COX-2 Inhibitor

LM-4108 (N-(2-Phenylethyl)-indomethacin amide) is a selective and orally active COX-2 inhibitor with an IC₅₀ of 0.06 μM for purified human COX-2. LM-4108 shows anti-inflammatory activity and may be effective in prevention of cancer. Half-lives for the disappearance of 10 μM LM-4108 in rat, human, and mouse liver microsomes were 11 min, 21 min, and 51 min, respectively.

COX-1/2-IN-12 is an orally active dual inhibitor of COX-1 and COX-2, with an IC₅₀ of 41.6 nM against human COX-1 and an IC₅₀ of 31.1 nM against human COX-2. COX-1/2-IN-12 induces antinociceptive activity and inhibits edema in in vivo experiments. COX-1/2-IN-12 can be used in research related to inflammation and pain.

Arnicolide B is a sesquiterpene lactone. Arnicolide B is isolated from Centipeda minima. Arnicolide B inhibits the phosphorylation of ERK, JNK and p38 proteins in the MAPK signaling pathway. Arnicolide B reduces the production of inflammatory mediators NO, PGE₂ and IL-6. Arnicolide B downregulates the overexpression of inflammatory proteins iNOS and COX-2. Arnicolide B has no effect on IκB-α degradation or NF-κB pathway activation. Arnicolide B is applicable to inflammation-related research.

COX-2-IN-5 (compound 11a) is a potent COX-2 inhibitor with an IC₅₀ value of 0.65 µM. COX-2-IN-5 has the potential for the research of inflammation.

(-)-Salcolin B (Tricin 4'-O-(threo-β-guaiacylglyceryl) ether) is an isomer of Salcolin B (HY-N16766) and anti-inflammatory agent. (-)-Salcolin B is isolable from Njavara. (-)-Salcolin B downregulates the activities of NF-κB and STAT3, reduces the expressions of iNOS and COX-2, activates the ERK signaling pathway, and inhibits LPS-induced NO and ROS production. (-)-Salcolin B induces Apoptosis. (-)-Salcolin B inhibits TPA (HY-18739)-induced ear edema. (-)-Salcolin B possesses antioxidant activity. (-)-Salcolin B can be used in research related to inflammatory diseases, colon adenocarcinoma, ovarian cancer and breast cancer.

Ginsenoside Rb3 (Standard) is the analytical standard of Ginsenoside Rb3. This product is intended for research and analytical applications. Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC₅₀ of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.

ISP-VT (Isopropyl vanillate) is a COX-2 inhibitor. ISP-VT exhibits anti-inflammatory, antipyretic and immunomodulatory activities. ISP-VT reduces neutrophil migration and the release of inflammatory factors. ISP-VT can be used for the research of inflammatory and immune diseases and other conditions.

G721-0282 is an orally active CHI3L1 inhibitor. G721-0282 can reduce the expression of inflammatory proteins and cytokines. G721-0282 inhibits the activation of the NF-κB signaling pathway. G721-0282 inhibits neuroinflammation and reduces anxious behavior. G721-0282 significantly inhibits the proliferation of osteosarcoma (OS) cells by suppressing the STAT3 signaling pathway. G721-0282 induces OS cell apoptosis by upregulating pro-apoptotic protein levels and downregulating anti-apoptotic protein levels. G721-0282 can be used for researches on neuroinflammatory conditions and cancer.

COX-2-IN-17 (compound 10) is a potent and BBB-penetrated COX-2 (cyclooxygenase-2) inhibitor, with an IC₅₀ of 0.02 μM. COX-2-IN-17 shows anti-inflammatory and analgesic activities. COX-2-IN-17 attenuates hyperalgesia in the neurogenic phase as well as the inflammatory phase.

VI-60 is a dual, orally active inhibitor of cPLA₂ and COX-2, which reveals an anti-inflammtory efficacy through the inhibition of p38 MAPK/cPLA₂/COX-2/PGE₂ pathway.

