Organometallic Ligands

<p>A 939572 is an inhibitor of stearoyl-CoA desaturase 1 (SCD1). It exhibits anticancer activity as it inhibits cell growth and promotes cell death in human non-small cell lung carcinoma cells.</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>Drotaverine is an antispasmodic drug that is used to alleviate gastrointestinal and genitourinary smooth muscle spasms. This drug works by inhibiting phosphodiesterase-4 and increasing levels of cAMP leading to smooth muscle relaxation.</p>

<p>Smoothened agonist and activator of the Hedgehog signalling pathway with EC50 of 3 nM. SAG binds to the Smoothened heptahelical bundle and antagonises effects of the Smoothened antagonist cyclopamine. In previous studies, SAG activated neurogenesis and neuronal survival in cell and animal models as well as improved cell differentiation of human induced pluripotent cells into the neuronal lineage.</p>

<p>Vanilloid receptor 1 antagonist</p>

<p>Inhibitor of Rho-kinases</p>

<p>A selective inhibitor of MEK5 protein kinase with an IC50 value of 4.3 nM. Blocks transcriptional activation of myocyte-specific enhancer factor 2C (MEF2C). Inhibits phosphorylation of ERK5 protein kinase and thereby reverses inhibition of TNF signaling induced by fluid shear stress in endothelial cells. Induces apoptosis in FLT3-ITD cells.</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>Inhibitor of p38 kinase</p>

<p>Inhibitor of transcriptional coactivator PGC-1a; anti-diabetic agent</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>A selective inhibitor of MEK1/2 kinase. Anti-proliferative and pro-apoptotic in multiple myeloma (MM) cells via G0/G1 cell cycle arrest and caspase 3 and PARP cleavage, respectively. Synergistic with other anti-MM therapies. Has anti-tumor effects in some solid tumors, such as in K-ras mutated colorectal cancer.</p>

<p>A potent inhibitor of phosphodiesterase type 9 (PDE9) tested in human and murine in vitro assays (IC50 values: 55 nM and 100 nM respectively). BAY 73-6691 induces long-term potentiation and improves memory in rodents. Has therapeutic potential for Alzheimer’s disease.</p>

<p>A potent ATP-competitive inhibitor of tropomyosin-related kinases (TRK1, TRK2 and TRK3), members of the receptor tyrosine kinase family of neurotrophin receptors. Tumors with oncogenic TRK fusions are sensitive to larotrectinib, leading to reduced proliferation and tumor growth in patients with soft tissue sarcoma, triple-negative breast cancer and lung cancer.</p>

<p>Anti-inflammatory; inducer of P450 II B family</p>

<p>Inhibitor of LRRK2 kinase</p>

<p>Allosteric activator of AMP-activated protein kinase (AMPK) acting on the AMPK-β subunit with therapeutic potential in metabolic disorders such as diabetes, obesity, etc. A769662 also blocks the differentiation of mouse embryonic stem cells (mESCs) and maintains the mESCs in naïve state even in the absence of leukemia inhibitory factor (2i/L).</p>

<p>Short acting monoamine oxidase inhibitor</p>

<p>A cannabinoid receptor agonist, which binds more selectively to CB2 than CB1 receptors (1000-fold). GW833972A inhibits vagus nerve depolarization induced by tussive agents, such as hypertonic saline (EC50 = 6.5 μM), capsaicin (EC50 = 33.9 μM) or PGE2 (EC50 = 15.9 μM).</p>

<p>Dutasteride is an androgenic compound and a 5α-reductase inhibitor that is used to treat benign prostatic hyperplasia (BPH) and male pattern baldness. Dutasteride reduces prostate volume and improves symptoms of BPH by inhibiting the enzyme 5α-reductase, which converts testosterone to dihydrotestosterone.</p>

<p>Fludarabine triphosphate trisodium is a nucleotide analog, which is a type of chemotherapy agent derived from purine nucleosides. This compound is the active metabolite of fludarabine, sourced from synthetic chemistry designed to mimic naturally occurring nucleotides involved in DNA replication. The mode of action involves its incorporation into the DNA strand during replication, where it effectively inhibits DNA polymerase and ribonucleotide reductase. This disruption impairs DNA synthesis, leading to apoptosis or programmed cell death, particularly in rapidly dividing cancer cells.</p>

