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.

EGFR/COX-2-IN-2 (Compound 10a) is a dual inhibitor targeting the epidermal growth factor receptor (EGFR) with an IC50 of 6.0 μM and cyclooxygenase-2 (COX-2) with an IC50 of 50 μM. It induces cell cycle arrest in the S phase and triggers apoptosis. EGFR/COX-2-IN-2 holds potential for research in cancer and inflammation-related diseases.

COX-2-IN-20 (Compound 5d) is a selective and orally active COX-2 inhibitor (IC50 = 17.9 nM) with anti-inflammatory activity [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-IN-21 (Compound 5c) is an orally active, selective COX-2 inhibitor with an IC50 of 0.039 μM, demonstrating significant anti-inflammatory potential.

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-IN-29 is a selective inhibitor of orally active COX-2 (IC50: 0.005 μM).

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

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-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-IN-53 (compound 9) is a potent COX-2 inhibitor with an IC50 value of 0.373 μM. It is effective in reducing oxidative stress caused by radiation.

COX-2-IN-37 (compound 11) is a potent and selective COX-2 inhibitor with significant antioxidant properties, exhibiting an IC50 value of 33.0 μg/mL.

COX-2/NLRP3-IN-1 (Compound 6k) is an inhibitor that targets COX-2 and NLRP3, exhibiting an IC50 value of 1.53 μM for COX-2. This compound exerts anti-inflammatory effects by inhibiting the NF-κB/NLRP3 signaling pathway.