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-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.

COX-2/LOX-IN-1 (compound 5) is a dual inhibitor of COX-2 and LOX enzymes, exhibiting IC50 values of 0.55 μM for COX-2 and 30 μM for LOX.

COX-2/LOX-IN-2 (compound 6) is a dual inhibitor of COX-2/LOX, with IC50 values of 7.0 μM and 27.5 μM, respectively. It exhibits antioxidant properties and shows promise for development as a non-steroidal anti-inflammatory drug (tNSAID).

COX-2-IN-41 (compound 5e) is a selective COX-2 inhibitor with an IC50 value of 1.74 μM. It demonstrates selectivity over COX-1, with a selectivity ratio of IC50(COX-1)/IC50(COX-2) = 16.32.

COX-2-IN-42 (Compound T1) is a COX-2 inhibitor that protects zebrafish from neuronal damage induced by PTZ.

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

COX-2-IN-54 (Compound 7y) is an orally active COX-2 inhibitor with an IC50 of 4.15 μM. It provides significant protection against DSS-induced ulcerative colitis, effectively reducing tissue damage. Additionally, COX-2-IN-54 exhibits anti-inflammatory properties.

COX-2-IN-55 (compound 1) is an orally active Celecoxib analogue with broad-spectrum anticancer properties and relatively weak COX-2 inhibition. It specifically inhibits SERCA2, leading to increased caspase-3 cleavage and DR5 levels, which activates GRP78 and suppresses the progression of triple-negative breast cancer (TNBC). Additionally, COX-2-IN-55 downregulates the angiogenesis markers VEGF-α and IL-8, thereby inhibiting microvessel formation.

COX-2-IN-56 (example 6) is a selective COX-2 inhibitor that shows no significant inhibitory effect on COX-1. It can be utilized in research on COX-2-dependent conditions such as inflammation.

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].