Organometallic Ligands

<p>PI3K enzyme inhibitor</p>

<p>Loreclezole is an antiepileptic drug, which is a synthetic compound with therapeutic effects on the central nervous system. This drug is classified as a 1,2-benzothiazole derivative and primarily impacts neuronal activity. Its source is entirely synthetic, developed through chemical synthesis processes designed to target specific neural pathways involved in seizure activity.</p>

<p>Farnesyltransferase inhibitor</p>

<p>Efficient chemiluminescent NH2-coupling reagent for detection of proteins</p>

<p>Inhibitor of γ-secretase and Notch signalling</p>

<p>Selective inhibitor histone methyltransferases SUV420H1 and SUV420H2 (IC50 values = 25 nM and 144 nM, respectively). Reduces histone H4K20me2 and H4K20me3 expression whilst increasing H4K20me1 global expression. Inhibits formation of p53-binding protein 1 (53BP1) foci upon ionizing radiation and reduces NHEJ-mediated DNA-break repair.</p>

<p>Ionic dimeric contrast agent for diagnostic imaging of the liver</p>

<p>Glucagon-like peptide 1 (GLP-1) receptor agonist; hypoglycemic agent</p>

<p>Ligand of plasminogen; used for bleeding control</p>

<p>A tyrosine kinase inhibitor with potent activity against EGFR, STAT3, JAK3/STAT, JAK3/AP-1 and JAK3/MAPK. Suppresses IL-2 signaling pathway, inhibits T-cell growth and activation of JAK3, AP-1, STAT, MAPK. Has anti-proliferative and anti-invasive effect on cancer cells.</p>

<p>Sodium channel blocker; anti-arrhythmic agent</p>

<p>Suzetrigine is a novel compound classified as a synthetic ligand, which is derived through advanced chemical synthesis techniques. This compound engages specific targets within biological systems, acting primarily as a selective modulator of ion channels.</p>

<p>Serotonin receptor and histamine (H1) receptor antagonist</p>

<p>D8-MMAE is a chemical conjugate product, which is composed of the highly potent cytotoxic agent monomethyl auristatin E (MMAE) linked to targeting moieties, often through a stable linker. This product is synthetic in origin, derived from auristatins, which are analogs of dolastatin 10, a natural peptide isolated from marine organisms. The mode of action of D8-MMAE involves specific binding to cellular targets, typically through an antibody-drug conjugate (ADC) mechanism, where the conjugate binds to antigens on cancer cells. Once internalized, the linker is cleaved, releasing MMAE within the cell. MMAE then binds to tubulin, inhibiting cell division by disrupting the microtubule network, leading to apoptosis.</p>

<p>Inhibitor of TASK tandem pore potassium channel; respiratory stimulant</p>

<p>Binds to FK506 binding proteins (FKBPs) to form a complex that inhibits mammalian targets of rapamycin (mTOR). Blocks p70 S6 kinase activation by interleukin-2 and thereby inhibits proliferation of T cells. Induces differentiation of human pluripotent stem cells (hPSCs) to mesendoderm and blood progenitor cells.</p>

<p>Small molecule antagonist of heparan sulfate that binds to glycosaminoglycans electrostatically. Surfen neutralised anti-coagulant activity of unfractionated and low molecular weight heparins, inhibited enzymatic sulfation and degradation reactions. Surfen also blocked signalling and cell adhesion to fibronectin that was triggered by heparan sulphate.</p>

<p>Heparinase II is an enzyme derived from the bacterium Flavobacterium heparinum, which is known for its ability to degrade glycosaminoglycans such as heparin and heparan sulfate through preferential endolytic cleavage. This enzyme specifically recognizes and acts upon the 1,4-glycosidic linkages in heparin and heparan sulfate substrates, leading to their depolymerization into smaller oligosaccharides.</p>

<p>Inhibitor of voltage-activated calcium channels</p>

<p>Dimethyl sphingosine-1-phosphate (d18:1) is a bioactive lipid molecule, specifically a sphingolipid derivative, which plays a critical role in cellular signaling pathways. It is a synthetic compound derived from natural sphingosine-1-phosphate (S1P), a signaling sphingolipid found in the membranes of eukaryotic cells. This compound acts by modulating signaling pathways involving G protein-coupled receptors (GPCRs), primarily the S1P receptors, influencing a wide range of cellular processes such as proliferation, migration, and survival.</p>