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-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-47 (compound 6c) is a selective inhibitor of COX-2, exhibiting an IC50 of 0.03 μM. This compound also displays antiedema activity.

COX-1-IN-2 (compound 5h) serves as a potent anti-inflammatory and analgesic agent. This compound demonstrates a significant inhibitory effect on COX-1, with an IC 50 value of 38.76 nM.

COX-2-IN-49 (compound 6c) is a potent inhibitor of cyclooxygenase-2 (COX-2), displaying an IC50 value of 2.671 µM. This compound exhibits anti-proliferative properties and holds potential for use in cancer research.

COX-2-IN-48 (5-25) serves as an inhibitor of COX-2, exhibiting an IC50 of 51.7 nM against human COX-2. It displays anti-inflammatory and analgesic effects in various rodent models through inhibition of the NF-κB pathway. COX-2-IN-48 (5-25) inhibits the degradation of IκB, phosphorylation and nuclear translocation of NF-κB p65, and the expression of COX-2 and iNOS.

COX-2 15-LOX-IN-6 (Compound 5l) is a dual inhibitor of COX-2 and 15-LOX with IC50 values of 0.201 μM and 11.723 μM, respectively. In serum, it suppresses the expression of PGE, TNF-α, IL-6, and iNOS, and demonstrates anti-inflammatory activity in a carrageenan-induced rat edema model.

COX-2-IN-51 (E25) is a potent COX-2 inhibitor with an IC50 of 70.7 nM. It significantly suppresses LPS-induced release of NO and PGE2, the expression of COX-2 and iNOS, and the activation of the NF-κB pathway. Displaying anti-inflammatory and analgesic effects in various mouse models through NF-κB pathway inhibition, COX-2-IN-51 has lower gastrointestinal side effects compared to Indomethacin.

COX-2-IN-52 (Compound 5l) is an orally active and selective COX-2 inhibitor with an IC50 of 54 nM. It can suppress the release of NO in cells, exhibiting anti-inflammatory properties. COX-2-IN-52 offers high gastrointestinal safety and is suitable for research on oral anti-inflammatory drugs.

EGFR COX-2-IN-1 is an EGFR COX-2 inhibitor that effectively targets EGFRWT, EGFRT790M, COX-1, and COX-2 with IC50 values of 0.12, 0.076, 20.1, and 1.52 μM, respectively. It inhibits MCF-7, HT-29, and A-549 cells with IC50 values of 1.20, 5.14, and 14.81 μM, respectively. The compound induces apoptosis by upregulating Bax protein and downregulating Bcl-2 protein levels. Additionally, EGFR COX-2-IN-1 significantly increases the proportion of cells in the G2 M phase in MCF-7 cells, demonstrating a broad-spectrum antitumor effect.

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

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-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-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].

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-1 2-IN-3 (Compound 7a) is a dual inhibitor of COX-1 and COX-2, exhibiting anti-inflammatory activity with low toxicity [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-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 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 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-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-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].