COX-2 Inhibitor

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.

BChE-IN-46 is a selective and brain-penetrant BChE inhibitor (eqBChE IC₅₀ = 7.44 × 10⁻⁵ μM, SI > 270,000; hBChE, IC₅₀ = 1.48 × 10⁻³ μM). BChE-IN-46 has COX-2 inhibitory activity (IC₅₀ = 0.11 μM). BChE-IN-46 exhibits neuroprotective effects, enhances acetylcholine levels, and alleviates cognitive deficits, anxiety, and learning/memory impairments. BChE-IN-46 can be used for the development of anti-Alzheimer's disease drugs.

Anti-inflammatory agent 122 is an orally active anti-inflammatory agent. Anti-inflammatory agent 122 inhibits the activation of the NF-κB signaling cascade. Anti-inflammatory agent 122 downregulates the phosphorylation levels of JNK, p38 MAPK and ERK, thereby inhibiting the activation of the MAPK pathway. Anti-inflammatory agent 122 reduces the levels of pro-inflammatory cytokines TNF-α, IL-1β, iNOS and COX-2. Anti-inflammatory agent 122 alleviates paw swelling symptoms in rats with adjuvant-induced arthritis. Anti-inflammatory agent 122 can be used in studies related to adjuvant-induced arthritis.

1-Hydroxy-4αH-1,10-secoeudesma-5(6),10(14),11(13)-trien-12,8β-olide is a neuroprotective agent. 1-Hydroxy-4αH-1,10-secoeudesma-5(6),10(14),11(13)-trien-12,8β-olide reduces the protein expression levels of iNOS and COX-2, blocks the DNA-binding activity of NF-κB, and inhibits nitric oxide production. 1-Hydroxy-4αH-1,10-secoeudesma-5(6),10(14),11(13)-trien-12,8β-olide promotes the polarization of microglia to the M2 phenotype by inducing the production of Arg-1, and alleviates cell damage induced by H₂O₂ and 6-Hydroxydopamine (HY-B1081).

EGFR/VEGFR2-IN-10 is a selective EGFR, VEGFR2 and COX2 inhibitor with IC₅₀s of 8.5, 68 and 158 nM, respectively. EGFR/VEGFR2-IN-10 induces G1-phase cell cycle arrest in MCF-7 cells. EGFR/VEGFR2-IN-10 increases the Bax/Bcl-2 ratio, upregulates caspase-8, and elevates caspase-9 protein levels, confirming activation of the intrinsic apoptotic pathway. EGFR/VEGFR2-IN-10 demonstrates exceptional therapeutic potential by simultaneously inhibiting tumor proliferation, angiogenesis, and inflammation pathways while maintaining a favorable selectivity profile. EGFR/VEGFR2-IN-10 can be used as a research tool for cervical, liver, colon, and breast cancer studies.

COX-1-IN-4 (Compound P10) is a selective COX-1 inhibitor (IC₅₀s: COX-1 = 0.09 μM; COX-2 = 2.49 μM). COX-1-IN-4 reduces the production of NO as well as the expression of the iNOS protein. COX-1-IN-4 can be used in the research of neuroinflammation.

COX-2-IN-47 (compound 6c ) is a selective COX-2 inhibitor with IC₅₀ value of 0.03 μM. COX-2-IN-47 has antiedema activity.

iNOS/COX-2-IN-1 (Compound 12e) is an inhibitor of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS). iNOS/COX-2-IN-1 inhibits the NF-κB and MAPKs signaling pathways and thus exerts anti-inflammatory effects.

GG13 is an anti-inflammatory peptide. GG13 reduces the expression of STAT1, NOS2, COX2, and CD40. GG13 decreases the expression and secretion of iNOS and TNF-α proteins. GG13 is applicable to the research of inflammatory diseases.

Zidometacin is a nonsteroidal anti-inflammatory agent. Zidometacin significantly inhibits prostaglandin synthesis with low gastrolesive influence. Zidometacin has antinociceptive and antipyretic activities and shows relatively low ulcerogenicity in rat models. Zidometacin can be used for analgesia and osteoarthritis research.

