Organometallic Ligands

<p>Inhibitor of mutant B-rafV600E protein that results in decreased proliferation of cancer cells with this mutation. Treatment of metastatic melanoma in patients harboring the V600E mutation, had improved disease outcome. This antitumor activity is enhanced when combined with MEK inhibitor trametinib.</p>

<p>Agonist of kainate receptors, a subclass of ionotropic glutamate receptors with neuroexcitatory action. At high concentrations, it can induce seizures and act as neurotoxin, causing neuron death due to overstimulation.</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>GSK-126 is a potent inhibitor of histone lysine methyl transferase 2, which is encoded by the enhancer of zeste homolog 2 gene (EZH2). The EZH2 protein regulates cell cycle as it represses the Polycomb-Repressive Complex 2 (PRC2), allowing cells to divide actively. GSK-126 inhibits the EZH2 by targeting the catalytic domain (SET) of the enzyme and therefore blocks the PCR2 repression mechanism, resulting in cell proliferation arrest. The compound has shown therapeutic potential for a variety of cancers.</p>

<p>Inhibits multiple protein kinases, such as PKC and FLT3</p>

<p>LGD 3303 is an investigational selective androgen receptor modulator (SARM), which is a compound designed to selectively interact with androgen receptors in the body. SARMs like LGD 3303 are researched for their potential to mimic anabolic activity with reduced androgenic effects compared to traditional anabolic steroids. LGD 3303 acts by binding to androgen receptors, and it is believed to promote muscle growth and bone health without significantly affecting other tissues.</p>

<p>Inhibitor of VEGF receptors</p>

<p>Inhibits cyclin-dependent kinase 4 and 6 (CDK4 and CDK6); antineoplastic</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>NMDA receptor antagonist</p>

<p>Ifosfamide is an alkylating agent and immunosuppressive drug used in chemotherapy for the treatment of various cancers such as ovarian, testicular, cervical and bladder. This drug interferes with the normal process of DNA replication causing damage to the DNA in cancer cells hence preventing them from growing and dividing.</p>

<p>Inhibitor of SHIP2 phosphatase</p>

<p>TIC10 is a small molecule, which is sourced from a synthetic chemical library, with a novel mode of action that involves the induction of the tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) pathway. This pathway is distinguished by its ability to selectively trigger apoptosis in cancer cells while sparing normal cells. TIC10 effectively crosses the blood-brain barrier, a feature that enhances its potential application in treating brain-related malignancies.</p>

<p>Please enquire for more information about S7958 including the price, delivery time and more detailed product information at the technical inquiry form on this page</p>

<p>Potent inhibitor of the sodium-coupled citrate cotransporter SLC13A5 (NaCT, INDY). The compound is not structurally related to citrate and is selective for SLC13A over other related transporters.</p>

<p>Calcium channel blocker</p>

<p>Baricitinib phosphate is a selective Janus kinase (JAK) inhibitor, which is a synthetic product developed through targeted molecular design. Its mode of action involves the inhibition of JAKs, which are intracellular enzymes that transmit cytokine-mediated signals via the JAK-STAT pathway. By blocking these signals, baricitinib phosphate effectively reduces inflammatory responses.</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>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>Inhibitor of CPT1 and CPT2 enzymes; inhibitor of mTORC1 kinase; anti-fungal</p>

<p>Esomeprazole is an anti-ulcer drug that is used in the treatment of GERD and to reduce the risk of ulcers associated with NSAID’s. This drug is a proton pump inhibitor that suppresses the release of gastric acid in the stomach.</p>

<p>A BCL-2 selective inhibitor with no effect on Bcl-xl and thereby prevents thrombocytopenia. Increased sensitivity observed in Bcl-2-dependent haematological tumour cell lines. Elicits additional benefits to tamoxifen treatment in ER-positive breast cancer xenografts.</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>Toxin; induces pulmonary hypertension</p>

<p>Dabigatran is an anticoagulant that is used for the treatment of atrial fibrillation and prevention of venous thromboembolic events. It is a drug that acts as an inhibitor of the enzyme thrombin. Dabigatran inhibits platelet activation and aggregation, which reduces the risk of stroke or other vascular events. Dabigatran is a prodrug and does not have any activity in its active form.</p>

<p>Anti-rheumatic; immunosuppressant; neuroprotective; neuroregenerative</p>

<p>Inhibitor of glutaminase; glutamine analogue</p>

<p>GPR68 PAM, bioavailable in mice and with excellent brain penetration</p>

<p>Bicuculline is a phthalide-isoquinoline compound and is a competitive GABA receptor antagonist. It blocks GABA’s inhibitory action, mimicking epilepsy. This compound is used in research to better study epilepsy.</p>

