Ligands organométalliques

<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>AP 1903 is a synthetic small molecule, which acts as a dimerizer ligand. It is derived from the modification of the macrolide antibiotic rapamycin to remove its immunosuppressive effects, thus enabling targeted control of cellular processes. The mode of action involves binding to engineered receptors on the cell surface that contain drug-dependent domains. This binding triggers the dimerization of these receptors, leading to downstream signaling and subsequent cellular responses.</p>

<p>A highly potent antagonist of group II metabotropic glutamate receptors (IC50 values = 21 nM and 14 nM at human mGluR2 and mGluR3 respectively). LY 341495 also inhibits group I and III mGluRs with lower potencies (IC50 values = 0.17, 7.8 and 8.2 µM at mGluR8, mGluR1a and mGluR5a respectively). There has been contradicting findings on the antidepressant and anxiolytic activities of this compound. Enhanced cognitive function and locomotor activity have also been described for LY 341495.</p>

<p>Inhibits FGFR family of kinases; antineoplastic; anti-angiogenic</p>

<p>Linagliptin is a dipeptidyl peptidase-4 inhibitor drug that is used to manage hyperglycaemia in patients with type 2 diabetes. This drug works by inhibiting the enzyme dipeptidyl peptidase-4 and allows for the breakdown of GLP-1 and glucose dependent insulinotropic polypeptide. As a result of this, breakdown of glycogen is reduced and release of insulin is increased.<br>Linagliptin 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>Pravastatin is an HMG-CoA reductase inhibitor that is used to lower lipid levels and manage cardiovascular events such as strokes and myocardial infarction. This drug inhibits HMG-CoA reductase allowing for a reduction in the level of cholesterol.</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>Promotes binding of vWf to glycoproteins on platelets, inducing aggregation</p>

<p>Inhibits histone deacetylase (HDAC)</p>

<p>Positive allosteric modulator (PAM) of cannabinoid receptors CB2. The C2 modulator is the first synthetic PAM of CB2 receptors with antinociceptive properties, which were observed in a mouse model of neuropathic pain.</p>

<p>Dopamine reuptake inhibitor; ligand of sigma receptors</p>

<p>Glucocorticoid receptor agonist; anti-inflammatory</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>Inhibitor of CDK2, JAK2 and FLT3; anticancer</p>

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

<p>Agonist of A3 adenosine receptor; antineoplastic</p>

<p>Aniracetam is a nootropic drug that is used to alleviate memory disturbances caused by cerebrovascular disease and brain disorders. This drug has anti-depressive and anxiolytic properties and is said to target serotonin and dopamine receptors.</p>

<p>Inhibitor of lactate uptake and efflux via monocarboxylate transporter MCT1. The blockade of lactate transport with BAY 8002 leads to accumulation of lactate and pyruvate in cells. The MCT1 inhibition decreased tumour growth most effectively in diffuse large B-cell lymphoma cell lines and in subsets of solid tumour models.</p>

<p>Hispolon is a naturally occurring polyketide compound, which is derived from the mushroom Phellinus linteus, commonly found in Asia. This compound is known for its diverse biological activities, primarily functioning as an antioxidant, anti-inflammatory, and antitumor agent. The mode of action of hispolon involves the modulation of multiple cellular pathways. It has been shown to induce apoptosis in cancer cells by triggering intrinsic and extrinsic apoptotic pathways. Additionally, hispolon exhibits the ability to inhibit the NF-κB pathway, subsequently decreasing the expression of pro-inflammatory cytokines and leading to an anti-inflammatory effect.</p>

<p>Olanzapine is an antipsychotic drug that is used in the treatment of schizophrenia and bipolar disorder. This drug inhibits multiple neuronal receptors such as dopamine and serotonin receptors. This allows for a decrease in symptoms such as hallucinations and disorganised behaviour.</p>