cu+

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-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-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-

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.

Copper Tripeptide-3 (AHK-Cu) is a bioactive peptide known to promote hair growth and is reported to be used as a cosmetic ingredient [1].

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-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-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(II)GTSM, a cell-permeable copper-complex, effectively inhibits GSK3β and shows inhibitory effects against Amyloid-β oligomers (AβOs) while reducing tau phosphorylation. Additionally, Cu(II)GTSM decreases the abundance of Amyloid-β trimers. With its potential as an anticancer and antimicrobial agent, Cu(II)GTSM exhibits promising therapeutic capabilities.

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.

TLR3-IN-1 (CU CPT 4a) is a selective TLR3 inhibitor (IC50: 3.44 μM in RAW 264.7 cells). It can inhibit TLR3/dsRNA complex-mediated downstream signaling pathways and inhibit the production of TNF-α and IL-1β in whole cells.

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(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.

(5Z,2E)-CU-3 is a potent and selective inhibitor of DGKα isozyme with an IC50 value of 0.6 μM and inhibition of DGKα by competing ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 is selective, targeting the catalytic region of DGKα, but does not act on the regulatory region. (5Z,2E)-CU-3 has antitumor and immunogenic effects, promoting apoptosis of cancer cells and activation of T cells.

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

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-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.

Copper tripeptide (GHK-Cu) is a naturally occurring copper complex of the tripeptide glycyl-L-histidyl-L-lysine. The tripeptide has strong affinity for copper(II) and was first isolated from human plasma. It can be found also in saliva and urine.

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-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)

NUN82647 (CU-242) is an Inhibitor of cell cycle at G2 phase, and apoptosis inducer.

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

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).

Prolyl-4-hydroxylase Inhibitor 11, a novel proline 4-hydroxylase inhibitor, shows protective effects against oxidative stress and Cu(II) toxicity in Chlorella vulgaris.

4-Ethylcatechol is present in red wine and can be extracted from Glechoma longituba (NaKai) Kupr.4-Ethylcatechol induces DNA damage in the presence of Cu(II).4-Ethylcatechol is a potent antiplatelet compound.

Chitotriose trihydrochloride is an orally active chitooligosaccharide known for its antioxidant properties. It effectively inhibits the hydroxylation of benzoate to salicylate by H 2 O 2 in the presence of Cu 2+, with an IC 50 value of 80 μM.

Salpyran is a selective chelator for Cu(II) ions, exhibiting potential therapeutic applications [1].

Iron (III) hexacyanoferrate (II) is a useful organic compound for research related to life sciences. The catalog number is T35378 and the CAS number is 14038-43-8.

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

DL-Alanine (DL-2-Aminopropionic acid) is an amino acid that is a racemic compound of L- and D-alanine.DL-Alanine is often used as a reducing and capping agent in conjunction with aqueous silver nitrate for nanoparticle generation.DL-Alanine is a sweetening agent, and can be grouped with glycine and sodium saccharin.DL-Alanine plays an important role in glucose-alanine cycling between tissues and liver.DL-Alanine can be used to study the chelation of transition metals such as Cu, Zn, and Cd. DL-Alanine plays an important role in the glucose-alanine cycle between tissues and the liver.DL-Alanine can be used to study the chelation of transition metals such as Cu, Zn, and Cd.

6,8-Diprenyleriodictyol is an antioxidant, which inhibits Cu(2+)-mediated oxidation of human low density lipoprotein (LDL).

Diglycyl-histidine is a tripeptide complexed with cupric ion designed to mimic specific Cu(II) transport site of ascorbate on albumin molecule.

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

Salinazid (Salicylaldehyde isonicotinoyl hydrazone) is a potent Cu(II) ionophore which preferentially kills HepG2 cells over HUVEC cells, and is superior to clioquinol.

BTTAA, a Cu(I)-stabilizing ligand, performs potently with ubiquitin Glu18AzF.

The metallo-protein Cu/Zn-superoxide dismutase (SOD1) is a ubiquitous enzyme responsible for scavenging superoxide radicals. Mutations in SOD1, which alter its metal binding capacity and can result in protein misfolding and aggregation, have been linked to familial amyotrophic lateral sclerosis (ALS). Cu-ATSM is an orally bioavailable, blood-brain barrier permeable complex that has traditionally been used in cellular imaging experiments to selectively label hypoxic tissue via its susceptibility to reduction by oxygen-depleted mitochondria. More recently, Cu-ATSM has been reported to improve locomotor function and survival in a transgenic ALS mouse model by delivering copper specifically to cells in the spinal cords of mice producing misfolded SOD1 proteins. Copper chaperone for SOD (CCS) is presumed to utilize the copper from Cu-ATSM to prevent misfolding of the SOD1 protein.

DL-Alanine-2,3,3,3-d4 is a deuterated compound of DL-Alanine. DL-Alanine has a CAS number of 302-72-7. DL-Alanine is an amino acid that is a racemic compound of L- and D-alanine.DL-Alanine is often used as a reducing and capping agent in conjunction with aqueous silver nitrate for nanoparticle generation.DL-Alanine is a sweetening agent, and can be grouped with glycine and sodium saccharin.DL-Alanine plays an important role in glucose-alanine cycling between tissues and liver.DL-Alanine can be used to study the chelation of transition metals such as Cu, Zn, and Cd. DL-Alanine plays an important role in the glucose-alanine cycle between tissues and the liver.DL-Alanine can be used to study the chelation of transition metals such as Cu, Zn, and Cd.

