cox-2-in-2

COX-2-IN-2, a selective inducible COX2 inhibitor, exhibits potent inhibition with an IC50 of 0.24 μM. Meanwhile, COX-2-IN-1 functions as an anti-inflammatory agent, demonstrating both anti-inflammatory and analgesic activities.

COX-2-IN-34 is a selective, orally potent COX-2 inhibitor that shows anti-inflammatory activity without gastric ulcer toxicity during experiments in mice.

COX-2-IN-1 is a potent and selective COX-2 inhibitor (IC50: 3.9 μM).

COX-2-IN-6 is a potent, selective, and orally available cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.84 μM and a Ki of 69 nM.COX-2-IN-6 inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM.COX-2-IN-6 is used to prevent colorectal cancer. COX-2-IN-6 can be used to prevent colorectal cancer.

COX-2-IN-31 (compound 7b) is an orally active dual inhibitor targeting COX-2 (IC50=60 nM) and 5-LOX (IC50=1.9 μM), and also inhibits transmembrane hCA IX (Ki=48.9 nM) and hCA XII (Ki=5.8 nM), demonstrating anti-inflammatory and analgesic activity [1].

COX-1 2-IN-4 (compound 2b) is a dual COX-1 and COX-2 inhibitor with IC50 values of 0.239 μM for COX-1 and 0.191 μM for COX-2, and demonstrates moderate anticancer activity with IC50 values of 30.79 μM against COLO205 cancer cell lines and 74.15 μM against B16F1 cancer cell lines [1].

COX-2-IN-7 (compound 4a) is a potent and selective COX-2 inhibitor with greater selectivity than Celecoxib and an IC50 value of 6.585 µM. It exhibits good anti-inflammatory properties and low ulcerogenic activity in vivo[1].

COX-2 NO-IN-1 is an orally active nitric oxide synthase (iNOS) and NO (IC50 of 3.52 μM) inhibitor that also suppresses COX-2 expression, exhibiting anti-inflammatory effects and reducing pathological damage to kidney tissues [1].

COX-2-IN-32 (Compound 2f) is a dual inhibitor of iNOS and COX-2 that downregulates NF-κB expression and demonstrates anti-inflammatory properties by impeding NO production in LPS-induced RAW264.7 macrophages with an IC50 value of 11.2 μM [1].

COX-2-IN-18 (Compound 3) is a highly effective COX-2 inhibitor with an IC50 value of 0.775 μM, demonstrating strong inhibitory activity against COX-2. Its potency is comparable to the reference drug Celecoxib (IC50 = 0.153 μM), showing promise in the field of cancer research [1].

COX-2-IN-11 (compound 7b2) is a potent and selective COX-2 inhibitor with potential applications in inflammation disease research[1].

COX-2-IN-43 (Compound MYM4) functions as a selective COX-2 inhibitor, exhibiting IC50 values of 0.983 μM for COX-1 and 0.247 μM for COX-2. It effectively inhibits cancer cell proliferation and colonization and also induces apoptosis [1].

COX-2-IN-39 (compound 44) potently inhibits COX-2, exhibiting an IC50 of 0.4 nM [1].

COX-2 15-LOX-IN-5 (Compound 4f) functions as a dual inhibitor of COX-2 and 15-LOX, demonstrating both anti-inflammatory and antioxidant properties [1]. This compound effectively reduces NF-κB activation in RAW 264.7 macrophages that is induced by lipopolysaccharide.

COX-2-IN-35 (compound 7) is a selective COX-2 inhibitor with anti-inflammatory activity, exhibiting an inhibitory concentration (IC 50) of 4.37 nM [1].

COX-2-IN-19 (Compound 24) is a highly potent cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1.76 μM, exhibiting significant in vivo anti-inflammatory activity [1].

COX-2-IN-13 (compound 13e) is a highly potent and selective COX-2 inhibitor with an impressive IC50 value of 0.98 μM. It exhibits strong anti-inflammatory activity and has shown favorable results in in vivo acute toxicity studies [1].

COX-2-IN-23 is a selective inhibitor of COX-2, with IC50 values of 0.28 and 20.14 μM for COX-2 and COX-1, respectively.COX-2-IN-23 exhibits anti-inflammatory effects as well as low ulcerogenic effects.

