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COX-2/5-LOX Inhibitor

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-111310
    ML351
    2 Publications Verification

    		 Lipoxygenase Neurological Disease Metabolic Disease
    ML351 is a potent and highly specific 15-LOX-1 inhibitor with an IC50 of 200 nM. ML351 shows excellent selectivity (>250-fold) versus the related isozymes, 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2 . ML351 prevents dysglycemia and reduces β-cell oxidative stress in nonobese diabetic mouse model of T1D .
    ML351
  • HY-N0232
    Psoralidin
    5 Publications Verification

    		 COX Lipoxygenase Notch Reactive Oxygen Species (ROS) Bacterial Cancer
    Psoralidin is a dual inhibitor of COX-2 and 5-LOX, regulates ionizing radiation (IR)-induced pulmonary inflammation.Anti-cancer, anti-bacterial, and anti-inflammatory properties . Psoralidin significantly downregulates NOTCH1 signaling. Psoralidin also greatly induces ROS generation .
    Psoralidin
  • HY-N7108
    7-Hydroxyflavone
    1 Publications Verification

    		 ERK Keap1-Nrf2 Apoptosis COX Pyruvate Kinase Lipoxygenase Enterovirus Virus Protease Infection Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology
    7-Hydroxyflavone is a flavonoid isolated from Clerodendrum phlomidis, with anti-inflammatory activity. 7-Hydroxyflavone protects renal cells from nicotine (NIC)-associated cytotoxicity via the ERK/Nrf2/HO-1 pathway. 7-Hydroxyflavone inhibits PKM2 with an IC50 of 2.12 μM. 7-Hydroxyflavone inhibits COX-2 and 5-LOX with IC50 of 27 µg/mL and 33 µg/mL. 7-Hydroxyflavone is orally active .
    7-Hydroxyflavone
  • HY-N0493
    Pectolinarigenin
    2 Publications Verification

    		 COX Lipoxygenase NF-κB p38 MAPK ERK HIF/HIF Prolyl-Hydroxylase Keap1-Nrf2 PI3K Apoptosis Autophagy Neurological Disease Inflammation/Immunology Cancer
    Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma .
    Pectolinarigenin
  • HY-10439
    HPGDS inhibitor 1

    		PGE synthase Inflammation/Immunology
    HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX .
    HPGDS inhibitor 1
  • HY-N1942
    5-O-Demethylnobiletin
    3 Publications Verification

    5-Demethylnobiletin

    		 Lipoxygenase Leukotriene Receptor Neurological Disease Inflammation/Immunology Cancer
    5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Citrus jambhiri Lush., is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM .
    5-O-Demethylnobiletin
  • HY-116763
    COX-2/5-LOX-IN-4

    		COX LOX-1
    COX-2/5-LOX-IN-4 (Compound 1) is a dual inhibitor that acts on both COX-2 and 5-LOX, with IC50 values of 0.05 μM for COX-2 and 0.003 μM for 5-LOX. By inhibiting the arachidonic acid metabolism pathway, COX-2/5-LOX-IN-4 reduces the production of prostaglandins and leukotrienes, alleviating inflammatory responses. In a rat ear edema model, intravenous administration (0.01 and 0.1 mg/kg) reduced edema by 41% and 44%, respectively, demonstrating significant anti-inflammatory effects. COX-2/5-LOX-IN-4 shows promise for studying the mechanisms of inflammatory diseases .
    COX-2/5-LOX-IN-4
  • HY-149269
    COX-2-IN-30

    		COX Carbonic Anhydrase LOX-1 Inflammation/Immunology
    COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect .
    COX-2-IN-30
  • HY-170938
    AChE-IN-82

    		Cholinesterase (ChE) Monoamine Oxidase Beta-secretase COX LOX-1 Neurological Disease
    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 .
    AChE-IN-82
  • HY-151173
    XO/COX/LOX-IN-1

    		Xanthine Oxidase Lipoxygenase COX Metabolic Disease Inflammation/Immunology
    XO/COX/LOX-IN-1 is a XO/COX/LOX inhibitor with an IC50 of 3.2 μM against rat XO, 10.83 μM against 5-LOX, 12.67 μM against COX-1, and 8.31 μM against COX-2. XO/COX/LOX-IN-1 binds to the active sites of XO, 5-LOX, COX-1 and COX-2, thereby blocking enzyme activities associated with uric acid, leukotriene, prostaglandin synthesis and inflammatory pathways. XO/COX/LOX-IN-1 can be used in the research of hyperuricemia and inflammation .
    XO/COX/LOX-IN-1
  • HY-175970
    MLS000099089