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 13.9 ± 3.21 µM and 6.4±0.74 µM, respectively.

SIN 14, a derivative of Sinomenine (HY-15122), is an orally active HO-1 activator (K_D = 17.2 μM). SIN 14 binds to the catalytic core domain of HO-1 and induces HO-1 activation in catalysis. SIN 14 significantly increases HO-1 stability. SIN 14 has anti-inflammatory effects and inhibits M1 macrophage polarization while promoting M2 polarization in LPS (Lipopolysaccharides)(HY-D1056)-induced RAW264.7 cells. SIN 14 inhibits inflammatory mediator production (eg: NO, IL-6, IL-1β and CCL2, inhibits production of ROS and down-regulates the expression of COX-2 and iNOS. SIN 14 can inhibit RA-related inflammatory edema in collagen-induced arthritis (ClA) mice.

COX-2-IN-46 (compound 5m) is an anti-inflammatory agent with potent analgesic activity. COX-2-IN-46 exhibits a significant inhibitory effect on COX-2 (IC₅₀=87.74 nM).

COX-2-IN-31 (compound 7b) is an orally active and dual inhibitor of COX-2 (IC₅₀=60 nM) and 5-LOX (IC₅₀=1.9 μM). COX-2-IN-31 also inhibits transmembrane hCA IX(K_i=48.9 nM) and hCA XII(K_i=5.8 nM) activity. COX-2-IN-31 exhibits anti-inflammatory and analgesic activity.

COX-2-IN-10 is a potent COX-2 inhibitor. COX-2-IN-10 inhibits the production of PGE₂ in concentration dependent manner (IC₅₀=2.54 µM). COX-2-IN-10 inhibits the expression of iNOS and COX-2 on mRNA and protein level . COX-2-IN-10 inhibits the production of IL-6, TNF-α and IL-1β.

Anti-inflammatory agent 111 is a potent anti-inflammatory agent. Anti-inflammatory agent 111 reduces Lipopolysaccharides (LPS) (HY-D1056)-induced i-NOS and COX-2 protein expression, decreases nitric oxide, IL-6, and TNF-α production. Anti-inflammatory agent 111 maintains normal cell viability at bioactive concentrations.Anti-inflammatory agent 111 can be used for the research of inflammation-related disorders.

Ephemeranthol A is a phenanthrene compound with anticancer and anti-inflammatory activities. Ephemeranthol A exerts significant anti-inflammatory effects in macrophages by inhibiting the NF-κB and MAPK signaling pathways. Ephemeranthol A induces apoptosis and inhibits metastasis of lung cancer cells by suppressing the FAK/Akt signaling and EMT processes. Ephemeranthol A can be used for the research of acute and chronic inflammatory diseases and non-small cell lung cancer.

5α-Epoxyalantolactone is an orally active, blood-brain barrier-permeable ANXA2 inhibitor. 5α-Epoxyalantolactone binds to ANXA2, blocks the formation of ANXA2-S100A10 heterotetramers, inhibits the membrane trafficking of E-cadherin, and prevents metastasis of breast cancer cells as well as proliferation of breast cancer stem cells. 5α-Epoxyalantolactone improves cognitive and memory impairments by inhibiting the iNOS/COX-2/NF-κB pathway and reducing the activity of cerebral AChE. 5α-Epoxyalantolactone can be used in studies related to Alzheimer's disease and triple-negative breast cancer.

D-glycero-D-galacto-heptose is a seven-carbon sugar that exerts immunomodulatory effects. It is the structural monosaccharide unit of the Eubacterium saburreum T18 antigen, enhances immune cell activation, and acts as a COX-2 ligand to participate in anti-inflammatory pathways. D-glycero-D-galacto-heptose can be used in research on triple-negative breast cancer.

Clematomandshurica saponins B shows significant inhibitory activity on cyclooxygenase-2 (IC₅₀=2.58 mM).