15-lo

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.

9c(i472) is an inhibitor of 15-lipoxygenase-1 (15-LO-1; IC50 = 0.19 μM).1 It decreases LPS- and IFN-γ-induced NF- B activity in RAW-Blue cells when used at concentrations of 0.2, 1, and 5 μM. 9c(i472) reduces LPS- and IFN-γ-induced increases in Nos2 expression and lipid peroxidation in RAW 264.7 cells when used at a concentration of 5 μM.

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.

Compound 105 (h15-LOX-2 inhibitor 1) is a potent inhibitor of human epithelial 15-lipoxygenase-2 (h15-LOX-2), exhibiting an IC50 of 0.34 μM [1].

COX-2 15-LOX-IN-2 is a potent inhibitor of COX-2 (IC50: 0.065 μM) and 15-LOX (IC50: 1.86 μM), also demonstrating significant antioxidant activity [1].

COX-2 15-LOX-IN-3 (compound 5k) is a dual inhibitor of COX-2 and 15-LOX with inhibitory concentrations (IC50) of 0.075 μM and 1.97 μM, respectively. This compound effectively suppresses LPS-induced production of pro-inflammatory cytokines (IL-6, ROS, and NO), exhibiting targeted anti-inflammatory effects [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 15-LOX-IN-5 (Compound 4f) functions as a dual inhibitor of COX-2 and 15-LOX, demonstrating both anti-inflammatory and antioxidant properties [1]. This compound effectively reduces NF-κB activation in RAW 264.7 macrophages that is induced by lipopolysaccharide.

Compound 10 (h15-LOX-2 inhibitor 2) suppresses h15-LOX activity, exhibiting IC 50 and K i values of 26.9 μM and 16.4 μM, respectively.

Compound 13, identified as h15-LOX-2 inhibitor 3, exhibits inhibitory activity against h15-LOX, with IC50 and Ki values of 25 μM and 15.1 μM, respectively.

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6 22 90 15 20 20 57 58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.

5-Fluorouracil (5-FU) is a uracil analog and inhibitor of DNA synthesis, exhibiting antitumor activity by affecting pyrimidine synthesis through thymidylate synthase inhibition; it induces apoptosis and autophagy.

Mdivi-1 (Mitochondrial division inhibitor 1) is a mitochondrial division inhibitor that inhibits DRP1 and Dynamin I (IC50=1-10 μM). Mdivi-1 inhibits mitochondrial autophagy.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) is a second messenger in cellular innate immunity, catalyzed by cGAMP synthase (cGAS) under DNA binding conditions. It binds to STING to form a dimer, inducing the production and expression of interferon-β and other cytokines.

Fludarabine (Fludarabinum) is a fluorinated purine analog, an inhibitor of nucleic acid synthesis and an inhibitor of STAT1 activation. Fludarabine has antitumor activity and can be used for the treatment of leukemia and lymphoma.

Capsaicin ((E)-Capsaicin) is a natural product extracted from Capsicum annuum, and is a TRPV1 agonist (EC50=0.29 μM). Capsaicin has antitumor, anti-inflammatory, antioxidant and neuroprotective activities.

Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist and IL receptor modulator with anti-inflammatory and immunosuppressive properties that induces autophagy and inhibits LPS-induced inflammatory responses in macrophages.

Imatinib Mesylate (STI-571) is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively).

Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

Defactinib (VS-6063) is a second-generation inhibitor of FAK that inhibits FAK phosphorylation at the Tyr397 site. Defactinib has potential antitumor activity.

RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.

Citronellol ((±)-β-Citronellol) is used in insect repellents and perfumes and as a mite attractant.