    		Lipoxygenase Neurological Disease
    MLS000099089 is a 12/15-lipoxygenase (12/15-LOX) inhibitor with IC50 values of 3.4 μM and 10 μM for human and mice 12/15-LOX, respectively. MLS000099089 displays higher selectivity for 12/15-LOX over 5-LOX and COX-2. MLS000099089 can be used for the study of stroke .
    MLS000099089
  • HY-N7108R
    7-Hydroxyflavone (Standard)

    		Reference Standards ERK Keap1-Nrf2 Apoptosis COX Pyruvate Kinase Lipoxygenase Enterovirus Virus Protease Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    7-Hydroxyflavone (Standard) is the analytical standard of 7-Hydroxyflavone. This product is intended for research and analytical applications. 7-Hydroxyflavone is a flavonoid isolated from Clerodendrum phlomidis, with anti-inflammatory activity. 7-Hydroxyflavone protects renal cells from nicotine (NIC)-associated cytotoxicity via the ERK/Nrf2/HO-1 pathway. 7-Hydroxyflavone inhibits PKM2 with an IC50 of 2.12 μM. 7-Hydroxyflavone inhibits COX-2 and 5-LOX with IC50 of 27 µg/mL and 33 µg/mL. 7-Hydroxyflavone is orally active .
    7-Hydroxyflavone (Standard)
  • HY-113807
    ZLJ-6

    		COX Lipoxygenase Inflammation/Immunology
    ZLJ-6 is a dual COX and 5-LOX inhibitor with oral activity. The IC50 values for COX-1, COX-2 and 5-LOX were 0.73, 0.31 and 0.99 μM, respectively. ZLJ-6 has anti-inflammatory and analgesic activity .
    ZLJ-6
  • HY-147951
    COX-2/5-LOX-IN-3

    		COX Lipoxygenase Inflammation/Immunology
    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 .
    COX-2/5-LOX-IN-3
  • HY-149270
    COX-2-IN-31

    		COX Inflammation/Immunology
    COX-2-IN-31 (compound 7b) is an orally active and dual inhibitor of COX-2 (IC50=60 nM) and 5-LOX (IC50=1.9 μM). COX-2-IN-31 also inhibits transmembrane hCA IX(Ki=48.9 nM) and hCA XII(Ki=5.8 nM) activity. COX-2-IN-31 exhibits anti-inflammatory and analgesic activity .
    COX-2-IN-31
  • HY-162523
    hMAO-B-IN-8

    		Monoamine Oxidase Cholinesterase (ChE) COX Lipoxygenase Neurological Disease
    hMAO-B-IN-8 (Compound 23) is a hMAO-B, eeAChE, COX-2 and 5-LOX inhibitor, with IC50 values of 0.037 μM, 0.071 μM, 14.3 μM and 0.59 μM, respectively. hMAO-B-IN-8 can be used for the research of Alzheimer's disease .
    hMAO-B-IN-8
  • HY-146295
    COX-2/5-LOX-IN-2

    		COX Inflammation/Immunology
    COX-2/5-LOX-IN-2 (5b) is a potent and dual inhibitor of COX-2/5-LOX. COX-2/5-LOX-IN-2 is a benzothiophen-2-yl pyrazole carboxylic acid derivative. COX-2/5-LOX-IN-2 shows the most potent analgesic and anti-inflammatory activities surpassing that of Celecoxib and Indomethacin. COX-2/5-LOX-IN-2 shows potent COX-1, COX-2 and 5-LOX inhibitory activity with IC50s of 5.40, 0.01 and 1.78 μM, respectively .
    COX-2/5-LOX-IN-2
  • HY-146294
    COX-2/5-LOX-IN-1

    		COX Inflammation/Immunology
    COX-2/5-LOX-IN-1 (compound 3a) is a potent and dual inhibitor of COX-2/5-LOX. COX-2/5-LOX-IN-1 is a benzothiophen-2-yl pyrazole carboxylic acid derivative. COX-2/5-LOX-IN-1 shows the most potent analgesic and anti-inflammatory activities surpassing that of Celecoxib and Indomethacin. COX-2/5-LOX-IN-1 shows potent COX-1, COX-2 and 5-LOX inhibitory activity with IC50s of 12.13, 0.4 and 4.96 μM, respectively .
    COX-2/5-LOX-IN-1
  • HY-172790
    Cbz-(S,S)-Pro-Pro-allyl

