cox 2 in 1

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

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.

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/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.

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/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-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-2/5-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-1/2-IN-2 is a potent inhibitor of both COX-1 and COX-2, with IC50 values of 9.7 ± 0.09 μM for COX-1 and 4.6 ± 1.45 μM for COX-2, respectively [1].

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.

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-2/15-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/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-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-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-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-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-1/2-IN-9 (Compound 3n) serves as a selective and potent inhibitor of both COX-1 and COX-2, demonstrating IC 50 values of 0.031 µM for COX-1 and 0.01 µM for COX-2. This compound exhibits antibacterial and anti-inflammatory properties, effectively targeting MRSA 1478 (MIC=50 μg/mL) and multidrug-resistant S. lentus (MIC=50 μg/mL). Furthermore, COX-1/2-IN-9 shows promise in relieving MRSA-induced pneumonia in conditions of compromised immunity.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

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.

Eltenac (B78820) is a non-steroidal anti-inflammatory, COX inhibitor with analgesic activity.Eltenac inhibits COX-1 and COX-2 and is used in the study of Acute Respiratory Distress Syndrome (ARDS).

Valdecoxib (SC 65872) is a prescription drug used in the treatment of osteoarthritis, rheumatoid arthritis, and painful menstruation and menstrual symptoms. It is classified as a nonsteroidal anti-inflammatory drug, or NSAID, and should not be taken by anyone allergic to these types of medications.