trimer

UCB-9260 inhibits TNF signaling by stabilizing an asymmetric form of the trimer.

Compound 48/80 (trimer) is the trimeric form of Compound 48/80. It is widely utilized as a "selective" mast cell activator in animal and tissue models.

The ETE-S trimer is a conjugated trimer that can polymerize under the action of peroxidases in plant cell walls, forming ion-electron mixed conductive polymers for use in bio-hybrid supercapacitors.

Lindetannin is an A-type proanthocyanidin trimer identified in the bark of Cinnamomum (cinnamon trees). Proanthocyanidins are a class of polyphenolic compounds found widely in higher plants, composed of electrophilic flavanyl units. They serve as antioxidants and anti-cancer agents and exhibit anti-inflammatory, cardioprotective, antibacterial, and antifungal properties, making them useful for researching conditions such as chronic venous insufficiency, capillary fragility, sunburn, and retinopathy.

Caprolactam cyclic trimer is a natural product that can be used in related research in the field of life sciences. Its product number is TN8717.

Letolizumab (BMS-986004) is a dimeric antibody targeting CD40L for the expression of mutant IgG1 that lacks effector functions including Fc binding and complement binding.1 Letolizumab does not induce platelet activation in vitro and does not affect coagulation factors or platelet counts/function after repeated dosing in non-human primates.

P2X3 antagonist 34, a potent, selective, and orally active antagonist, targets the P2X3 homotrimeric receptor, exhibiting IC50s of 25 nM, 92 nM, and 126 nM for human, rat, and guinea pig P2X3 receptors respectively. It shows reduced activity against P2X2/3 heterotrimeric receptors across human, rat, and guinea pig models. Notably, this compound demonstrates a significant anti-tussive effect without altering taste[1].

PH-064 (BIM-46187) is an inhibitor of the heterotrimeric G-protein complex.

BIM-46187 4HCl (PH-064 4HCl) is a heterotrimeric G-protein complex inhibitor.

Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.

FSC(PEG4-avb6)3 is an imaging agent specifically targeting the αvβ6 integrin trimer, with an IC50 of 0.69 nM. This compound is used in the study of head and neck cancer, lung cancer, breast cancer, and pancreatic cancer.

iMQT_020 is a selective allosteric SLC1A5_var inhibitor. It disrupts the trimer assembly of SLC1A5_var, leading to a metabolic crisis in cancer cells and selectively inhibiting their growth. iMQT_020 reduces compensatory glutamine metabolism and oxidative phosphorylation, causing widespread metabolic disruption in cancer cells. It lowers GSH levels while increasing intracellular and mitochondrial ROS levels. Additionally, iMQT_020 induces apoptosis and ferroptosis and upregulates PD-L1 expression through epigenetic mechanisms. This compound is applicable in research on pancreatic, lung, and colon cancers.

SARS-CoV-2-IN-120 (Compound S22) is a targeted inhibitor that prevents SARS-CoV-2 from entering cells. It binds to and accumulates within the cavity at the apex of the SARS-CoV-2 spike protein trimer, blocking the interaction between the RBD and ACE2. This compound is capable of neutralizing the BA.2 as well as subsequent Omicron variants and can suppress SARS-CoV-2 replication in mice.

EGFR-IN-200 is an inhibitor targeting EGFR, TNF-α, and the IL-6/GP130 complex, effectively interacting with human EGFR (IC50=0.03 μM), TNF-α (IC50=3.1 μM), and the IL-6/GP130 complex (IC50=1.6 μM). It binds the ATP pocket of EGFR, the trimer interface of TNF-α, and the cytokine-receptor interface of IL-6/GP130, inducing cell cycle G2/M phase arrest, apoptosis, and antiproliferative effects. EGFR-IN-200 is characterized by high gastrointestinal absorption and low blood-brain barrier permeability, adhering to Lipinski's rules. It is applicable in research on lung cancer and breast adenocarcinoma.

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 an effective and orally active TNFα inhibitor that distorts the TNFα trimer upon binding, causing abnormal signal transduction when it binds to TNFR1, and can be used to study rheumatoid arthritis.

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.

Fulvic Acid is a natural product of humus produced by microorganisms in soil, sediment or aquatic environments. Fulvic acid is a phenolic acid and fungal metabolite isolated from Penicillium for the first time. Fulvic Acid inhibits the dimerization of amyloid b (17-42) (AB17-42), destroys the pre-formed trimer of AB17-42, and binds to the catalytic site of phosphodiesterase 5A (PDE5A), which can regulate the body's immune system, affect the oxidation state of cells, and improve gastrointestinal function. Fulvic Acid can be used as an oxidant or reducing agent and has the potential to study chronic inflammatory diseases such as diabetes.

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.

trans-Miyabenol C is a natural resveratrol trimer, acting as a protein kinase C inhibitor.

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.

PRL-IN-1 (compound 43), a phosphatase of regenerating liver (PRL) inhibitor, directly targets and binds the PRL1 trimer interface, thereby inhibiting PRL1 trimerization. This compound demonstrates potent anticancer activities [1].

Balinatunfib (SAR-441566) is an orally active and highly selective inhibitor of TNFR1 signaling that exerts its mechanism of action by binding to the central pocket of the soluble TNFα (sTNFα) trimer, stabilizing an asymmetric and inactive conformation that selectively blocks interaction with TNFR1 without affecting TNFR2, Balinatunfib suppresses downstream proinflammatory signaling cascades and demonstrating robust anti-inflammatory activity suitable for mechanistic and translational research in autoimmune and inflammatory diseases.