Organometallic Ligands

<p>Indomethacin is a nonsteroidal anti-inflammatory drug that inhibits the production of prostaglandin PGE2. It is used to treat pain, fever, and inflammation. Indomethacin's mechanism of action is not well understood, but it may be due to interference with the ability of PMNs to bind to the surface of bacteria or to release reactive oxygen species. The drug has been shown to reduce mitochondrial membrane potential in mammalian cells, leading to apoptosis. This effect on mitochondria may also contribute to Indomethacin's anti-inflammatory effects. Indomethacin 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>A selective and potent inhibitor of phosphodiesterase 2 (PDE2). Raises cAMP and cGMP levels in neurons, improves social recognition and object memory in murine animals. Reverses anxiolytic effects induced by oxidative stress in mice by blocking cGMP-PKG signaling.</p>

<p>Estrogen receptor degrader; therapeutic use in breast cancer</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>A specific inhibitor of Bone Morphogenetic Protein (BMP) type 1 receptors ALK2 and ALK3 (IC50  &lt; 0.5 µM). Dorsomorphin analog that exclusively targets the BMP but not VEGF signaling. It is able to inhibit the BMP-induced Smad1/5/8 activation but not the p38/MAP kinase signaling or Activin A-induced Smad2 activation.</p>

<p>LOXO-305 is a small molecule inhibitor, which is a synthesized chemical compound designed to selectively target specific enzymes or pathways. Its source is rooted in medicinal chemistry and pharmacological research aimed at elucidating pathways involved in oncogenesis.</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>Selective c-Met kinase inhibitor</p>

<p>Vipivotide tetraxetan is a radioactive therapeutic agent, which is a radioligand conjugate composed of a DOTA chelator linked to a targeting moiety. The source of this compound lies in its synthesis, where the DOTA ligand is conjugated to a peptide or small molecule that targets specific cell surface antigens expressed on cancer cells.</p>

<p>Agonist of calcium sensing receptor CASR; calcimimetic agent</p>

<p>Prostaglandin D2 receptor antagonist</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>ÎŽ opioid receptor agonist; anti-nociceptive; anti-depressant</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>Thioglycosyl Naphthalimide is a highly potent human O-GlcNAcase (hOGA) inhibitor with good selectivity against human β-N-acetylhexosaminidase B (HsHexB).</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>Androgen receptor antagonist</p>

<p>Antagonist of nociceptin receptors</p>

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

<p>5-HT1A serotonin receptor agonist; alleviates symptoms of depression</p>

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

<p>CXCR3 antagonist</p>

<p>Inhibitor of ABC transporters; oral bioenhancer for anti-cancer therapy</p>

<p>Acecelofenac is a non-steroidal anti-inflammatory drug that is used in the treatment of osteoarthritis, arthritis, and ankylosing spondylitis. This drug is also a cyclooxygenase inhibitor and works by inhibiting this enzyme so that pain and inflammation is reduced.</p>

<p>γ-secretase inhibitor; reduces amyloid-β in brainÂ</p>

<p>Inhibitor of protein kinase CK2</p>

<p>Etodolac is a non-steroidal anti-inflammatory drug (NSAID) used to treat osteoarthritis and rheumatoid arthritis. It is also used to treat acute pain. This drug works by inhibiting prostaglandin synthesis from the inhibition of the enzyme cyclooxygenase.</p>

<p>Pantoprazole is a proton pump inhibitor drug that is used to treat erosive esophagitis and promotes healing of tissue damage caused by gastric acid. It is used for the management of GERD. Through the proton pump inhibition, the formation of hydrochloric acid is inhibited thus inhibiting gastric secretion.</p>

<p>Histamine (H2) receptor antagonist</p>

<p>Pasireotide acetate is a synthetic cyclic peptide and a somatostatin analogue, which is derived from the chemical synthesis based on the structure of native somatostatins. It operates by binding to somatostatin receptors with high affinity, primarily targeting the sst1, sst2, sst3, and sst5 receptor subtypes. This binding inhibits the secretion of adrenocorticotropic hormone (ACTH), which can modulate the excess production of cortisol in conditions such as Cushing’s disease.</p>

