cox-2-in-2 — TargetMol Chemicals (2024)

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Results for "cox-2-in-2" in TargetMol Product Catalog

T10032134729-13-8In house

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-34 is a selective, orally potent COX-2 inhibitor that shows anti-inflammatory activity without gastric ulcer toxicity during experiments in mice.

T10033787623-48-7In house

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

T620612756347-91-6In house

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-31 (compound 7b) is an orally active dual inhibitor targeting COX-2 (IC50=60 nM) and 5-LOX (IC50=1.9 μM). Additionally, it inhibits the activity of transmembrane hCA IX (Ki=48.9 nM) and hCA XII (Ki=5.8 nM). This compound demonstrates anti-inflammatory and analgesic activity [1].

COX-2-IN-32 (Compound 2f) is a dual inhibitor of iNOS and COX-2, known to downregulate NF-κB expression. Demonstrating anti-inflammatory properties, it impedes NO production in LPS-induced RAW264.7 macrophages with an IC50 value of 11.2 μM [1].

COX-1/2-IN-4 (compound 2b) is a dual COX-1 and COX-2 inhibitor with respective IC50 values of 0.239 μM for COX-1 and 0.191 μM for COX-2. Additionally, it demonstrates moderate anticancer activity, exhibiting IC50 values of 30.79 μM against COLO205 cancer cell lines and 74.15 μM against B16F1 cancer cell lines [1].

COX-2-IN-18 (Compound 3) is a highly effective COX-2 inhibitor with strong inhibitory activity against COX-2 (IC 50 = 0.775 μM). Its potency is comparable to the reference drug Celecoxib (IC 50 = 0.153 μM). This compound, COX-2-IN-18, shows promise in the field of cancer research [1].

COX-2/NO-IN-1 is an orally active nitric oxide synthase (iNOS) and NO ( IC 50 of 3.52 μM) inhibitor as well as suppresses the expression of COX-2. COX-2/NO-IN-1 has anti-inflammatory effects and reduces pathological damage to kidney tissues[1].

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

COX-2-IN-7 (compound 4a) is a potent, selective, and orally active COX-2 inhibitor which is higher selectivity than Celecoxib with an IC 50 value of 6.585 uM. COX-2-IN-7 has good anti-inflammatory and low ulcerogenic activity in vivo[1].

COX-2-IN-35 (compound 7) is a selective inhibitor of COX-2, demonstrating anti-inflammatory activity, with an inhibitory concentration (IC 50) of 4.37 nM [1].

COX-2-IN-8 (Compound 6a) is a potent, selective, orally active COX-2 inhibitor (IC50: 6.585 μM) with a higher COX-2 selectivity than Celecoxib.

COX-2-IN-16 (compound 2b) is a potent, selective, and orally active inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 102 μM. It effectively reduces nitric oxide (NO) production and demonstrates anti-inflammatory activity [1].

COX-2/15-LOX-IN-1 (Compound 14) is a COX-2 and 15-lipoxygenase (15-LOX) inhibitor that acts on COX-1 (IC50: 10.65 μM), COX-2 (IC50: 0.075 μM) and 15-LOX (IC50: 2.98 μM). 25 has an anti-inflammatory effect.

COX-2-IN-13 (compound 13e) is a highly potent and selective inhibitor of COX-2, demonstrating a remarkable IC50 value of 0.98 μM. It exhibits strong anti-inflammatory activity and has shown favorable results in vivo acute toxicity studies [1].

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-19 (Compound 24) is a highly potent inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 1.76 μM. Notably, COX-2-IN-19 exhibits robust in vivo anti-inflammatory activity [1].

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-10 is a potent inhibitor of COX-2. COX-2-IN-10 exhibits inhibitory effects on the production of IL-6, TNF-α and IL-1β. COX-2-IN-10 inhibits PGE2 production in a concentration-dependent manner with an IC50 value of 2.54 μM. COX-2-IN-10 inhibits the expression of iNOS and COX-2 at the mRNA and protein levels. COX-2-IN-10 inhibited the expression of iNOS and COX-2 at the mRNA and protein levels.

COX-2/PI3K-IN-2 (compound 5f) has properties of anti-inflammatory and anti-cancer. COX-2/PI3K-IN-2 is a selective inhibitor of COX-2 (Ki = 3.02 nM) as well as a potent inhibitor of PI3K (IC 50 = 2.78 nM) [1].

COX-2/15-LOX-IN-4 (compound 5i) is a dual inhibitor with IC50 values of 0.075 μM for COX-2 and 1.97 μM for 15-LOX. It inhibits LPS-induced production of pro-inflammatory cytokines (IL-6, ROS) and exhibits targeted anti-inflammatory effects [1].

COX-2-IN-28 is a potent and selective COX-2 inhibitor capable of acting on COX-2 (IC50: 0.054 μM), 15-LOX (IC50: 2.14 μM) and COX-1 (IC50: 13.21 μM).

COX-2-IN-14 (compound 2a) is a highly potent and selective inhibitor of COX-2 (cyclooxygenase-2), with strong binding affinity at the active site of 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].

Topo I/COX-2-IN-2 (Compound W10) is a potent dual Topo I (IC50: 0.90 μM) and COX-2 (IC50: 2.31 μM) inhibitor.Topo I/COX-2-IN-2 induces apoptosis in cancer cells using the mitochondrial pathway.

