Organometallic Ligands

<p>Levetiracetam is a modulates the activity of the synaptic vesicle protein 2A (SV2A) in the brain and is used to treat epilepsy.It is not clear exactly how Levetiracetam affects the activity of SV2A and if this is through inhibiting the release of neurotransmitters. However, it is thought to work by binding to a specific site on SV2A, which interferes with its normal function and ultimately leads to changes in exocytosis. One of the postulated mechanisms of action is that this modulates glutamate release. Levetiracetam is used to treat certain types of seizures in people with epilepsy.<br>Levetiracetam 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>(±)-Vasicine is an alkaloid compound, which is a naturally occurring, organic molecule found primarily in the plant Adhatoda vasica. This alkaloid is extracted from the leaves of the plant, which is native to parts of Asia, particularly India and Pakistan. (±)-Vasicine is known for its bronchodilatory and respiratory stimulant activities.</p>

<p>Idelalisib is a pharmaceutical drug that functions as a PI3Kδ inhibitor, developed through synthetic chemical processes. Its mode of action involves selectively targeting and inhibiting phosphatidylinositol 3-kinase delta (PI3Kδ), a lipid kinase that plays a crucial role in the signaling pathways responsible for cell proliferation, survival, and differentiation. By inhibiting this enzyme, Idelalisib effectively impedes pathways that are often hyperactivated in certain hematologic malignancies, thereby exerting antitumor effects.</p>

<p>Afatinib is a small molecule that inhibits the activity of cellular kinases that are involved in the progression of cancer. It is an Irreversible inhibitor of three members of the ErbB family. This molecule binds covalently to cysteine 797 residue in HER2 and blocks downstream cellular signalling which inhibits cellular growth and promotes apoptosis. It has been researched for the treatment of non-small cell lung cancer (NSCLC), breast cancer, pancreatic cancer and colorectal cancer.</p>

<p>Carmustine is a DNA alkylating agent which also cross-links DNA. As a result, Carmustine disrupts the function of DNA, resulting in the arrest the cell cycle and apoptosis. Consequently these properties of Carmustine, in addition to its ability to easily transmit through the blood-brain barrier, means it can be used as a cancer treatment, treating cancers such as, breast, ovarian and pancreatic as well as lymphomas and leukemias. Furthermore Carmustine can contribute to cytotoxic effects through its ability to carbamoylate DNA repair enzymes and proteins.</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>Proteosome inhibitor; pro-apoptotic; has anti-myeloma activity</p>

<p>Inhibits actin polymerization</p>

<p>Inhibitor of BACE1 protease</p>

<p>PYR-41 is a small molecule inhibitor, which is sourced from chemical synthesis. It functions primarily by targeting ubiquitin-activating enzymes, particularly the E1 enzyme, to disrupt the ubiquitination process. This mechanism effectively hampers the transfer of ubiquitin to substrate proteins, thereby modulating protein degradation and signaling pathways.</p>

<p>Inhibits multiple tyrosine kinases (Abl1, Src family kinases, Tie-2 and VEGFR-2)</p>

<p>Inhibitor of TGF-α, CTGF, ERK1/2, NF-κB and FasL; anti-inflammatory</p>

<p>Calcitriol is a steroid hormone, vitamin D metabolite and agonist of vitamin D receptor (VDR), also known as calcitriol receptor. It regulates absorption of calcium from intestine, resorption of bone calcium and calcium excretion via kidneys. This compound also controls cell cycle, promotes cell differentiation, triggers apoptosis and acts as anti-inflammatory factor within the tumor microenvironment. It has anti-proliferative effects in malignant epithelial cells and in tumour-derived endothelial cells (TDEC). Also, it is a potent inhibitor of retinal neoangiogenesis in vitro.</p>

<p>Dual inhibitor of the adaptor protein 2-associated kinase 1 (AAK1) and BMP2-inducible kinase (BMP2K) with IC50 values of 270 nM and 1 μM, respectively. In a recent study, SGC AAK1 1 stabilised β-catenin, inhibited phosphorylation of the AP2 complex subunit mu protein (AP2M1) and activated Wnt signalling in in vitro experiments._x000D_</p>

<p>Specific inhibitor of glycogen synthase kinase 3 (GSK-3) with IC50 in low nanomolar range. Studies showed that BIO maintains self-renewal in embryonic stem cells (ESCs) as well as increases activity of β-catenin. In neonatal cardiomyocytes, BIO promotes cell cycle by stimulating cell entry into S phase as well as cytokinesis. In germline stem cells from female mice (FGSCs), BIO promoted proliferation and maintenance of FGSCs by activating β-catenin and up-regulating E-cadherin.</p>

