COX-2 Inhibitor

EGFR/COX-2-IN-3 is a selective EGFR/COX-2 dual inhibitor with IC₅₀ values of 0.098 μM and 0.05 μM, respectively. EGFR/COX-2-IN-3 is predicted to have oral activity and blood-brain barrier permeability. EGFR/COX-2-IN-3 exhibits both potent analgesic activity and anti-glioblastoma effects. EGFR/COX-2-IN-3 can be used in the research of tumors such as glioblastoma.

Ramifenazone (Isopropylaminoantipyrine) Standard is the analytical standard of Ramifenazone (HY-B1137). This product is intended for research and analytical applications. Ramifenazone (Isopropylaminoantipyrine) is a pyrazolone non-steroidal anti-inflammatory agent (NSAID) and a potent COX-2 inhibitor. Ramifenazone exhibits analgesic, antipyretic, anti-inflammatory, and antibacterial activities. Ramifenazone can be used for research on inflammation.

Vitacoxib is an Imidazole (HY-D0837) derivative, selective COX-2 inhibitor, anti-inflammatory agent. Vitacoxib can be used in the research of inflammatory diseases, pain and fever.

CHNQD-03005 is an orally active anti-inflammatory agent. CHNQD-03005 inhibits the expression of iNOS and COX-2, reduces inflammatory signal transduction, suppresses NO production, and downregulates the pro-inflammatory cytokines TNF-α, IL-6 and IL-1β. CHNQD-03005 can be used in the research of inflammatory diseases such as colitis.

COX-2/sEH-IN-1 (Compound 9c) is an orally active, dual COX-2 and sEH (soluble epoxide hydrolase) inhibitor with IC₅₀ values of 1.24 µM and 0.40 nM against COX-2 and sEH, respectively. COX-2/sEH-IN-1 shows improved anti-inflammatory activity and highly reduced cardiovascular risks.

Meloxicam sodium is a non-steroidal anti-inflammatory agent that can pass through the blood-brain barrier, inhibits COX activity, with IC₅₀s of 0.49 μM and 36.6 μM for COX-2 and COX-1, respectively.

2,4-Dihydroxybenzaldehyde (Standard) is the analytical standard of 2,4-Dihydroxybenzaldehyde. This product is intended for research and analytical applications. 2,4-Dihydroxybenzaldehyde is an endogenous metabolite. 2,4-Dihydroxybenzaldehyde is a pharmaceutical intermediate that can be used to synthesize various Schiff base compounds. 2,4-Dihydroxybenzaldehyde exhibits significant anti angiogenic, anti-inflammatory, and analgesic activities. 2,4-Dihydroxybenzaldehyde reduces the production of NO and ROS by inhibiting the expression of iNOS and COX-2. 2,4-Dihydroxybenzaldehyde is commonly used in the study of inflammatory conditions.

COX-2-IN-60 is a potent, orally active, and selective COX-2 inhibitor with an IC₅₀ of 0.06 μM. COX-2-IN-60 exhibits ~100-fold selectivity over COX-1 (IC₅₀ = 5.93 ). COX-2-IN-60 reduces oxidative stress and neuroinflammatory cytokines, and effectively counteracts epileptogenesis. COX-2-IN-60 exhibits significant anticonvulsant effects and protects against hippocampal injury by suppressing oxidative stress (reducing MDA and NO), pro-inflammatory signaling (reducing TNF-α and IL-6), and glial activationin in the Pilocarpine (HY-B0726A)-induced seizure mouse model. COX-2-IN-60 can be used for the research on neuroinflammatory and epilepsy.

COX-2-IN-48 (5-25), a COX-2 inhibitor with an IC₅₀ of 51.7 nM for human COX-2, exerts anti-inflammatory and analgesic effects in various rodent models by inhibiting NF-κB pathway. COX-2-IN-48 (5-25) inhibits the degradation of IκB, the phosphorylation and nuclear translocation of NF-κB p65, and the expression of COX-2 and iNOS.

Mycosporine glycine (Mycosporine-Gly) is a mycosporine-like amino acid derived from marine organisms, which possesses free radical scavenging, antioxidant, anti-inflammatory and photoprotective activities. Mycosporine glycine inhibits the UV-induced upregulation of COX-2 mRNA and gene expression levels, scavenges free radicals, ROS and peroxyl radicals, and inhibits free radical chain lipid peroxidation and phosphatidylcholine peroxidation. Mycosporine glycine restores PCOLCE and elastin levels suppressed by ultraviolet radiation, alleviates photooxidative stress and UV-mediated skin cell damage. Mycosporine glycine can be used in studies related to UV-induced skin inflammation, skin photoaging and skin damage.

COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC₅₀=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC₅₀=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss K_i values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect.

LYRM03 is a derivative of Ubenimex (HY-B0134) and a Aminopeptidase N inhibitor. LYRM03 is isolated from Streptomyces HCCB10043. LYRM03 inhibits TLR4, MyD88, NLRP3, ASC, NF-κB and p38 MAPK, stabilizes IκB, and suppresses LPS-induced expression of iNOS and COX-2. LYRM03 reduces the levels of inflammatory cytokines and oxidative stress markers, and alleviates pulmonary edema. LYRM03 exhibits anticancer activity against breast cancer. LYRM03 has anti-inflammatory activity. LYRM03 can be used in the research of acute lung injury and breast cancer.

cis-5-Dodecenoic acid (Standard) is the analytical standard of cis-5-Dodecenoic acid (HY-N8469). This product is intended for research and analytical applications. cis-5-Dodecenoic acid is an inhibitor of COX-I and COX-II with anti-inflammatory activity. cis-5-Dodecenoic acid reduces prostaglandin synthesis by inhibiting COX enzyme activity and is involved in the fatty acid -β oxidative metabolic pathway. The metabolic rate of cis-5-Dodecenoic acid is significantly lower than that of saturated fatty acids. cis-5-Dodecenoic acid can be used in the research of anti-inflammation, fatty acid metabolism mechanisms and related physiological and pathological processes.

Oxaprozin potassium is an orally active and potent COX inhibitor, with IC₅₀ values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin potassium also inhibits the activation of NF-κB. Oxaprozin potassium induces cell apoptosis. Oxaprozin potassium shows anti-inflammatory activity. Oxaprozin potassium-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties.

Taraxerol acetate is a COX-1 and COX-2 inhibitor with IC₅₀ values of 116.3 μM and 94.7 μM, respectively. Taraxerol acetate the has the anticancer potential and induces cell apoptosis.

COX-2-IN-16 (compound 2b) is a potent, selective and orally active COX-2 inhibitor with an IC₅₀ of 102 µM. COX-2-IN-16 inhibits the NO production. COX-2-IN-16 shows anti-inflammatory activity.

EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor. EGFR/COX-2-IN-1 inhibits EGFR^WT, EGFR^T790M, COX-1 and COX-2 with IC₅₀s of 0.12, 0.076, 20.1 and 1.52 μM respectively. EGFR/COX-2-IN-1 inhibits and with IC₅₀s of , respectively. EGFR/COX-2-IN-1 inhibits MCF-7, HT-29 and A-549 with IC₅₀s of 1.20, 5.14 and 14.81 μM, respectively. EGFR/COX-2-IN-1 displays Apoptosis induction by up-regulating Bax and down-regulating Bcl-2 protein levels. EGFR/COX-2-IN-1 results in a significant increase in the percentage of cells at the G2/M in MFC-7 cells. EGFR/COX-2-IN-1 exhibits broad-spectrum antitumor effects.

Nrf2/HO-1 activator 4 is a Nrf2/HO-1 activator. Nrf2/HO-1 activator 4 inhibits nitric oxide production and the expression of pro-inflammatory cytokines IL-1β, IL-6, TNF-α, as well as upstream inflammatory enzymes COX-2 and iNOS. Nrf2/HO-1 activator 4 reduces ROS accumulation, and restores GSH levels and SOD activity. Nrf2/HO-1 activator 4 ameliorates depression-like behaviors in mice. Nrf2/HO-1 activator 4 can be used for research on major depressive disorder.

COX-2-IN-14 (compound 2a) is a potent and selective COX-2 (cyclooxygenase-2) inhibitor. COX-2-IN-14 shows effective binding at the active site of COX-2 co-crystal. COX-2-IN-14 exhibits a high level of in vivo anti-inflammatory activity, reducing ear edema and myeloperoxidase (MPO) activity in mice.

COX-2/Aromatase-IN-1 is a potent dual inhibitor of COX-2 and aromatase. COX-2/Aromatase-IN-1 can simultaneously inhibit COX-2 and aromatase, significantly suppress inflammation and induce proliferation inhibition of breast cancer cells. COX-2/Aromatase-IN-1 exerts anti-breast cancer and anti-inflammatory effects in the MCF-7 breast cancer cell and carrageenan-induced rat paw edema model. COX-2/Aromatase-IN-1 can be used for the study of inflammation and breast cancer.