit Quimica against all claims in connection with the performance of the respective commercial agreement (e.g. supply agreement) and possible infringements of intellectual property rights.</p>

<p>Oxybutynin is an antimuscarinic agent that is used to aid the bladder in relaxing and preventing the urge to void. This drug is used in the treatment of an overactive bladder and reduces detrusor muscle activity. Oxybutynin works by inhibiting the action of acetylcholine on smooth muscle.</p>

<p>Androgen receptor antagonist</p>

<p>Atenolol is a beta-blocker that slows the heart rate and decreases the force of contraction, which reduces the workload on the heart. Atenolol has been shown to be effective in lowering blood pressure in people with chronic kidney disease who are not taking angiotensin-converting enzyme inhibitors. It is also used to treat hypertension and chronic angina.</p>

<p>mTOR serine/threonine kinase inhibitor</p>

<p>AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with binding affinity of 1.6 nM, 6-fold selective for MTC1 over MCT2.</p>

<p>Pemirolast is an antihistamine drug that is used for the treatment of allergies such as hay fever and allergic conjunctivitis. This drug binds to the histamine H1 receptor and blocks the action of histamine which results in the relief of allergic symptoms brought on by histamine. This drug is also a mast cell stabilizer.</p>

<p>Metabotropic glutamate receptor subtype-5 antagonist</p>

<p>Inhibitor of CDK4/6 serine/threonine kinases; antineoplastic</p>

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

<p>Calcium channel blocker</p>

Potent and selective inhibitor of the glycogen synthase kinase GSK-3. Promotes cell renewal in embryonic stem cells by modulating Notch, MAPK and TGF-β signalling pathways, which are involved in pluripotency. It also affects the Wnt/β-catenin pathway and alters expression of genes coding for proteins, epigenetic regulatory elements and non-coding RNAs. The combination of CHIR 99021 and basic fibroblast growth factor (bFGF) allows long-term self-renewal in adult mouse retinal progenitor cells.

<p>A selective inhibitor of glial glycine transporter type 1 (GlyT-1b). It has no considerable affinity for noradrenaline, dopamine, serotonin and GABA receptors. Increases amplitude of electronically evoked NMDA receptor-mediated glutamatergic excitatory postsynaptic current (eEPSCs). This raises glycine levels in spinal cord slides and extends the duration of current at glycinergic synapses.</p>

<p>Abiraterone is an antiandrogen drug used in the treatment of metastatic prostate cancer. It is a derivative of steroidal progesterone. This drug inhibits the enzyme CYP17 irreversibly, thus inhibiting the synthesis of androgen. It specifically inhibits the conversion of 17-hydroxyprognenolone to dehydroepiandrosterone to decrease serum levels of testosterone and other androgens.</p>

<p>Topoisomerase II inhibitor; chemotherapeutic drug</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>Agonist of H3 and H4 receptors</p>

<p>Inhibits type III tyrosine kinases (PDGFRα, PDGFRβ, FLT3)</p>

<p>Inhibitor of VEGFR; antineoplastic</p>

<p>FP receptor ligand; activator of PGF2αR</p>