<p>Furosemide is a potent loop diuretic that is used in the treatment of hypertension, liver cirrhosis, renal disease and heart failure. This drug acts on the kidney to increase water loss from the body. It inhibits electrolyte reabsorption. Furosemide also exerts vasodilatory effects.</p>

<p>Brimonidine-D-tartrate is a selective alpha-2 adrenergic agonist, which is a pharmacological compound derived synthetically, targeting specific receptor subtypes in the adrenergic receptor family. Its mode of action involves reducing aqueous humor production and increasing uveoscleral outflow in the eye, thereby lowering intraocular pressure. Additionally, it induces peripheral vasoconstriction, playing a role in reducing redness in rosacea.</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>Ebselen is a non-toxic organoselenium compound with antioxidant, anti-inflammatory and cytoprotective properties. Ebselen is an inhibitor of lipoxygenases, nitric oxide (NO) synthases, protein kinase C, H+/K+-ATPase, thioredoxin reductase and NADPH oxidase. Recently, ebselen has been identified by several studies as a covalent inhibitor of the main protease Mpro from coronaviruses. For the SARS-CoV-2 main protease Mpro, the IC50 value is 0.67 μM and EC50 is 4.57 μM.</p>

<p>S26131 is an advanced glycation end product (AGE) inhibitor, which is a synthetic compound designed for laboratory research purposes. It is derived from chemical synthesis processes, offering a robust tool for investigating the biochemical pathways associated with glycation. Its mechanism of action involves the inhibition of AGE formation, which is a post-translational modification resulting from the non-enzymatic reaction between sugars and proteins or lipids. This biochemical modulation is vital for studying the implications of glycation in various physiological and pathological contexts.</p>

<p>Inhibits platelet glycoprotein IIb/IIIa receptors</p>

<p>Dual COX/5-LO inhibitor; anti-inflammatory; analgesic</p>

<p>Racemic mixture of AMG 510</p>

<p>GnRH super-agonist</p>

<p>(2R)-Arimoclomol maleate is an investigational pharmaceutical compound, which is an orally bioavailable small molecule with pharmacological activity primarily targeting cellular protein homeostasis mechanisms. This therapeutic agent is derived from molecular chaperones and operates by selectively enhancing the expression of heat shock proteins (HSPs). The mechanism of action involves the modulation of the heat shock response, wherein (2R)-Arimoclomol maleate amplifies the natural cellular defense pathways against protein misfolding and aggregation.</p>

<p>Inhibitor of glycogen synthase 3 (GSK-3) and cyclin-dependent kinases CDK1, CDK2 and CDK5. Kenpaullone can substitute transcription factor Klf4 in reprogramming of fibroblast to induced pluripotent stem cells when using the method of ectopic expression of transcriptional factors. In an in vitro model for Alzheimer’s disease, kenpaullone decreased production of amyloid beta peptides Aβ40 and Aβ42.</p>

<p>Inhibitor of EIF2AK3/PERK kinases</p>

<p>AZD-7648 is a selective inhibitor of DNA-dependent protein kinase (DNA-PK), which is a pivotal enzyme involved in the non-homologous end joining (NHEJ) pathway of DNA repair. This product is derived from extensive chemical synthesis and optimization, designed for its specificity and efficacy in inhibiting DNA-PK activity. The mode of action involves binding to the ATP-binding site of DNA-PK, thereby obstructing its ability to facilitate the repair of double-strand DNA breaks.</p>

<p>Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin receptors. It was designed to treat mood disorders, such as depression. It has been shown to improve mood by increasing the levels of certain neurotransmitters in the brain such as dopamine and noradrenaline. Agomelatine has beneficial phase-shifting effects in humans; it causes a sleep phase advance, a drop in body temperature, and an initial release of melatonin. According to controlled human studies, Agomelatine is equally effective at treating severe depression as the SSRI antidepressants paroxetine and sertraline.</p>

<p>Inhibits p38 MAP kinase; anti-inflammatory; neuroprotective</p>

<p>Zileuton is an inhibitor of the 5-lipoxygenase enzyme, thus preventing the leukotrienes LTE4, LDT4, LTB4 and LTC4 from being formed. This in turn reduces inflammation, bronchoconstriction and mucus secretion in the airways. As a result, Zileuton can be used in the treatment and management of asthma and allergic rhinitis. Studies have shown that Zileuton has the potential to reverse dementia-related brain damage.</p>

