COX-2 Inhibitor

2'-Hydroxy-4-methoxychalcone is a PPARγ agonist. 2'-Hydroxy-4-methoxychalcone also exhibits inhibitory activity against gelatinase/collagenase and human glutathione S-transferase (GST), with an IC₅₀ of 5.2 μM and a K_i of 15.36 μM against GST. 2'-Hydroxy-4-methoxychalcone inhibits both the NF-κB and AP-1 signaling pathways, exerting anti-inflammatory activity; it also inhibits COX-2, conferring anti-cancer/anti-angiogenic activity. 2'-Hydroxy-4-methoxychalcone can be used in studies related to atherosclerosis, inflammatory diseases and cancer.

AChE-IN-82 (compound 49) is an acetylcholinesterase (AChE) inhibitor. AChE-IN-82 inhibits eeAChE, eqBChE, hMAO-A, hMAO-B, and BACE-1 with IC₅₀s of 0.072, 9.81, 14.52, 0.024, 2.42 μM, respectively. AChE-IN-82 inhibits COX-1, COX-2 and 5-LOX with IC₅₀s of 60.41, 0.187, 0.18 μM, respectively. AChE-IN-82 shows an excellent neuroprotective effect by significantly reducing oxidative stress induced by H₂ O₂.

Akt/NF-κB/MAPK-IN-1 (compound 2m) is a potent and orally active inhibitor against NO (IC₅₀=7.70 μM) with no significant toxicity. Akt/NF-κB/MAPK-IN-1 shows anti-inflammatory activity by inhibiting Akt/NF-κB and MAPK signaling pathways.

DPAP is a p-ERK1/2 inhibitor with an IC₅₀ of 7.85 μM against p-ERK1/2. DPAP inhibits the expression of p-MEK1/2 and disrupts the Ras-ERK signaling pathway. DPAP inhibits the expression of COX-2 in nerve cells. DPAP damages DNA and mitochondria, induces Apoptosis via the mitochondrial pathway, and upregulates PD-L1. DPAP inhibits melanoma metastasis and angiogenesis, and inactivates spinal microglia and astrocytes. DPAP exhibits anti-melanoma activity and can be combined with anti-PD-1 monoclonal antibodies to modify anti-tumor effects. DPAP is applicable for the research of melanoma.

N1-Acetyl-5-methoxykynuramine hydrochloride (AMK hydrochloride) is an active metabolite of Melatonin (HY-B0075) with antioxidant activity and blood-brain barrier permeability. N1-Acetyl-5-methoxykynuramine hydrochloride inhibits LPS-induced activation of inducible nitric oxide synthase and COX-2, scavenges ROS, hydroxyl radicals, carbonate radicals and ABTS cation radicals, and protects bovine serum albumin from peroxyl radical-mediated damage. N1-Acetyl-5-methoxykynuramine hydrochloride reduces the increase in cytoplasmic and mitochondrial lipid peroxidation in the substantia nigra and striatum in MPTP (HY-15608)-induced mouse models of Parkinson's disease. N1-Acetyl-5-methoxykynuramine hydrochloride can be used in studies related to Parkinson's disease, metabolism-related diseases and oxidative stress.

(±)-Methotrexate-¹³C,d₃ disodium ((±)-Amethopterin-¹³C,d₃ disodium; (±)-CL14377-¹³C,d₃ disodium; (±)-WR19039-¹³C,d₃ disodium) is the deuterated, ¹³C-labeled (±)-Methotrexate (HY-121151). (±)-Methotrexate is the racemate of Methotrexate (HY-14519). Methotrexate is an orally active antifolate (Antifolate). Methotrexate inhibits dihydrofolate reductase (DHFR), blocks tetrahydrofolate production, suppresses purine/pyrimidine synthesis and transmethylation, and causes intracellular accumulation of AICAR. Methotrexate promotes extracellular adenosine release, regulates the cytokine network, and inhibits the alarmin function of HMGB1. Methotrexate induces apoptosis and cytotoxicity, upregulates the expression of iNOS and COX-2, suppresses hippocampal neurogenesis, and induces pulmonary fibrosis. Methotrexate is used in the research of various immune and inflammation-related diseases such as arthritis, psoriasis, systemic lupus erythematosus, as well as pulmonary fibrosis and breast cancer.

(+)-Lariciresinol 4,4'-O-bis-β-D-glucopyranoside is a COX-2 inhibitor. (+)-Lariciresinol 4,4'-O-bis-β-D-glucopyranoside exhibits inhibitory effects on LPS (HY-D1056)-induced COX-2 activity in mouse peritoneal macrophages and reduces PGE₂ levels in the supernatant. (+)-Lariciresinol 4,4'-O-bis-β-D-glucopyranoside can be used for inflammation-related research.

