COX-2 Inhibitor

Jaceosidin (Standard) is the analytical standard of Jaceosidin. This product is intended for research and analytical applications. Jaceosidin is a flavonoid isolated from Artemisia vestita, induces apoptosis in cancer cells, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin exhibits anti-cancer, anti-inflammatory activities, decreases leves of inflammatory markers, and suppresses COX-2 expression and NF-κB activation.

EGFR-IN-190 (Compound 3o) is an inhibitor that targets both EGFR (IC₅₀ = 0.028 μM) and COX-2 (IC₅₀ = 0.208 μM). EGFR-IN-190 exhibits potent inhibitory activity against MCF-7 cells and induces apoptosis (apoptosis). EGFR-IN-190 can be used for research on breast cancer.

COX-2/CA II-2 is an orally active dual selective inhibitor targeting COX-2 and hCA II. COX-2/CA II-2 inhibits COX-2 with an IC₅₀ value of 0.05 μM (SI = 12.02 vs COX-1) and hCA II with a K_i value of 62.6 nM (SI = 704.2 vs hCA I). COX-2/CA II-2 demonstrates significant analgesic and anti-inflammatory effects with rapid onset and sustained duration in animal models, shows improved gastric safety with reduced ulcerogenic liability, and exhibits a gradual intraocular pressure (IOP)-lowering effect without statistical significance relative to the sham-treated eye in rabbit glaucoma models. COX-2/CA II-2 can be used for anti-inflammatory, analgesic and antiglaucoma research.

JNUTS013 is a NLRP3 inflammasome inhibitor. JNUTS013 promotes proteasome-dependent degradation of NLRP3 and inhibits the release of downstream cytokines. JNUTS013 downregulates the expression of inflammation-related proteins including iNOS and COX-2. JNUTS013 exhibits anti-inflammatory activity and can be used in the research of inflammatory diseases.

Brazzein is a functional sweetener with antioxidant, anti-inflammatory, and anti-allergic activities.

COX-1-IN-1 (compound 15a) is a selective inhibitor for cyclooxygenase (COX), with IC₅₀s of 0.23 μM (COX-1) and >50 μM (COX-2), selective index (COX-2 IC₅₀/COX-1 IC₅₀) is 217. COX-1-IN-1 inhibits platelet aggregation.

Desmethyl etoricoxib (example 21) is a selective COX-2 inhibitor with an IC₅₀ of 1 μM in whole blood. Desmethyl etoricoxib inhibits COX-1 with an IC₅₀ of 16 μM in U937 cells. Desmethyl etoricoxib has anti-inflammatory effects.

COX-2/LOX-IN-1 (compound 5) is a dual cyclooxygenase-2/lipoxygenase (COX-2/LOX) inhibitor with IC₅₀s of 30 μM and 0.55 μM, for LOX and COX-2, respectively. .

COX-1/2-IN-2 is a potent COX1/2 inhibitor. COX-1/2-IN-2 exhibits significant inhibitory effect against COX-1 and COX-2 inhibitor with IC₅₀ values of 9.7 ± 0.09 µM and 4.6 ± 1.45 µM, respectively.

Topo I/COX-2-IN-2 (Compound W10) is a potent dual-target inhibitor of Topo I and COX-2 with IC₅₀ values of 0.90 μM and 2.31 μM, respectively. Topo I/COX-2-IN-2 induces cancer cell apoptosis through the mitochondrial pathway.

Sargachromanol E is an apoptosis inducer, anti-inflammatory agent, and anti-aging agent. Sargachromanol E activates caspase-3, mediates PARP cleavage, downregulates Bcl-xL and upregulates Bax levels, and drives sub-G1 phase cell cycle arrest, inhibits LPS-induced COX-2 and iNOS transcription and expression (NO: IC₅₀ = 6.99 μg/mL), reduces p38 MAPK and ERK1/2 phosphorylation levels, and suppresses the release of pro-inflammatory mediators such as TNF-α, IL-1β, and prostaglandin E₂ (PGE₂). Sargachromanol E can be used for research on skin aging, leukemia, oral squamous cell carcinoma, and inflammation-related studies.

Cassiatannin A is a tetramer of proanthocyanidin (HY-N0794) found in Cinnamomum cassia. Cassiatannin A shows COX-2 inhibitor activity with inhibition rate of 38, 52 and 97% at 10, 100 and 1000 μg/mL. Cassiatannin A can be used for the research of inflammation.

TX-1123 is a potent protein tyrosine kinase (PTK) inhibitor for Src, eEF2-K, and PKA, and EGFR-K/PKC. TX-1123 is a cyclo-oxygenase (COX) inhibitor with IC₅₀ values of 1.16 μM and 15.7 μM for COX2 and COX1, respectively. TX-1123 has low mitochondrial toxicity. TX-1123 can be used in research of cancer.

Hordenine-d₆ hydrochloride (Ordenina-d₆ hydrochloride; Peyocactine-d₆ hydrochloride) is the deuterated-labeled Hordenine hydrochloride (HY-N0113B). Hordenine hydrochloride (Ordenina hydrochloride; Peyocactine hydrochloride) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine hydrochloride inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine hydrochloride inhibits melanin synthesis in melanocytes and reconstructed epidermis. Hordenine hydrochloride activates the Wnt/β-catenin signaling pathway. Hordenine hydrochloride activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine hydrochloride inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine hydrochloride limits alcohol intake, reduces relapse drinking behavior. Hordenine hydrochloride can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.

COX-2-IN-21 (Compound 5c) is a selective and orally active COX-2 inhibitor with an IC₅₀ of 0.039 μM. COX-2-IN-21 shows promising anti-inflammatory potential.

COX-2-IN-70 is an orally active and selective COX-2 inhibitor with an IC₅₀ of 1.86 μM. COX-2-IN-70 reduces the production of prostaglandins and thromboxanes by inhibiting the COX-2 isoenzyme. COX-2-IN-70 can be used for inflammation research.

Anti-inflammatory agent 109 (Compound 2m) is an anti-inflammatory agent. Anti-inflammatory agent 109 directly interacts with p65, attenuates aberrant activation of the NF-κB pathway. Anti-inflammatory agent 109 significantly suppresses the release of key pro-inflammatory mediators, including IL-1β, COX-2, and iNOS. Anti-inflammatory agent 109 conferres robust protection against LPS-induced acute liver injury in septic mice.

Longiferone B is a daucane sesquiterpene, that can be isolated from Boesenbergia longiflora rhizomes. Longiferone B shows anti-inflammatory activity against NO release with an IC₅₀ of 21.0 μM. Longiferone B also suppresses the iNOS and COX-2 mRNA expression.

MAO-B-IN-56 is a multi-target-directed ligand with AChE, BChE, MAO-B, and BACE1 inhibitory activity, with IC₅₀ values of 0.35 μM, 3.22 μM, 0.14 μM, and 3.85 μM respectively, and shows selectivity for AChE over BChE and MAO-B over MAO-A.MAO-B-IN-56 reduces amyloid-beta production, reduces paw edema, improves spatial memory, and enhances Alzheimer's disease hallmarks and associated histopathological alterations.MAO-B-IN-56 can be used for the research of alzheimer's disease.

COX-2-IN-27 is a potent and selective COX-2 inhibitor with IC₅₀ values of 13.22, 0.045, 1.67 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-27 shows anti-inflammatory activity.