Organometallic Ligands

Bruton's tyrosine kinase antagonist; reduces Fcγ receptor signaling

Dopamine D2 receptor antagonist

Melatonin is a neurotransmitter produced by the pineal gland that is involved in the regulation of sleep-wake cycles. It can be used to treat several conditions like shift work disorders, insomnia, jet lag, and alterations of the circadian rhythm. Some authors also proposed the use of melatonin against cognitive disorders. In an interesting research conducted on zebrafish, it was found that memory formation occurs better during daytime compared to nighttime, suggesting a role of melatonin in this process. When melatonin was administered during the daytime it caused reduced memory formation. On the contrary, removing the pineal gland or treating the fish with a melatonin antagonist significantly improves nighttime memory formation.

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.

Positive allosteric modulator of the metabotropic glutamate receptor mGluR5 with EC50 in submicromolar range. The compound is able to increase mGluR5 function in vitro and in vivo. A study showed that ADX-47273 enhanced fear extinction learning as well as improved reversal learning in experimental animals.

Pasireotide acetate is a synthetic cyclic peptide and a somatostatin analogue, which is derived from the chemical synthesis based on the structure of native somatostatins. It operates by binding to somatostatin receptors with high affinity, primarily targeting the sst1, sst2, sst3, and sst5 receptor subtypes. This binding inhibits the secretion of adrenocorticotropic hormone (ACTH), which can modulate the excess production of cortisol in conditions such as Cushing’s disease.

Antagonist of muscarinic acetylcholine receptors

γ-secretase inhibitor; inhibits notch signaling

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.

Bexarotene is a retinoid and antineoplastic agent that is used for the treatment of solid tumours and t-cell lymphomas. It inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin and research has shown that it induces tumor regression in vivo in some animal models.