<p>Activates CFTR channels</p>

<p>Naloxone hydrochloride is a competitive antagonist at mu-, delta- and kappa-opioid receptors. Naloxone binding to receptors blocks the effects of opioids such as morphine, heroin, or oxycodone. Naloxone has been shown to be effective in treating acute overdoses of these drugs and reversing the depression of respiratory function that accompanies opioid overdose. It is also used to alleviate withdrawal symptoms and in the treatment of neonatal abstinence syndrome (NAS). NAS is a condition that occurs when infants are exposed to addictive levels of opioids in utero and go through withdrawal after birth.</p>

<p>Inhibitor of VEGFR; antineoplastic</p>

<p>Inhibitor of TRPC6 cation channel</p>

<p>Eplerenone is a drug known as an aldosterone antagonist. It is a type of potassium-sparing diuretic that is used to treat chronic heart failure and high blood pressure, particularly for patients with resistant hypertension due to elevated aldosterone. It does this by blocking the activity of the enzyme that produces aldosterone, which increases levels of sodium and water in the body. This leads to a decrease in blood pressure.</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>Potent inhibitor of c-Met catalytic activity. Selective over other tyrosine and serine-threonine kinases (600-fold selectivity). Ability to block constitutive or HGF-stimulated phosphorylation of c-Met demonstrated in vitro. JNJ 38877605 reduces radiation-induced invasion, apoptosis and proliferation of cancer cells in vitro.</p>

<p>BMH-7 is a small molecule inhibitor used in molecular biology, which is derived from chemical synthesis methods. It interacts with specific protein domains to disrupt protein-protein interactions within cellular pathways. The mode of action involves binding to target proteins, thereby inhibiting essential interactions that are crucial for the stability and function of multiprotein complexes. This targeted approach allows researchers to dissect complex signaling pathways and understand the underlying mechanisms of cellular functions.</p>

<p>Agonist of ghrelin receptor; growth hormone secretagog</p>

<p>BMH-9 is a peptide inhibitor, which is sourced from natural extracellular matrix components. Its mode of action involves binding specifically to target proteins, thereby inhibiting their interaction with other molecules. This specificity makes it a valuable tool in biochemical and cellular studies designed to elucidate protein functions and pathways.</p>

<p>Inhibitor of protein kinase CK2</p>

<p>Selective and potent inhibitor of 8-oxoguanine DNA glycosylase OGG1 with IC50 of 0.6 μM. OGG1 is a key enzyme in DNA repair mechanism called base excision repair (BER). The compound inhibits the hydrolysis of glycosidic bond required for the excision of 8-oxoguanine from double stranded DNA, which leads to accumulation of mutations. It has been proposed as monotherapy for certain types of cancers as well as adjuvant for cancer therapy with DNA damaging agents. It has potential to sensitize tumours for chemotherapy and inhibit development of drug resistance mechanisms.</p>

<p>Lenvatinib is a tyrosine kinase inhibitor that is used to treat cancers such as solid tumours. This drug inhibits the activity of VEGR receptors. It also inhibits other receptors such as fibroblast growth factor.</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>Endothelin receptor antagonist</p>

<p>4,5,6,7-Tetrabromobenzimidazole is a brominated heterocyclic compound, which is synthesized chemically from benzimidazole. Its bromination at the 4, 5, 6, and 7 positions of the benzimidazole ring enhances its reactivity, making it a highly potent inhibitor in various enzymatic processes. This compound is primarily sourced through methods that involve controlled bromination reactions in laboratory settings.</p>

<p>Icatibant is a 10 amino acid peptidomimetic of bradykinin and a selective antagonist to the bradykinin B2 receptor. Icabinant has been used for the treatment of attacks in patients with hereditary angioedema. Recent evidence has shown a link between dysregulated bradykinin‐mediated inflammation and acute respiratory distress syndrome (ARDS), a common complication in COVID-19 patients. Icatibant was proposed to inhibit excessive activation of the bradykinin B2 receptor during the SARS-CoV-2 infection, reducing the risk of ARDS.</p>

<p>PD 168393 is a potent and selective irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It is synthesized through advanced chemical processes, designed to specifically target and covalently modify the ATP-binding site of EGFR. The mode of action involves the irreversible binding to the cysteine residue in the ATP-binding pocket, leading to the inhibition of EGFR autophosphorylation and subsequent downstream signaling pathways.</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>Tretoquinol is a bronchodilator, which is synthesized from specific chemical reactions involving quinoline derivatives. It functions primarily as a beta-adrenergic agonist, stimulating beta-2 adrenergic receptors. This activation leads to the relaxation of bronchial smooth muscle, resulting in widened air passages and improved airflow. Tretoquinol's mechanism of action involves enhancing cyclic adenosine monophosphate (cAMP) levels, which then promotes the relaxation of the bronchial and vascular musculature.</p>

<p>Dofetilide belongs to the class of antiarrhythmic agents. It is a class III antiarrhythmic agent, which acts by blocking the potassium ion channels in the heart. It is used for the management of normal sinus rhythm and in atrial fibrillation. In vitro studies have shown that Dofetilide can prevent arrhythmias resulting from experimental models of congestive heart failure and can prevent re-entry mechanisms that lead to tachycardia.</p>