    		COX Lipoxygenase Inflammation/Immunology
    Cbz-(S,S)-Pro-Pro-allyl (compound 1a) is a dual inhibitor of cyclooxygenase-2 and 5-lipoxygenase with IC50 values of 0.146 nM, 0.003 nM, 0.64 nM for COX-1, COX-2, 5-LOX, respectively. Cbz-(S,S)-Pro-Pro-allyl has anti-inflammatory activity .
    Cbz-(S,S)-Pro-Pro-allyl
  • HY-N0232R
    Psoralidin (Standard)

    		Reference Standards COX Lipoxygenase Notch Reactive Oxygen Species (ROS) Bacterial Cancer
    Psoralidin (Standard) is the analytical standard of Psoralidin. This product is intended for research and analytical applications. Psoralidin is a dual inhibitor of COX-2 and 5-LOX, regulates ionizing radiation (IR)-induced pulmonary inflammation.Anti-cancer, anti-bacterial, and anti-inflammatory properties . Psoralidin significantly downregulates NOTCH1 signaling. Psoralidin also greatly induces ROS generation .
    Psoralidin (Standard)
  • HY-114796
    tHGA

    		Lipoxygenase Inflammation/Immunology
    tHGA is a compound with anti-inflammatory activity and has the activity to inhibit soybean 15-LOX. tHGA showed significant inhibitory effects in experiments on human leukocytes, with an IC50 value of 0.42 μM, which is close to the effect of commonly used standard NDGA. tHGA concentration-dependently inhibits the synthesis of 5-LOX products, especially the cysteine leukotriene LTC(4), with an IC50 value of 1.80 μM. and showed no cytotoxicity. The anti-inflammatory effects of tHGA do not appear to be through redox or metal chelation mechanisms, as the compound was negative in these bioactivity tests. tHGA works through a dual LOX/COX inhibition mechanism and has higher selectivity for 5-LOX and COX-2, with an IC50 value of 0.40 μM .
    tHGA
  • HY-N1942R
    5-O-Demethylnobiletin (Standard)

    5-Demethylnobiletin (Standard)

    		 Reference Standards Lipoxygenase Leukotriene Receptor Neurological Disease Inflammation/Immunology Cancer
    5-O-Demethylnobiletin (Standard) is the analytical standard of 5-O-Demethylnobiletin. This product is intended for research and analytical applications. 5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Citrus jambhiri Lush., is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM .
    5-O-Demethylnobiletin (Standard)
  • HY-159169
    5-LOX/sEH-IN-1

    		COX Epoxide Hydrolase Lipoxygenase Inflammation/Immunology
    5-LOX/sEH-IN-1 (Compound 8o) is a dual 5-LOX/sEH-IN-1 inhibitor with cardioprotective effects, exhibiting IC50 values of 3.05 μM and 2.20 nM respectively, and 5-LOX/sEH-IN-1 can also inhibit the activity of COX-2 (IC50=10.50 μM). 5-LOX/sEH-IN-1 has analgesic and anti-inflammatory effects, while reducing ulcer pathogenicity, and can be used to develop anti-inflammatory agents with fewer gastrointestinal and cardiovascular side effects .
    5-LOX/sEH-IN-1
  • HY-N0493R
    Pectolinarigenin (Standard)

    		Reference Standards COX Lipoxygenase NF-κB p38 MAPK ERK HIF/HIF Prolyl-Hydroxylase Keap1-Nrf2 PI3K Apoptosis Autophagy Inflammation/Immunology
    Pectolinarigenin (Standard) is the analytical standard of Pectolinarigenin. This product is intended for research and analytical applications. Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma.
    Pectolinarigenin (Standard)
  • HY-181044
    COX-2/5-LOX-IN-6

    		Lipoxygenase COX Inflammation/Immunology Cancer
    COX-2/5-LOX-IN-6 (Compound 4c) is a potent and selective 5-LOX (IC50 = 0.10 μM) and COX-2 (IC50: 2.88 μM) inhibitor. COX-2/5-LOX-IN-6 displays potent anticancer activity against ovarian cancer. COX-2/5-LOX-IN-6 would not cause cytotoxic effects in noncancerous cells. COX-2/5-LOX-IN-6 is a potential anti-inflammatory agent .
    COX-2/5-LOX-IN-6
  • HY-10439R
    HPGDS inhibitor 1 (Standard)

