cu+

CU-CPD107 is a selective agonist of toll-like receptor 8 (TLR8) and also shows activation activity against ssRNA ligands. CU-CPD107 acts as an inhibitor of TLR8 signaling in the presence of R848 (IC50=13.7 μM). CU-CPD107 exhibited coagonist activity in the presence of ssRNA, while CU-CPD107 alone could not affect TLR8 signal transduction.

CU-115 is a selective and potent TLR8 antagonist with IC50 of 1.04 µM and =>50 µM for TLR8 and TLR7, respectively. CU-115 decreases production of TNF-α and IL-1β activated by R-848 in THP-1 cells.

CU-T12-9 is a potent TLR1 2 agonist(EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay). It acts by activating the NFkB pathway, upregulating proinflammatory cytokines, and enhancing TLR1 and TLR2 dimerization.CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1 2 heterodimer, not TLR2 6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.

CU-CPT9b (TLR8-specific antagonist 1) is an antagonist of toll-like receptor 8 (TLR8; Kd = 21 nM). It inhibits activation of NF- B induced by the TLR8 agonist R-848 in TLR8-overexpressing HEK-Blue cells with an IC50 value of 0.7 nM.

CU-CPT-9a is a potent TLR8 inhibitor (IC50 : 0.5 nM), that suppresses TLR8-mediated proinflammatory signaling in various cell lines and human primary cells-

(5Z,2E)-CU-3 is a potent and highly selective inhibitor of the DGKα isozyme with an IC50 value of 0.6 μM, competing with ATP and exhibiting a Km value of 0.48 mM. It specifically targets the catalytic region of DGKα without affecting the regulatory region and has demonstrated antitumor and immunogenic effects by promoting cancer cell apoptosis and T cell activation.

CU-CPT17e is a potent agonist of TLR(TLR3, TLR8, and TLR9).

CU-CPT22 is the first probe for the complex between toll-like receptors TLR1 and TLR2. CU-CPT22 binds at the interface of TLR1 and TLR2 (IC50 = 0.58 μM). It competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1 2 (Ki: 0.41 μM).

FA4-Cu is a compound formed from the effective pancreatic cancer inhibitor FA4 and Cu(II), which can induce apoptosis by triggering ER and mitochondrial stress.

CU-3 is a potent and selective inhibitor of diacylglycerol kinase alpha (DGKalpha). CU-3 attenuates cancer cell proliferation and simultaneously enhances immune responses including anti-cancer immunity.

CU-32 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50= 0.45 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. It is also selective for cGAS over toll-like receptors (TLRs) at 50 μM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP synthase inhibitorsJ. Org. Chem.85(3)1579-1600(2020)

CU-76 is an inhibitor of cyclic GMP-AMP synthase (cGAS; IC50= 0.24 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. CU-76 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP synthase inhibitorsJ. Org. Chem.85(3)1579-1600(2020)

Cu (II) Protoporphyrin IX functions as a negative control for Zn (II) Protoporphyrin, a heme oxygenase inhibitor. Heme oxygenase is involved in tumor cell resistance to chemotherapy and the regulation of free radical formation, inflammation, and vascular repair.

Cu(II)GTSM is a cell permeable copper complex that significantly inhibits GSK3β activity and suppresses levels of neurotoxic amyloid β-trimers and phosphorylated tau, and is able to reverse cognitive deficits in Alzheimer's disease mice.

CU-6PM is a new fluorescent RXR agonist. CU-6PMN was designed based on the fact that umbelliferone emits strong fluorescence in a hydrophilic environment, but the fluorescence intensity decreases in hydrophobic environments such as the interior of proteins. The developed assay CU-6PMN enabled screening of rexinoids to be performed easily within a few hours by monitoring changes of fluorescence intensity with widely available fluorescence microplate readers, without the need for processes such as filtration.

CU-2010 is a synthetic serine protease inhibitor with antifibrinolytic and anticoagulant properties. CU-2010 dose-dependently reduces postoperative blood loss and improves postischemic recovery after cardiac surgery in a canine model.

CU-CPT-8m (TLR8-specific antagonist) is an toll-like receptor 8 (TLR8) antagonist (IC50 : 67 nM)

SA09-Cu is a potent, noncompetitive inhibitor of NDM-1, with an IC50 of 9.6 nM. It inactivates NDM-1 by oxidizing the enzyme's Zn(II)-thiolate site and resists reduction by bacterial intracellular thiols. SA09-Cu effectively restores Meropenem efficacy against various clinical NDM-1-producing carbapenem-resistant Enterobacteriaceae (CRE) and hampers the progression of carbapenem resistance [1].

Cu(II)-Elesclomol is a complex formed by the anticancer agent Elesclomol and Cu(II), which selectively transports copper to mitochondria.Cu(II)-Elesclomol has anticancer activity, inhibits the growth of human leukemia K562 cells, and induces cell-cycle arrest, and is used in the study of leukemias.

GHK-Cu acetate, a complex of the tripeptide Gly-His-Lys and a copper(II) ion, exhibits wound healing and anti-inflammatory properties. It enhances fibroblast proliferation, collagen production, and the release of pro-matrix metalloproteinase-2 (MMP-2) and glycosaminoglycans (GAGs), while also increasing decorin expression in rat wound tissue. Furthermore, at a concentration of 10 µM, it reduces levels of reactive oxygen species (ROS), interleukin-6 (IL-6), and tumor necrosis factor-alpha (TNF-α) in LPS-stimulated RAW 264.7 cells. Additionally, GHK-Cu at 10 µg/g mitigates LPS-induced reductions in lung superoxide dismutase (SOD) activity and glutathione (GSH) levels, decreases the accumulation of cells and total protein in bronchoalveolar lavage fluid (BALF), and thus, attenuates acute lung injury in mice.

Cu(Ⅱ)-EDTA disodium tetrahydrate is a complex of EDTA with heavy metals and is recognized as a common pollutant found in industrial wastewater. It is utilized in research focused on the recovery of heavy metals from mixed wastewater.

Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood. Remibrutinib is an effective and orally active Bruton tyrosine kinase inhibitor (IC50: 1 nM). Remibrutinib has the potential for Chronic urticaria (CU) treatment.

EML631 is a potent and selective SPIN1 inhibitor (SPIN1 Kd= 3 microM).

Esomeprazole Magnesium (NEXIUM) is the S-isomer of omeprazole, can reduce gastric acid secretion with selective and irreversible proton pump inhibitor activity.Esomeprazole magnesium acts as an exosome inhibitor by blocking the exosome release via the inhibition of V-H+-ATPases