<p>6-Thioguanine is a purine analog used in the therapy for leukemia and for remission consolidation in patients with acute nonlymphocytic anemia. This drug also has antimetabolite action. It replaces guanine during DNA replication. This substitution disrupts the accurate pairing of DNA bases, leading to errors in DNA replication and hinders cell division.</p>

<p>A potent inhibitor of STING protein (stimulator of interferon genes), a protein that partakes in intracellular DNA sensing pathway.  H 151 blocks palmitoylation of STING, which is required for the formation of multimeric complexes for recruiting downstream signalling molecules. Inhibition of STING by H 151 reduces pro-inflammatory cytokine synthesis.</p>

<p>Histamine (H2) receptor antagonist; treats ulcers and acid reflux</p>

<p>Sphingosine-1-phosphate receptor modulator</p>

<p>KBU2046 is an antimicrobial peptide, which is derived from natural or synthetic peptide sequences with potential therapeutic properties. It exerts its effects by disrupting the structure and integrity of bacterial cell membranes through the formation of pores or micelles. This action alters membrane permeability, ultimately leading to cell lysis and death.</p>

<p>17:0-20:4 Pi (4,5) P2 is a synthetic phosphoinositide, which is a chemically defined lipid derived from laboratory synthesis. It features a specific acyl chain composition with a heptadecanoic acid (17:0) at the sn-1 position and an arachidonic acid (20:4) at the sn-2 position. This phosphoinositide mimics naturally occurring phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2), an essential component of cellular membranes.</p>

<p>Inhibits MET, VEGFR1-3, Tie and Ron tyrosine kinases; antineoplastic</p>

<p>Dopamine D2 receptor antagonist</p>

<p>Prostaglandin F2α receptor agonist</p>

<p>SIRT1 activator</p>

<p>SHP099 is an allosteric inhibitor of the SHP2 protein, which is derived from targeted small-molecule drug development. Its mode of action involves binding to SHP2 in a region distinct from the catalytic site, thereby stabilizing the protein in its auto-inhibited conformation and preventing activation. This disrupts downstream signaling pathways mediated by SHP2, a protein-tyrosine phosphatase essential in promoting oncogenic signaling through the RAS/MAPK pathway.</p>

<p>Icilin is a transient receptor potential M8 (TRPM8) agonist drug that is used for the treatment of pruritis. This drug has shown to be effective in producing an extreme cold sensation in both human and animal models. It is used in research for studying TRP channels.</p>

<p>mGluR5 antagonist</p>

<p>BRK tyrosine kinase (PTK6) inhibitor; anti-proliferative in breast cancer cells</p>

<p>Prilocaine is a drug used as a local anaesthetic in dental procedures. It has been shown to reduce the incidence of pain caused. This drug is also a sodium channel blocker that blocks the influx of sodium into cells.</p>

<p>Antagonist of muscarinic acetylcholine receptors</p>

<p>Inhibitor of isocitrate dehydrogenase 2</p>

<p>ABTL-0812 is an investigational anticancer compound, which is a synthetic small molecule with a novel mechanism of action. It is derived from the research efforts focused on targeting key metabolic pathways in cancer cells. The mode of action of ABTL-0812 involves the modulation of the Akt/mTOR pathway, leading to the induction of autophagy-mediated cell death, a process that is selectively cytotoxic to cancer cells.</p>

<p>Sorafenib is a drug that belongs to the class of multikinase inhibitors. It inhibits a number of kinases, including the Mcl-1 protein, which is involved in apoptosis along with blocking picolinic acid (PA), an endogenous metabolite involved in apoptosis signal transduction. Sorafenib also binds to epidermal growth factor receptor (EGFR) on the surface of cancer cells, inhibiting the production of proteins that are required for angiogenesis, thus blocking the formation of new blood vessels. Sorafenib may also inhibit P-glycoprotein (Pgp) activity. Overall, these cytotoxic effects give Sorafenib anti-tumor properties, inhibiting angiogenesis and cellular transformation, which are the two main processes of tumor growth and metastasis. Sorafenib tosylate has been shown to be effective against a range of solid tumors such as breast, prostate and lung cancers and is also used for the treatment of metastatic colorectal cancer and renal cell carcinoma. A combination therapy group found that sorafenib was more effective when used with interferon alfa-2b for the treatment of advanced renal cell carcinoma. Sorafenib also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes.</p>