<p>AZD9567 is a selective glucocorticoid receptor modulator (SGRM), which is a synthetic pharmaceutical compound. Its source is rooted in medicinal chemistry efforts to design ligands that selectively interact with glucocorticoid receptors. The mode of action of AZD9567 involves binding to glucocorticoid receptors with high specificity, modulating their activity to trigger anti-inflammatory and immunomodulatory responses while minimizing common side effects associated with traditional glucocorticoids.</p>

<p>Inhibits tankyrase (TNKS1 and TNKS2 with IC50 values of 11 and 4 nM respectively), by binding to the catalytic poly-ADP-ribose polymerase (PARP) domain. This stabilizes cytoplasmic protein Axin, mediating β-catenin depletion and thereby suppresses Wnt signalling pathway. XAV 939 has anti-proliferative and pro-apoptotic effects on neuroblastoma and colorectal cancer cells.</p>

<p>5-HT3 receptor antagonist; alpha-7 nicotinic acetylcholine receptor partial agonist</p>

<p>Tacrolimus is a calcineurin inhibitor drug that is used for the prevention of rejection after an organ transplant. This drug can also be used in the treatment of severe atopic dermatitis. Tacrolimus’ mechanism of action is not well known however it is understood that this drug inhibits T-lymphocyte activation by binding to an intracellular protein called FKBP-12. This drug also has anti-inflammatory properties.</p>

<p>Carvediol is a nonselective beta-adrenoceptor blocking agent and an alpha 1-adrenoceptor blocker. It can be used as a drug, belonging to the class of beta blockers, in the treatment of heart failure, coronary artery disease, and hypertension. Carvedilol has been shown to reduce the risk of death in patients with heart failure and improve symptoms. Furthermore it has an effect on blood pressure by decreasing peripheral vascular resistance and mean arterial pressure. Carvedilol can be metabolized by cytochrome P450 enzymes and CYP2D6 and CYP2C9 liver enzymes.</p>

<p>Loratadine is a non-sedating, inverse agonist antihistamine used for the treatment of allergic rhinitis, an IgE (immunoglobulin E) mediated disease. Loratadine binds to histamine H1 receptors, preventing histamine from binding and causing an allergic reaction.It has been found to inhibit the release of eosinophil cationic protein by acting on different components of allergic inflammation, in particular in the modulation of ICAM-1 expression on nasal epithelial cells as a mechanism of protective for the epithelium, and therefore, the damage of mucosa is reduced. In recent studies, it was found that loratadine is a potent HR1 antagonist with in vitro inhbitory effect on human mast-cell lines, HMC-1 (from mast cell leukaemia) with an IC50 between 10 and 50 μM.Loratadine 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>5-Fluorouracil is a cytotoxic drug that inhibits the synthesis of DNA. It is used in combination therapy to treat cancer and is a pyrimidine analog. This drug inhibits the formation of thymidylate synthase from uracil. As a result, this leads to DNA and RNA synthesis inhibition and cell death.</p>

<p>Inhibitor of COX-2 and PDE4 enzymes; NSAID of coxib class</p>

<p>Malotilate is a pharmacological agent that is used to treat symptoms of hepatitis, bowel disease, and collagen diseases. This drug reduces collagen synthesis and cell migration activity of fibroblasts in vitro. It also has been shown to facilitate liver regeneration in rats.</p>

<p>Inhibitor of the Bruton tyrosine kinase</p>

<p>Medetomidine is a synthetic compound of the benzodiazepine class. It has a variety of pharmacological effects, including sedation and muscle relaxation, and is used in veterinary medicine as an anesthetic agent for animals. Medetomidine can be administered intravenously, intramuscularly, or subcutaneously. The drug crosses the blood-brain barrier to produce its sedative effect. This agent has been shown to be effective in inducing anesthesia in experimental animals with a wide range of body weights. Medetomidine has also been shown to have cardiovascular effects such as lowering systolic pressure and heart rate. Medetomidine HCl is soluble in water and trifluoroacetic acid (TFA).<br>Medetomidine HCl is rapidly hydrolyzed by esterases at physiological pH to medetomidinol (MTM) and then further metabolized by glucuronide conjugation to form medetominol glucuronide</p>

