Organometallic Ligands

Apatinib, also known as rivoceranib, is an inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR2) tyrosine kinase. Apatinib targets VEGFR2 with its action and has proven to have strong anti-tumor effects in human cancers. In studies in mice, apatinib acted as an Inhibitor of VEGFR2 and played an antiangiogenic effect. Apatinib has been suggested for the treatment of ischemia-induced proliferative retinopathy and neovascular age-related macular degeneration.

UM171 is a small-molecule compound, which is derived from synthetic chemical processes with properties that enable the expansion of human hematopoietic stem cells (HSCs) in vitro. It acts by targeting and modulating specific cellular pathways to enhance the self-renewal and proliferation of HSCs without inducing differentiation.

The primary application of UM171 lies in the field of regenerative medicine and transplantation. By facilitating the expansion of HSCs, UM171 holds significant potential in improving the outcomes of bone marrow and cord blood transplants. This is particularly relevant in contexts where donor cell availability is limited or where augmenting the engraftment potential of HSCs is critical. The ability to expand HSCs ex vivo opens avenues for improved treatment of hematological disorders, potentially allowing for more effective and accessible transplant therapies. Researchers are exploring its utility in diverse experimental setups, aiming to translate this compound's capabilities into clinical settings to enhance patient outcomes in hematopoietic recovery and therapy.

Inhibits acetylcholinesterase (AChE); antispasmodic agent

Inhibits human and mouse diacylglycerol O-acyltransferase 1 (DGAT-1) with IC50 values of 9 and 22 nM, respectively. Selective for DGAT-1 over DGAT-2 (IC50 = 53 µM), acyl coenzyme A transferase (IC50 = 296 µM) and other acyltransferases. Reduces plasma and liver triglycerides, FFA, chylomicron secretion and increases HDL cholesterol in vivo.

Multi-kinase inhibitor; inhibits epoxide hydrolase; antineoplastic

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Loreclezole is an antiepileptic drug, which is a synthetic compound with therapeutic effects on the central nervous system. This drug is classified as a 1,2-benzothiazole derivative and primarily impacts neuronal activity. Its source is entirely synthetic, developed through chemical synthesis processes designed to target specific neural pathways involved in seizure activity.

5-HT6 serotonin receptor antagonist; anti-convulsant

C16(Plasm) LPC is a lysophosphatidylcholine, a type of lysophospholipid derived predominantly from plasma membrane phospholipids. It originates from the enzymatic action of phospholipase A2, which cleaves the fatty acid chain, typically at the sn-2 position. This leaves behind the lysophospholipid with a single acyl chain.

Ligand of plasminogen; used for bleeding control

Antagonist of serotonin receptors 5-HT3

Recombinant protein against VEGF(A); binds placental growth factor (PIGF)

Uricosuric agent

A tyrosine kinase inhibitor with potent activity against EGFR, STAT3, JAK3/STAT, JAK3/AP-1 and JAK3/MAPK. Suppresses IL-2 signaling pathway, inhibits T-cell growth and activation of JAK3, AP-1, STAT, MAPK. Has anti-proliferative and anti-invasive effect on cancer cells.

Inhibitor of protein kinases; induces apoptosis; anti-cancer

Sodium channel blocker; anti-arrhythmic agent

Muscle relaxant; anti-inflammatory

Selective inhibitor histone methyltransferases SUV420H1 and SUV420H2 (IC50 values = 25 nM and 144 nM, respectively). Reduces histone H4K20me2 and H4K20me3 expression whilst increasing H4K20me1 global expression. Inhibits formation of p53-binding protein 1 (53BP1) foci upon ionizing radiation and reduces NHEJ-mediated DNA-break repair.