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.

CU06-1004 (Sac-1004) is an orally active compound that acts as an endothelial dysfunction blocker. It mitigates endothelial dysfunction by inhibiting hyperpermeability and inflammation. The compound demonstrates efficacy in reducing vascular leakage and inflammation across multiple animal models, including those for diabetic retinopathy, stroke, cancer, and inflammatory bowel disease. Additionally, CU06-1004 improves conditions in a CDAA-induced mouse model of NASH and enhances cardiac function [1] [2] [3].

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.

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.

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.

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)

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

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).

Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.

Evolocumab is a human IgG2 monoclonal antibody that binds to human PCSK9 Proprotein Convertase Subtilisin Kexin Type 9).

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].

Aucubin (Rhinanthin) is an iridoid glycoside with anti-inflammatory, anti-microbial, anti-algesic as well as anti-tumor activities.

Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.

Sacubitril/Valsartan (LCZ696) is an orally bioavailable, dual angiotensin II receptor and neprilysin inhibitor for the treatment of hypertension and heart failure.

4-Methylesculetin (Methylesculetin) is one of the coumarin derivatives with great anti-oxidant and anti-inflammatory activities.

Cue-lure (Pherocon (4-(4-Acetoxyphenyl)-2-butanone)) is a standard melon fly attractant

Docusate sodium (Aerosol OT) is an orally available, over-the-counter laxative and stool softener used to treat or prevent constipation. Docusate has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury with jaundice.

Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt/β-catenin pathway, and inhibits LPS induction of iNOS expression [3].

Cuprizone is a copper chelator.Cuprizone is used to induce schizophrenia in mice.Cuprizone induces oligodendrocyte death and induces a demyelination response.

Ensaculin (Anseculin), a novel benzopyrone partially substituted with piperazine, showed memory-enhancing effects in passive and conditioned avoidance paradigms in normal and artificially amnesic rodents. It showed neuroprotective activity in a model of NMDA toxicity and neurotrophic effects in primary cultured rat brain cells.Ensaculin can be used for the treatment of dementia.

Nicodan Percutan (Propylnicotinat) is the propyl ester form of niacin, which is found in various animal and plant tissues to form the coenzymes NAD and NADP.

Cussosaponin C is a natural product isolated from Pulsatilla koreana Nakai.

Aucuparin (2,6-dimethoxy-4-phenylphenol) is a plant antibiotic with anti-inflammatory activity. Aucuparin inhibited pulmonary fibrosis in mouse models induced by bleomycin (BLM). ABTS and FRAP showed clear scavenging activity. Aucuparin inhibited superoxide production of human neutrophils induced by fmlp, and its IC50 was 17.0μM.

Sculponeatin A is a natural product from Rabdosia amethystoides.

Pencycuron (Monceren) is a phenylurea fungicide.

Sacubitril-(2S,4S)-Isomer ((2S,4S)-Sacubitril) is the isomer of Sacubitril which is a neprilysin inhibitor.

MCUF-651 is a guanylyl cyclase A receptor positive allosteric modulators, EC50=0.45 μM.

D-Glucuronic acid sodium salt monohydrate (Sodium D-glucuronate) is a carboxylic acid and highly soluble in water. In humans, glucuronic acid is often linked to toxic or poisonous substances to allow for subsequent elimination, and to hormones to allow for easier transport.

Sodium Glucuronic Acid (4-FLUOROCINNAMONITRILE) is used in the treatment of hepatitis and liver cirrhosis.

6-Chloro-3-indolyl-β-D-Glucuronide (cyclohexylammonium salt) is a chromogenic substrate for β-glucuronidase. 6-Chloro-3-indolyl-β-D-Glucuronide (cyclohexylammonium salt) can be used in the histochemical analysis of β-glucuronidase activity.

Oroxylin A 7-O-β-d-glucuronide was a new alkaloid which found in the bulbs of Lycoris radiata.

Procurcumadiol (5-Hydroxyprocurcumenol) is a natural product found in Curcuma longa and Curcuma phaeocaulis.

MCU-i11 is a novel negative modulator of the MCU, binding MICU1 and impairing muscle cell growth.

Sacubitril Enantiomer (ahu377 isomer 2) is the enantiomer of Sacubitril which is a neprilysin inhibitor.

picumeterol FA is a potent and selective β2-adrenergic receptor agonist. In in vitro and in vivo tests, picumeterol FA produces long-lasting airway smooth muscle relaxation. picumeterol FA is a pure R-enantiomer and can be used to improve lung function and reduce airway hyperresponsiveness in patients with asthma.

Sculponeatin O may have protective effects on the lipid peroxidation-damaged live cells.