<p>Ramipril is an angiotensin-converting enzyme (ACE) inhibitor. It is used in the treatment of high blood pressure, congestive heart failure and other cardiovascular diseases. Ramipril inhibits the conversion of angiotensin I to angiotensin II by blocking ACE, which lowers blood pressure and reduces fluid retention.This product 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>K02288 is a small molecule inhibitor, which is derived from extensive chemical synthesis and compound screening techniques. It functions as a selective antagonist of the activin receptor-like kinase (ALK) pathway, specifically inhibiting Transforming Growth Factor-beta (TGF-β) superfamily receptor signaling. This pathway is crucial in a variety of cellular processes including proliferation, differentiation, and apoptosis, thereby making K02288 an important tool in cell signaling and cancer research.</p>

<p>Opioid receptor antagonist</p>

<p>Ketanserin is a 5-HT2A serotonin receptor antagonist that is used for the treatment of hypertension. This drug is also used in research to study the serotonergic system. Ketanserin has been found to also block the vesicular monoamine transporter 2.</p>

<p>Inhibitor of PDE4 enzyme; anti-inflammatory</p>

<p>Antagonist of Wnt signalling pathway by inhibiting the activity of Porcn, a member of the membrane-bound O-acyltransferase (MBOAT) family. Porcn is required for the palmitoylation of Wnt, mediating its secretion and signalling. Inhibits self-renewal in embryonic stem cells, whilst promoting differentiation to epiblast stem cells.</p>

<p>Analeptic</p>

<p>Il-1β is a pro-inflammatory cytokine, which is a type of signaling molecule involved in immune system regulation and inflammation. It is primarily produced by activated macrophages, which are a type of white blood cell that engulfs and digests cellular debris and pathogens. The mode of action of Il-1β involves binding to the interleukin-1 receptor (IL-1R) on target cells, which triggers a cascade of intracellular signaling pathways that lead to the expression of various inflammatory genes.</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>Dothiepin is a tricyclic antidepressant used to treat depression in patients who are not responding to alternative therapies. This drug inhibits the reuptake of norepinephrine and serotonin, increasing available neurotransmitter levels at the synaptic cleft. It also exhibits anticholinergic, antihistamine and central sedative properties.</p>

<p>Docetaxel is an antineoplastic agent that is used to treat various cancers such as breast and prostate cancer. This drug interferes with the normal function of microtubule growth. It is an anti-mitotic drug used in chemotherapy. Research has shown that this drug also induces programmed cell death in cancer cells.</p>

<p>Thalidomide is a piperidinyl isoindole drug that is used to treat various cancers such as myeloma and erythema nodosum leprosum. This drug is immunosuppressive and has anti-angiogenic activity. Thalidomide’s mechanism of action is not fully understood however it is thought to block the activity of tumor necrosis factor-alpha (TNF-α).</p>

<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>Inhibitor of COX1 cyclooxygenase</p>

<p>Aminopterin is an antineoplastic agent and antifolate, which is a synthetic derivative of pteroylglutamic acid. It functions as a chemotherapeutic agent by inhibiting dihydrofolate reductase, an enzyme crucial in the folic acid pathway, thereby preventing the conversion of dihydrofolate to tetrahydrofolate. This disruption leads to impaired synthesis of purine nucleotides and thymidylate, which are essential for DNA synthesis and cell division.</p>

<p>OSU 6162 hydrochloride is a research chemical classified as a dopamine stabilizer, derived synthetically. It primarily acts as a dopamine receptor antagonist, targeting both D2 and D3 dopaminergic receptors in the central nervous system. By modulating dopamine receptor activity, OSU 6162 hydrochloride can help balance dopaminergic signaling, which is crucial in various neurological and psychiatric conditions.</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>Dual inhibitor of thromboxane receptor and DP2 postanoid receptor</p>