COX-2-IN-22 is a COX-2 inhibitor (IC50: 8.6 μM) that can cross the blood-brain barrier and also exhibits inhibitory effects on AChE (IC50: 2.8 μM), BChE (IC50: 6.3 μM), β-Secretase (IC50: 15.3 μM), LOX-5 (IC50: 13.9 μM) and DPPH ( IC50: 6.8 μM) showed inhibitory effects.

COX-2 15-LOX-IN-1 (Compound 14) is a dual inhibitor of COX-2 and 15-lipoxygenase (15-LOX) with IC50 values of 10.65 μM for COX-1, 0.075 μM for COX-2, and 2.98 μM for 15-LOX, exhibiting an anti-inflammatory effect.

COX-2-IN-16 (compound 2b) is a potent, selective, and orally active inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 102 μM, effectively reducing nitric oxide (NO) production and demonstrating anti-inflammatory activity [1].

COX-2-IN-8 (Compound 6a) is a potent, selective, orally active COX-2 inhibitor (IC50: 6.585 μM) with a higher COX-2 selectivity than Celecoxib.

COX-2 15-LOX-IN-4 (compound 5i) is a dual inhibitor with IC50 values of 0.075 μM for COX-2 and 1.97 μM for 15-LOX. It inhibits LPS-induced production of pro-inflammatory cytokines (IL-6, ROS) and exhibits targeted anti-inflammatory effects [1].

COX-2-IN-10 is a potent COX-2 inhibitor that exhibits inhibitory effects on the production of IL-6, TNF-α, and IL-1β, and inhibits PGE2 production in a concentration-dependent manner with an IC50 value of 2.54 μM. Additionally, COX-2-IN-10 inhibits the expression of iNOS and COX-2 at both mRNA and protein levels.

COX-2-IN-14 (compound 2a) is a highly potent and selective inhibitor of COX-2 (cyclooxygenase-2), binding strongly at the active site of the COX-2 co-crystal. Demonstrating remarkable in vivo anti-inflammatory activity, COX-2-IN-14 effectively reduces ear edema and myeloperoxidase (MPO) activity in mice [1].

COX-2-IN-28 is a potent and selective COX-2 inhibitor, with IC50 values of 0.054 μM for COX-2, 2.14 μM for 15-LOX, and 13.21 μM for COX-1.

COX-2/sEH-IN-1 is an orally active dual inhibitor of COX-2 (IC50: 1.24 μM) and sEH (IC50: 0.40 μM), a soluble epoxide hydrolase. COX-2/sEH-IN-1 increases anti-inflammatory effects and significantly reduces cardiovascular risk.

COX-2-IN-24 is an orally active COX-2 inhibitor [IC50: 0.17 μM] with anti-inflammatory and hypo-ulcerogenic effects.

COX-2-IN-20 (Compound 5d) is a selective and orally active COX-2 inhibitor (IC50 = 17.9 nM) with anti-inflammatory activity [1].

COX-2 PI3K-IN-2 (compound 5f) possesses anti-inflammatory and anti-cancer properties, functioning as a selective inhibitor of COX-2 (Ki = 3.02 nM) and a potent inhibitor of PI3K (IC50 = 2.78 nM) [1].

Topo I COX-2-IN-2 (Compound W10) is a potent dual inhibitor of Topo I (IC50: 0.90 μM) and COX-2 (IC50: 2.31 μM), inducing apoptosis in cancer cells via the mitochondrial pathway.

COX-2 5-LOX-IN-3 (compound 5b) is a powerful dual inhibitor of COX-2 and 5-LOX, with IC50 values of 45.73 μM, 5.45 μM, and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively, showing promise for the investigation of inflammatory diseases [1].

COX-2-IN-12 (compound 3b) is a potent and selective COX-2 inhibitor with an IC50 of 19.98 μM, demonstrating anti-inflammatory properties and safety in in-vivo acute toxicity studies [1].

COX-1 2-IN-6 (compound 4 h) acts as a dual inhibitor of COX-1 and COX-2, exhibiting potent inhibitory activity with IC50 values of 68 nM and 91 nM, respectively. It is utilized in the research of inflammatory diseases [1].

