Organometallic Ligands

<p>Selective and potent inhibitor of glucose transporter GLUT1 with IC50 of 2 nM. The compound limits glucose uptake and is able to block basal as well as stress-regulated glycolysis in ovarian cancer cells. It supresses proliferation, viability and tumorigenicity of ovarian cancer cells.</p>

<p>Gardos channel inhibitor</p>

<p>SIRT1 activator</p>

<p>Bremelanotide is a 7 amino acid peptide that is used to treat hypoactive sexual desire disorder in premenopausal women. This drug is an agonist of many melanocortin receptors. Although, its mechanism is unknown, it is said to increase melanin expression which aids in the regulation of sexual arousal.</p>

<p>Potent and selective inhibitor of polycomb repressive complex 2 (PRC2), by binding to the K27me3-pocket of the regulatory EED subunit. Inhibits H3K27 methylation in histone 3. Has anti-tumor activity in murine xenograft models. Synergistic with EZH2 inhibitor against cancer cell growth.</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>Inhibitor of Rho-kinases</p>

<p>13:0 Lyso PS is a lysophosphatidylserine, which is a synthetic lipid derivative that serves as a crucial component in biochemical research. It is synthesized from naturally occurring phospholipids, offering a structurally simplified molecule that retains the functional headgroup critical for biological activity. As a single fatty acid chain molecule, its mode of action includes the modulation of cellular processes through interactions with lysophospholipid receptors and participation in signaling pathways. These interactions can influence cell proliferation, apoptosis, or differentiation, depending on the biological context.</p>

<p>Aripiprazole is an antipsychotic drug that is used in the treatment for various mood and psychotic disorders such as schizophrenia, depression and bipolar disorder. Although, its mechanism is not fully understood, the antipsychotic action of aripiprazole is likely due to its partial agonist activity on D2 and 5-HT1A receptors as well as its antagonist activity at 5-HT2A receptors.</p>

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

<p>Mibefradil is a calcium channel antagonist with the highest selectivity for T- and L-type channels, but also effective for N-, Q-, and R-type calcium channels at micromolar range. It decreases smooth muscle proliferation in response to vascular injury and causes vessel dilatation.</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>Amlexanox is an antiallergic and anti-inflammatory drug that has been shown to be effective in treating rhinitis and allergic asthma in clinical studies. It prevents the slow-reacting substance of anaphylaxis (SRS-A) from being released chemically as a mediator and may have antagonistic effects on interleukin-3.</p>

<p>Antagonist of muscarinic acetylcholine receptors</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>This compound is a novel negative allosteric modulator of glutamate metabotropic receptor mGlu7. It is highly selective for mGlu7 over other receptors of mGlu class with IC50 = 795 nM. Although VU 6010608 showed favourable brain penetration in rats, it has been proposed as an in vitro tool for electrophysiology studies. The mGlu7 is broadly distributed within the mammalian central nervous system and it plays a key role in neuronal function and synaptic plasticity.</p>

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

<p>Lovastatin is an HMG-CoA reductase inhibitor that is used to lower LDL cholesterol levels and to aid in the management of cardiovascular diseases. Animal studies have demonstrated that this drug has vasculoprotective properties.</p>

<p>NADPH oxidase inhibitor; anti-inflammatory</p>