Temocapril hydrochloride (CS-622 HCl), the hydrochloride of Temocapril, is a long-acting ACE inhibitor used for the therapy of hypertension.

Temocapril is an inhibitor of tyrosine kinase.

D-Glucaric acid potassium (D-Saccharic acid potassium salt) is a compound formed from oxidizing sugars, which can be used to test for the presence of hepatic enzyme induction. Studies indicate that D-glucuronolactone dehydrogenase oxidizes D-Saccharic acid potassium salt into D-glucaro-l,4;6,3-dilactone. Alternate studies suggest that D-Saccharic acid potassium salt forms a complex with Cu(II) and H2O2to decolorize azo, acridine, triphenyl methane, anthraquinone and thiazine-based dyes.

Esomeprazole Magnesium trihydrate ((S)-Omeprazole magnesium trihydrate) is a proton pump inhibitor indicated for the short-term treatment of gastroesophageal reflux disease in patients with a history of erosive esophagitis.Esomeprazole magnesium trihydrate acts as an exosome inhibitor by blocking the exosome release via the inhibition of V-H+-ATPases

1. Tiliroside (Tribuloside) shows anticarcinogenic activity. 2. Tiliroside shows hepatoprotective activity. 3. Tiliroside shows antioxidant and anti-inflammatory activity, can inhibit neuroinflammation in neurodegenerative disorders. 4. Tiliroside has anti-diabetic effect, are at least partially mediated through inhibitory effects on carbohydrate digestion and glucose uptake in the gastrointestinal tract. 5. Tiliroside and gnaphaliin are antioxidants against in vitro Cu(2+)-induced LDL oxidation in the same order of magnitude compared to that of the reference drug, probucol. 6. Tiliroside enhances fatty acid oxidation via the enhancement adiponectin signaling associated with the activation of both AMP-activated protein kinase and peroxisome proliferator-activated receptor α and ameliorates obesity-induced metabolic disorders.

Pyclen is an inhibitor of cell death induced by oxidative stress and an inhibitor of AB1-40 aggregation induced by Cu2+ ion. It can both prevent and disrupt Cu(2+) induced AB(1-40) aggregation.

AqB007 is a selective blocker of the Aquaporin-1 ion channel conductance, thereby slowing cancer cell migration.

Salpyran is a Cu(II) selective chelator with therapeutic potential.

CB2 PET Radioligand 1 (compound [18F]9) is a positron emission tomography (PET) radioligand with high affinity for the human cannabinoid receptor 2 (hCB2, Ki=7.7 nM). It is synthesized via Cu-mediated 18F-fluorination and demonstrates significant brain uptake in a mouse model of neuroinflammation [1].

NSC 689534 forms a chelate with copper (Cu 2+), resulting in the NSC 689534/Cu 2+ complex, which is a potent inducer of oxidative stress and exhibits antitumor activity [1].

Docosahexaenoic acid alkyne, an ω-alkyne derivative of docosahexaenoic acid, enables Cu(I)-catalyzed cycloaddition with azide-containing molecules for efficient click chemistry applications. It can be further utilized to produce alkyne-modified products like glycerophospholipids. Additionally, this compound permits the monitoring of fatty acid metabolism in cells through click chemistry linkage to fluorophores.

AChE/BuChE-IN-1, a selective butyrylcholinesterase (BuChE) inhibitor derived from chrysin, exhibits a potent efficacy with an IC50 of 0.48 μM against BuChE and a lesser inhibitory effect on acetylcholinesterase (AChE) with an IC50 of 7.16 μM. It demonstrates significant hydroxyl radical (·OH) scavenging activity, achieving an IC50 of 0.1674 μM, and effectively inhibits reactive oxygen species (ROS) and Aβ 1-42 aggregation, including self-aggregation, copper (Cu 2+)-induced, and AChE-induced aggregation. Characterized by high blood-brain barrier (BBB) permeability, bioavailability, and low cellular toxicity, AChE/BuChE-IN-1 holds promising potential for Alzheimer's disease (AD) research.

CU239 is a selective non-retinoid inhibitor of RPE65 which suppresses visual cycle and prevents retinal degeneration.

L-Alanine (L-2-Aminopropionic acid) is an Amino Acid. The chemical classification of alanine is Amino Acids. Alanine is a small non-essential amino acid in humans, Alanine is one of the most widely used for protein construction and is involved in the metabolism of tryptophan and vitamin pyridoxine.

Alanine is a nonessential amino acid made in the body from the conversion of the carbohydrate pyruvate or the breakdown of DNA and the dipeptides carnosine and anserine. D-Alanine ((R)-Alanine) is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.

β-Alanine (3-Aminopropanoic acid) is a naturally occurring beta amino acid formed in vivo by the degradation of dihydrouracil and carnosine. It acts as a neurotransmitter by activating glycine and GABA receptors.