1-(2,5-Dihydroxyphenyl)-3-hydroxybutan-1-one is an inhibitor of iNOS and COX-2. 1-(2,5-Dihydroxyphenyl)-3-hydroxybutan-1-one inhibits LPS-induced excessive production of NO and PGE₂, as well as the mRNA expression of pro-inflammatory cytokines TNF-α, IL-1β, IL-6 and IL-12. 1-(2,5-Dihydroxyphenyl)-3-hydroxybutan-1-one can be used in inflammation-related research.

COX-2-IN-49 (compound 6c) is a potent cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ value of 2.671 µM. COX-2-IN-49 shows antiproliferative activity. COX-2-IN-49 has the potential for the research of cancer.

PYZ18 is a selective COX-2 inhibitor with an IC₅₀ of 7.07 μM. PYZ18 is the best lead compound for COX-2 inhibitors. PYZ18 has anti-inflammatory and other biological properties.

Avicularin (Standard) is the analytical standard of Avicularin. This product is intended for research and analytical applications. Avicularin is an orally active flavonoid. Avicularin inhibits NF-κB (p65), COX-2 and PPAR-γ activities. Avicularin has anti-inflammatory, anti-infectious anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities.

COX-2-IN-44 is a potent and orally active COX-2 inhibitor with IC₅₀ values of 0.18,1.14 µM for COX-2, COX-1, respectively. COX-2-IN-44 shows anti-inflammatory activity.

Speranskoside is a dual COX-2/15-LOX inhibitor with a COX-2 IC₅₀ of 2.62 μg/mL and a 15-LOX IC₅₀ of 5.51 μg/mL. Speranskoside can be used for the research of gastric ulcers.

COX-2-IN-24 is an orally active inhibitor of COX-2 with IC₅₀ value of 0.17 μM, shows anti-inflammatory and low ulcerogenic activities.

PI3K/AKT-IN-6 is an orally effective PI3K/AKT signaling pathway inhibitor and anti-inflammatory agent. PI3K/AKT-IN-6 inhibits the production of pro-inflammatory cytokines TNF-α and IL-6, and downregulates the expression of inflammatory mediators COX-2 and iNOS. PI3K/AKT-IN-6 improves related symptoms in colitis mice. PI3K/AKT-IN-6 can be used for the research of inflammatory diseases such as colitis.

COX-2/5-LOX-IN-3 (compound 5b) is a potent and dual COX-2/5-LOX inhibitor with IC₅₀ values of 45.73, 5.45 and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively. COX-2/5-LOX-IN-3 has the potential for the research of inflammation diseases.

Akt/NF-κB/JNK-IN-1 (Compound 2i) is an inhibitor of Akt, NF-κB and JNK signaling pathways. Akt/NF-κB/JNK-IN-1 inhibits nitric oxide production with an IC₅₀ of 3.15 μM. Akt/NF-κB/JNK-IN-1 shows anti-inflammatory activities.

COX-2-IN-57 is an orally active COX-2 inhibitor with an IC₅₀ value of 0.02 μM. COX-2-IN-57 reduces MyD88 expression and decreases serum levels of COX-2, PGE2, and COX-1 in Cisplatin (HY-17394)/radiation-induced neuropathy rat model. COX-2-IN-57 demonstrates superior antinociceptive efficacy in hot plate, cold allodynia, and Randall-Selitto tests, along with hepato-/renal protection. COX-2-IN-57 can be used for the study of inflammation.

Leupeptin hydrochloride is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin hydrochloride significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin hydrochloride inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin hydrochloride can be used in research on chronic inflammatory diseases and skin tumorigenesis.

TLR4-IN-2 (Compound Racemic-11k) is inhibitors of TLR4, JNK, and NF-κB. TLR4-IN-2 inhibits NO production in LPS-stimulated RAW264.7 cells with an IC₅₀ value of 23.2 µM. TLR4-IN-2 exerts anti-inflammatory activity by inhibiting TLR4 expression, reducing JNK phosphorylation, thereby suppressing the activation of NF-κB, blocking the transcription of inflammation-related genes, reducing the expression of iNOS and COX-2, and decreasing the production of inflammatory mediators such as NO, PGE 2, and TNF-α. TLR4-IN-2 is promising for research of inflammatory diseases, such as rheumatoid arthritis and various inflammatory disorders.