    		Reference Standards PGE synthase Inflammation/Immunology
    HPGDS inhibitor 1 (Standard) is the analytical standard of HPGDS inhibitor 1 (HY-10439). This product is intended for research and analytical applications. HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX .
    HPGDS inhibitor 1 (Standard)
  • HY-W676872
    Dihydroflavokawin B

    		COX Parasite Infection Inflammation/Immunology
    Dihydroflavokawin B is a selective COX-1 inhibitor with an IC50 of 1.22 μM. Dihydroflavokawin B weakly inhibits COX-2 and 5-LOX. Dihydroflavokawin B inhibits promastigote forms of Leishmania panamensis and Leishmania braziliensis. Dihydroflavokawin B inhibits rabbit platelet aggregation induced by Arachidonic acid, platelet activating factor, and adenosine diphosphate. Dihydroflavokawin B exhibits in vitro anti-inflammatory activity. Dihydroflavokawin B can be used for the research of leishmaniasis .
    Dihydroflavokawin B
  • HY-183764
    COX-2/5-LOX-IN-8

    		COX Lipoxygenase TNF Receptor Interleukin Related MMP Inflammation/Immunology
    COX-2/5-LOX-IN-8 is an orally active dual COX-2/5-LOX inhibitor, with an IC50 of 6.30 μM against sheep-derived COX-2 and an IC50 of 8.09 μM against 5-LOX. COX-2/5-LOX-IN-8 acts as a membrane stabilizer that stabilizes erythrocyte membranes against hypotonicity-induced hemolysis. COX-2/5-LOX-IN-8 functions as a protein stabilizer that inhibits heat-induced denaturation of bovine serum albumin. COX-2/5-LOX-IN-8 reduces paw swelling, improves hind limb weight-bearing function, decreases serum levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, CRP), and lowers serum levels of cartilage degradation biomarkers (COMP, MMP-3, CTX-II). COX-2/5-LOX-IN-8 can be used in the research of osteoarthritis .
    COX-2/5-LOX-IN-8
  • HY-181273
    COX-2/5-LOX-IN-7

    		COX Lipoxygenase Inflammation/Immunology
    COX-2/5-LOX-IN-7 (Hybrids 9) is a COX-2 (IC50 = 3.3 μM)/5-LOX (IC50 = 3.1 μM) inhibitor. COX-2/5-LOX-IN-7 can be used in research on diseases such as inflammation .
    COX-2/5-LOX-IN-7
  • HY-118506
    BRP-7

    		FLAP Inflammation/Immunology
    BRP-7 is a 5-lipoxygenase activating protein (FLAP) inhibitor with an IC50 of 0.31 μM. BRP-7 inhibits the co-localization of 5-lipoxygenase (5-LOX) and FLAP by targeting FLAP, thereby blocking the transfer of arachidonic acid (AA) to 5-LOX and suppressing the production of leukotrienes (LTs) (IC₅₀ = 0.15 μM). BRP-7 does not inhibit cyclooxygenase (COX-1/COX-2) or microsomal prostaglandin E₂ synthase-1 (mPGES-1), and does not affect cell viability or AA release. BRP-7 exhibits significant anti-inflammatory effects in rat pleurisy and mouse peritonitis models. BRP-7 can be used for the study of inflammatory diseases .
    BRP-7
  • HY-181061
    COX/5-LO-IN-2

    		COX EGFR Lipoxygenase FAK Raf Apoptosis Caspase Bcl-2 Family Cancer
    COX/5-LO-IN-2 is a COX2, EGFR, COX1, 5-LOX, BRAF and FAK inhibitor with IC50 of 1.22 μM, 2.5 μM, 2.95 μM, 4.65 μM, 7.4 μM, 12.2 μM, respectively. COX/5-LO-IN-2 induces cell growth arrest at G2/M phase. COX/5-LO-IN-2 triggers apoptotic activity by up-regulating proapoptotic proteins p53, Bax, and caspase-7 and down-regulating anti-apoptotic protein Bcl-2. COX/5-LO-IN-2 can be used for the research of breast cancer .
    COX/5-LO-IN-2

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