Chir 2279 is a N-(substituted)glycine peptoid trimer with high-affinity binding for alpha 1-adrenoceptors. CHIR 2279 antagonized the epinephrine-induced increase in intraurethal pressure (pseudo pA2, 6.86) in dogs.
TNF-α-IN-2 is a highly potent and orally bioavailable inhibitor of tumor necrosis factor alpha (TNFα), exhibiting an IC50 of 25 nM in the HTRF assay. It exerts its inhibitory effects by inducing conformational changes in the TNFα trimer upon binding, resulting in disrupted signaling when the trimer interacts with TNFR1. TNF-α-IN-2 holds promise as a valuable tool for investigating the pathogenesis of rheumatoid arthritis[1].
Dichloroacetate (DCA) is an inhibitor of all pyruvate dehydrogenase kinase (PDHK) isoforms, which are enzymes that phosphorylate and inhibit PDH in mitochondria. Inhibition of PDHK shifts cell metabolism from glycolysis to mitochondrial glucose oxidation, an effect that has relevance to cancer, type 2 diabetes, and other diseases. CAY10703 is a DCA trimer that is at least 10-fold more cytotoxic against leukemia cell lines than DCA. It is approximately 3-fold less cytotoxic than DCA against peripheral blood mononuclear cells from healthy blood donors. CAY10703 significantly reduces both basal and maximal respiration in leukemia cells. It is stable in vivo after subcutaneous inoculation, remaining in circulation for more than five hours after injection.
AB-729, a nucleoside analogue functioning as an RNA interference (RNAi), links to a GalNAc (N-acetylgalactosamine) trimer ligand facilitating hepatocyte uptake through the asialoglycoprotein receptor (ASGR). This compound effectively impedes viral replication and diminishes HBV antigens.
UCB-6876 is a novel inhibitor of TNF signalling by stabilising an asymmetric form of the trimer, displaying a concentration-dependent response curve and selectivity over the TNFR1 extracellular domain and control proteins.
UCB-6786 is a novel inhibitor of TNF signalling by stabilising an asymmetric form of the trimer, displaying a concentration-dependent response curve and selectivity over the TNFR1 extracellular domain and control proteins.