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

COX-2-IN-20 (Compound 5d) is a selective and orally active inhibitor of COX-2 (IC 50 = 17.9 nM) with anti-inflammatory activity [1].

COX-2/5-LOX-IN-3 (compound 5b) is a powerful and 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. This compound, COX-2/5-LOX-IN-3, shows promise for the investigation of inflammatory diseases [1].

COX-2-IN-12 (compound 3b) is a potent and selective COX-2 inhibitor with an IC 50 of 19.98 μM. COX-2-IN-12 is an anti-inflammatory agent that shows safety in-vivo acute toxicity studies [1].

COX-2-IN-30, a benzenesulfonamide derivative, is an orally active, dual inhibitor of cyclooxygenase-2 (COX-2; IC50 = 49 nM) and cyclooxygenase-1 (COX-1; IC50 = 10.4 μM), as well as 5-lipoxygenase (5-LOX; IC50 = 2.4 μM). Additionally, it inhibits the transmembrane isoforms of human carbonic anhydrase IX and XII with nanomolar class Ki values. Demonstrating analgesic and anti-inflammatory properties, COX-2-IN-30 is devoid of acute gastric effects, avoiding ulcerogenic activity [1].

COX-2/15-LOX-IN-2 is a potent inhibitor of both COX-2 and 15-LOX, demonstrating IC50 values of 0.065 μM for COX-2 and 1.86 μM for 15-LOX. Additionally, it exhibits significant antioxidant activity [1].

COX-2/5-LOX-IN-1 (compound 3a), a benzothiophen-2-yl pyrazole carboxylic acid derivative, is a potent and dual inhibitor of COX-2 / 5-LOX. It exhibits superior analgesic and anti-inflammatory properties compared to Celecoxib and Indomethacin. COX-2/5-LOX-IN-1 displays 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-26 is a potent, orally active, selective COX-2 inhibitor that acts 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 has a gastrointestinal safety profile.

COX-2/PI3K-IN-1 (compound 5d) is a potent inhibitor of PI3K (IC50: 1.14 nM). COX-2/PI3K-IN-1 is a selective inhibitor of COX-2 (Ki: 3.24 nM).

COX-2-IN-9 is a selective, potent, orally active COX-2 inhibitor (IC50: 10.17 μM).COX-2-IN-9 has a higher COX-2 selectivity than Celecoxib.COX-2-IN-9 exhibits good in vivo anti-inflammatory activity and low ulcerogenic effect.

COX-2-IN-33 (compound 5f) is a selective COX-2 inhibitor with an IC50 value of 45.5 nM and exhibits potential as an anti-inflammatory agent. It effectively suppresses pro-inflammatory cytokine production in vivo while maintaining gastric safety [1].

COX-2/15-LOX-IN-3 (compound 5k) serves as a dual inhibitor for COX-2 and 15-LOX, demonstrating inhibitory concentrations (IC50) of 0.075 μM and 1.97 μM, respectively. This compound effectively suppresses LPS-induced cellular production of pro-inflammatory cytokines (IL-6, ROS, and NO), exhibiting targeted anti-inflammatory effects [1].

COX-1/2-IN-5 (compound 2a) functions as a dual inhibitor of COX1/2, demonstrating inhibitory concentrations (IC50) of 2.650 μM and 0.958 μM, respectively, and exhibits anticancer activity by inhibiting liver cancer HepG2 cells with an IC50 of 60.75 μM [1].

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

COX-2-IN-17 is a potent, blood-brain barrier permeable COX-2 (cyclooxygenase-2) inhibitor (IC50: 0.02 μM) with anti-inflammatory and analgesic activity.

COX-2/5-LOX-IN-2 is a benzothiophen-2-ylpyrazole carboxylic acid derivative. COX-2/5-LOX-IN-2 (5b) inhibited both COX-2 and 5-LOX. The IC50s of COX-2/5-LOX-IN-2 inhibiting COX-1, COX-2 and 5-LOX were 5.40, 0.01 and 1.78 μM, respectively. COX-2/5-LOX-IN-2 showed more analgesic and anti-inflammatory activities than Celecoxib and Indomethacin.

COX-2-IN-21 (Compound 5c) is an orally active, selective COX-2 inhibitor (IC50: 0.039 μM). COX-2-IN-21 has good anti-inflammatory potential.

Topo I/COX-2-IN-1 (1H-30) is a potent Topo I/COX-2 inhibitor with the IC50 of 0.24 μM and 4.42 μM for COX-2 and Topo I, respectively. Topo I/COX-2-IN-1 induces apoptosis and inhibits migration of cancer cells, shows anti-cancer activity.

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

COX-1/2-IN-3 (Compound 7a) is a dual inhibitor of COX-1 and COX-2. COX-1/2-IN-3 has 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].

Diclofenac Potassium (CGP-45840B) is a nonsteroidal anti-inflammatory drug taken to reduce inflammation and as an analgesic reducing pain in certain conditions.

Guaiacol (2-Methoxyphenol) is a precursor to various flavorants, such as eugenol and vanillin. Its derivatives are used medicinally as an expectorant, antiseptic, and local anesthetic. It also can be used as an indicator in chemical reactions that produce oxygen. When oxygen binds to it, the complex turns yellowish brown and absorbs light maximally at about 470 nm.

Ketorolac (Acuvail) is a non-steroidal anti-inflammatory drug (NSAID) in the family of heterocyclic acetic acid derivatives. It acts by inhibiting the bodily synthesis of prostaglandins.