COX-2-IN-40 (compound 17), a COX-2 inhibitor, exhibits an IC 50 value of 14.86 μM and is utilized in the study of chronic pain [1].

COX-1 2-IN-8 (compound 11f) is an orally active inhibitor of both COX-1 and COX-2, with IC50 values of 2.14 µM and 0.58 µM, respectively. Its anti-inflammatory activity surpasses that of celecoxib.

COX-2 15-LOX-IN-2 is a potent inhibitor of COX-2 (IC50: 0.065 μM) and 15-LOX (IC50: 1.86 μM), also demonstrating significant antioxidant activity [1].

COX-2-IN-9 is a selective, potent, orally active COX-2 inhibitor (IC50: 10.17 μM).COX-2-IN-9 has a higher COX-2 selectivity than Celecoxib.COX-2-IN-9 exhibits good in vivo anti-inflammatory activity and low ulcerogenic effect.

COX-2-IN-30, a benzenesulfonamide derivative, is an orally active, dual inhibitor of cyclooxygenase-2 (COX-2; IC50 = 49 nM) and cyclooxygenase-1 (COX-1; IC50 = 10.4 μM), as well as 5-lipoxygenase (5-LOX; IC50 = 2.4 μM). Additionally, it inhibits the transmembrane isoforms of human carbonic anhydrase IX and XII with nanomolar class Ki values. Demonstrating analgesic and anti-inflammatory properties, COX-2-IN-30 is devoid of acute gastric effects, avoiding ulcerogenic activity [1].

COX-2 5-LOX-IN-1 (compound 3a), a benzothiophen-2-yl pyrazole carboxylic acid derivative, is a potent dual inhibitor of COX-2 and 5-LOX, exhibiting superior analgesic and anti-inflammatory properties compared to Celecoxib and Indomethacin. It demonstrates strong inhibitory activity against COX-1, COX-2, and 5-LOX, with IC50 values of 12.13 μM, 0.4 μM, and 4.96 μM, respectively [1].

COX-2 PI3K-IN-1 (compound 5d) is a potent inhibitor of PI3K with an IC50 of 1.14 nM and selectively inhibits COX-2 with a Ki of 3.24 nM.

COX-2-IN-26 is a potent, orally active, selective COX-2 inhibitor, acting on COX-1 (IC50: 10.61 μM), COX-2 (IC50: 0.067 μM), and 15-LOX (IC50: 1.96 μM). COX-2-IN-26 is anti-inflammatory and possesses a gastrointestinal safety profile.

COX-2-IN-33 (compound 5f) is a selective COX-2 inhibitor with an IC50 of 45.5 nM, demonstrating potential as an anti-inflammatory agent by effectively suppressing pro-inflammatory cytokine production in vivo while maintaining gastric safety [1].

COX-2 15-LOX-IN-3 (compound 5k) is a dual inhibitor of COX-2 and 15-LOX with inhibitory concentrations (IC50) of 0.075 μM and 1.97 μM, respectively. This compound effectively suppresses LPS-induced production of pro-inflammatory cytokines (IL-6, ROS, and NO), exhibiting targeted anti-inflammatory effects [1].

COX-1 2-IN-5 (compound 2a) is a dual inhibitor of COX1 2, demonstrating inhibitory concentrations (IC50) of 2.650 μM and 0.958 μM, respectively, and exhibits anticancer activity against liver cancer HepG2 cells with an IC50 of 60.75 μM [1].

COX-1/2-IN-2, a potent inhibitor of both COX-1 and COX-2, demonstrates significant inhibitory activity, with IC50 values of 13.9 ± 3.21 μM for COX-1 and 6.4 ± 0.74 μM for COX-2, respectively [1].

COX-2-IN-21 (Compound 5c) is an orally active, selective COX-2 inhibitor with an IC50 of 0.039 μM, demonstrating significant anti-inflammatory potential.

Topo I COX-2-IN-1 (1H-30) is a potent Topo I COX-2 inhibitor with IC50 values of 0.24 μM for COX-2 and 4.42 μM for Topo I. It induces apoptosis and inhibits cancer cell migration, demonstrating anti-cancer activity.