Organometallic Ligands

Inhibitor of HIF1-α transcription factor and repressor of HIF1-α-regulated genes in adult and embryonic stem cell models as well as in tumoral cell lines. FM19G11 inhibits the expression of undifferentiating factors Oct4, Sox2, Nanog, and Tgf-α at transcriptional and protein level. FM 19G11 affects also epigenetic events by reducing histone acetylation and leading to repression of p300, a HIF-transcription activation co-factor.

Lodoxamide is a type of ophthalmic medication known as a mast cell stabilizer, which is chemically synthesized from non-steroidal structures. It works by inhibiting the degranulation of sensitized mast cells and subsequent release of inflammatory mediators such as histamine. This action is achieved through the stabilization of the cell membrane of mast cells, thus preventing cellular activation.

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.

Bruton's tyrosine kinase antagonist; reduces Fcγ receptor signaling

Rabeprazole is a proton pump inhibitor drug that is used to treat symptoms of GERD, heal gastrointestinal ulcers and eradicate Helicobacter pylori. This antiulcer drug suppresses gastric acid by inhibiting the gastric H+/K+ ATPase at the parietal cell.

Solifenacin is a muscarinic antagonist drug that is used to treat symptoms associated with an overactive bladder such as urine urgency and urinary incontinence. This drug has high affinity for M1, M2 and M3 receptors, with its highest being for M3 receptors. Antagonism of these receptors prevent contraction of smooth muscles in the bladder.

Interleukin-13 human is a recombinant cytokine, which is derived from the expression of the human IL-13 gene in suitable host systems, such as E. coli or mammalian cells. This cytokine belongs to the interleukin family and plays a pivotal role in the immune response by modulating inflammatory pathways. The mode of action of interleukin-13 involves binding to specific cell surface receptors, IL-13Rα1 and IL-13Rα2, which facilitates the activation of various intracellular signaling cascades, including the JAK/STAT pathway. This promotes the differentiation and proliferation of certain immune cells, influencing the production of IgE and contributing to the regulation of inflammatory responses.

ÎŽ opioid receptor agonist; anti-nociceptive; anti-depressant

Polmacoxib is a non-steroidal anti-inflammatory drug (NSAID), which is derived through synthetic chemical processes. It functions as a selective cyclooxygenase-2 (COX-2) inhibitor. By selectively inhibiting the COX-2 enzyme, polmacoxib reduces the conversion of arachidonic acid to prostaglandins that mediate inflammation and pain, while sparing the COX-1 enzyme that protects gastric mucosa and maintains platelet function.

Anastrozole is a non-steroidal drug that belongs to the class of aromatase inhibitors. It inhibits the production of estrogen by blocking the conversion of androgens to estrogens in peripheral tissues. The drug has been shown to be effective in treating breast cancer in postmenopausal women. In vitro assays have shown that Anastrozole can inhibit tumor growth as well as induce apoptosis in human serum cells, which suggests that it may be effective against a variety of cancers.

Atenolol is a beta-blocker that slows the heart rate and decreases the force of contraction, which reduces the workload on the heart. Atenolol has been shown to be effective in lowering blood pressure in people with chronic kidney disease who are not taking angiotensin-converting enzyme inhibitors. It is also used to treat hypertension and chronic angina.

5-HT1A serotonin receptor agonist; alleviates symptoms of depression

Ramelteon is a synthetic drug, which is a melatonin receptor agonist with high affinity for MT1 and MT2 receptors. These receptors are primarily located in the suprachiasmatic nucleus of the brain, an area responsible for regulating circadian rhythms. By binding to these receptors, Ramelteon mimics the effects of the endogenous hormone melatonin, promoting the onset of sleep.

γ-secretase inhibitor; reduces amyloid-β in brainÂ

Ractopamine hydrochloride is a beta-agonist that stimulates the release of fatty acids from adipose tissue, increasing food intake and weight gain in pigs. It has been shown to have significant interactions with other drugs used for bowel disease, as well as with sodium carbonate, which can be used for control analysis. Ractopamine hydrochloride is an effective drug to stimulate the release of estradiol benzoate in rats during pregnancy. The matrix effect observed when analyzing samples containing ractopamine hydrochloride may be due to its ability to bind to serum proteins or lipids. This drug has been shown to have molecular docking properties that are similar to those found in other molecules.

Histamine (H2) receptor antagonist

A selective and potent inhibitor of phosphodiesterase 2 (PDE2). Raises cAMP and cGMP levels in neurons, improves social recognition and object memory in murine animals. Reverses anxiolytic effects induced by oxidative stress in mice by blocking cGMP-PKG signaling.

Vitamin B6 antimetabolite

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.

Phosphodiesterase (PDE5, 6, 9 and 11) inhibitor