Ginsenoside C-K (Standard) is the analytical standard of Ginsenoside C-K. This product is intended for research and analytical applications. Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.

COX-2/5-LOX-IN-8 is an orally active dual COX-2/5-LOX inhibitor, with an IC₅₀ of 6.30 μM against sheep-derived COX-2 and an IC₅₀ of 8.09 μM against 5-LOX. COX-2/5-LOX-IN-8 acts as a membrane stabilizer that stabilizes erythrocyte membranes against hypotonicity-induced hemolysis. COX-2/5-LOX-IN-8 functions as a protein stabilizer that inhibits heat-induced denaturation of bovine serum albumin. COX-2/5-LOX-IN-8 reduces paw swelling, improves hind limb weight-bearing function, decreases serum levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, CRP), and lowers serum levels of cartilage degradation biomarkers (COMP, MMP-3, CTX-II). COX-2/5-LOX-IN-8 can be used in the research of osteoarthritis.

COX-2/15-LOX-IN-6 (Compound 5l) is the dual inhibitor for COX-2 and 15-LOX, with IC₅₀ of 0.201 μM and 11.723 μM. COX-2/15-LOX-IN-6 inhibits the expression of PGE, TNF-α, IL-6 and iNOS in serum, and exhibits anti-inflammatory effect in Carrageenan (HY-125474)-induced rats edema model.

δ-Viniferin is a COX-1/COX-2 inhibitor (with an IC₅₀ of 5 µM for both enzymes). δ-Viniferin induces the expression of SIRT1, catalase and HO-1, promotes the phosphorylation of eNOS, and stimulates nitric oxide (NO) production. δ-Viniferin is applicable to research related to atherosclerosis, downy mildew, Gram-positive bacterial infections, inflammation, infections, cardiovascular diseases and diabetes.

Neuroprotective agent 18 is a potent neuroprotective agent. Neuroprotective agent 18 inhibits the activity of NF-κB thereby significantly downregulating the expression of downstream pro-inflammatory mediators (TNF-α, IL-6) and inflammatory enzymes (COX-2) in the hippocampus. Neuroprotective agent 18 binds to AChE thereby partially inhibiting it and modulating cholinergic neurotransmission. Neuroprotective agent 18 can be used in research on Alzheimer's disease.

COX-2-IN-51 (E25) is a potent COX-2 inhibitor, with an IC₅₀ of 70.7 nM. COX-2-IN-51 significantly inhibits LPS-induced release of NO and PGE2, expression of COX-2 and iNOS, and activation of NF-κB pathway. COX-2-IN-51 exhibits anti-inflammatory and analgesic effects in diverse murine models through inhibiting NF-κB pathway. COX-2-IN-51 has lower gastrointestinal side effects than Indomethacin (HY-14397).

EGFR/VEGFR2-IN-11 is an EGFR/VEGFR2 inhibitor with IC₅₀ values of 0.62 μM (human EGFR), 2.26 μM (human VEGFR-2), 17.38 μM (human COX-2), and 19.31 μM (human tubulin). EGFR/VEGFR2-IN-11 inhibits COX-2 activity and tubulin polymerization. EGFR/VEGFR2-IN-11 induces cell cycle arrest and apoptosis. EGFR/VEGFR2-IN-11 exerts selective and antiproliferative activity against human cancer cells. EGFR/VEGFR2-IN-11 can be used for the research of colon carcinoma, breast carcinoma, leukemia, lymphoma, glioblastoma.

COX-2-IN-65 is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ of 10.24 μM. COX-2-IN-65 inhibits Staphylococcus aureus and Escherichia coli growth. COX-2-IN-65 scavenges reactive oxygen species (ROS). COX-2-IN-65 can be used for the researches of bacterial infections and inflammation.

COX-2-IN-58 is a COX-2 inhibitor. COX-2-IN-58 exhibits remarkable anti-inflammatory activity in Carrageenan (HY-125474)-induced paw edema model of Balb/C mice. COX-2-IN-58 can be used for the research of inflammation.

Ginsenoside Rd (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.