<p>17:0-20:4Pi (4) P is a synthetic phosphoinositide, which is a type of phospholipid. It is typically sourced from laboratory synthesis, often incorporating stable isotopes or specific fatty acid chains to mimic natural compounds found in cell membranes. This product functions primarily as a probe in biochemical experiments, particularly for studying lipid signaling pathways within cells.</p>

<p>Dopamine reuptake inhibitor</p>

<p>Antagonist of cardiac potassium channel HERG; anti-psychotic</p>

<p>3-Hydroxy-5-{[(naphthalen-2-yl)carbamoyl]amino}benzoic acid is a synthetic compound characterized by its complex molecular structure incorporating naphthalene and benzoic acid moieties. As a derivative of benzoic acid, it is typically synthesized through a series of chemical reactions designed to introduce the 3-hydroxy and carbamoyl functional groups, creating a compound with potentially unique bioactive properties.</p>

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

<p>Lomustine is an alkylating agent that is used as chemotherapy for treating metastatic brain tumors and relapsed Hodgkin’s disease in combination with radiation treatments. This drug causes alkylation and cross-linking of DNA, thus inducing cytotoxicity. Furthermore, this drug inhibits DNA synthesis.</p>

<p>Omeprazole is a proton pump inhibitor (PPI) that inhibits the production of gastric acid in the stomach. This is due to Omeprazole binding through a stable disulphide bond to the H+/K+ ATPase enzyme found on parietal cells, and preventing hydrogen ion transport. Consequently, gastric acid secretion is supressed. As a PPI, Omerprazole can be used to treat disorders where gastric acid is over-secreted. Examples of these disorders are gastroesophageal reflux disease (GERD) and peptic ulcer disease.</p>

<p>Potent and selective positive allosteric modulator (PAM) of metabotropic glutamate receptor mGlu4. Valiglurax is orally bioavailable and CNS-penetrant mGlu4 PAM in preclinical development for the Parkinson’s disease therapy and alleviation of the motor symptoms.</p>

<p>Synthetic antineoplastic agent</p>

<p>Cetirizine is a selective histamine-1 antagonist drug used for the treatment of allergies. One of the common uses is for a condition called allergic rhinitis. As Cetirizine is an antihistamine, its main mode of action is by selectively inhibiting H1 receptors. In vivo and ex vivo animal models have shown insignificant anticholinergic and antiserotonergic effects.</p>

<p>AZD 1152 is an Aurora kinase inhibitor, which is a type of small-molecule therapeutic agent. It is derived from the pharmaceutical research conducted by AstraZeneca. Its primary mode of action involves the selective inhibition of Aurora B kinase, an enzyme crucial for the regulation of mitosis. By interfering with this enzyme, AZD 1152 disrupts the normal progression of cell division, leading to the inhibition of proliferation and induction of apoptosis in rapidly dividing cells.</p>

<p>CMX 001 is an antiviral medication that is a prodrug of cidofovir, which is derived from nucleoside analogs with direct inhibition of viral DNA polymerase. This mechanism of action allows CMX 001 to effectively disrupt viral replication by integrating into viral DNA and halting its synthesis. Designed to target a broad range of DNA viruses, this drug offers a robust means of controlling viral infections.</p>

<p>Activates CFTR channels</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>Inhibitor of protein kinase CK2</p>

<p>NAP is a neuroprotective peptide, which is derived from activity-dependent neuroprotective protein (ADNP), with a mechanism involving microtubule stabilization and neuronal protection. It exhibits the ability to protect neurons from various types of damage, including oxidative stress and conditions mimicking neurodegenerative diseases. NAP enhances axonal transport and increases the resilience of neurons to insults that would typically result in cell death. This peptide has shown promise in preclinical studies for its potential to halt or reverse cognitive decline, making it a focal point for research into therapeutic strategies for disorders like Alzheimer's disease and other tauopathies. The peptide operates by binding to microtubules, promoting stability, and facilitating efficient transport of cellular components. Studies have highlighted its role in traversing the blood-brain barrier, which makes it a viable candidate for central nervous system-targeted therapies. Researchers continue to explore its efficacy and possible applications in improving cognitive function and providing neuroprotection in aging populations.</p>

<p>Pan-class I phosphatidylinositide 3-kinase (PI3K) inhibitor (IC50 = 3, 33, 3 and 75 nM at catalytic subunits p110α, p110β, p110δ and p110γ respectively). Inhibits proliferation in several cancer cell lines, such as glioblastoma, breast and prostate cancer cells. Has synergistic anti-cancer effect in combination with MEK/ERK kinase inhibitor GDC-0973 (cobimetinib).</p>

<p>NMDA glutamate receptor antagonist</p>

<p>Inhibitor of MEK1 and MEK2 kinases</p>