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.

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

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.

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

RO5263397 is a TAAR1 specific agonist with oral activity that has been used in antidepressant studies. It has also been found to act as an inhibitor of the enzyme cyclooxygenase-2 (COX-2), which is involved in the synthesis of prostaglandins.

SC58451 is a novel potent, orally active and selective COX-2 inhibitor.SC58451 showed anti-inflammatory activity in a rat model of arthritis.

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).

Floctafenine (R-4318) is an orally available nonsteroidal anti-inflammatory compound that is a COX-I and COX-2 inhibitor and interferes with the antiplatelet effects of aspirin.Floctafenine has analgesic activity and is used in the study of pain.

LM-1685 is a potent and selective inhibitor of COX-2 IN human monocytes and whole blood with IC50 of 0.65µM and IC50 = 4.3μM, respectively, and is a potential compound for the treatment of inflammation.

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.

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.

Indomethacin is an orally active nonsteroidal anti-inflammatory drug (NSAID) that non-selectively inhibits cyclooxygenase enzymes COX-1 and COX-2, with IC₅₀ values of 18 nM and 26 nM, respectively. It exhibits good blood-brain barrier permeability and shows significant anti-inflammatory, anti-tumor, and anti-infective activities. Indomethacin is widely used in research related to cancer, inflammation, and viral infections, and is also commonly used to induce gastric ulcer models in animals.

Sulindac (Sulindac sulfoxide) is a sulfinylindene derivative prodrug with potential antineoplastic activity. Converted in vivo to an active metabolite, sulindac, a nonsteroidal anti-inflammatory drug (NSAID), blocks cyclic guanosine monophosphate-phosphodiesterase (cGMP-PDE), an enzyme that inhibits the normal apoptosis signal pathway; this inhibition permits the apoptotic signal pathway to proceed unopposed, resulting in apoptotic cell death.

Loxoprofen (Koloxo) is an anti-inflammatory non-steroidal medicine.

Triflusal (UR1501) is a 2-acetoxy-4-trifluoromethylbenzoic acid and it is an aspirin chemically-related molecule but not a derivative.