S1396 |
Resveratrol
|
Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis. |
-
Biochem Biophys Res Commun, 2024, 723:150186
-
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
-
Cell Death Dis, 2023, 14(6):367
|
|
S8011 |
U73122
|
U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca2+ increases in platelets and PMN. U73122 potently inhibits human 5-lipoxygenase (5-LO). |
-
Nat Commun, 2024, 15(1):1300
-
Autophagy, 2024, 10.1080/15548627.2024.2395797
-
Cell Rep, 2024, 43(3):113929
|
|
S1443 |
Zileuton
|
Zileuton is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma. Zileuton induces apoptosis while inhibits ferroptosis. |
-
Nat Commun, 2024, 15(1):8663
-
J Transl Med, 2023, 21(1):923
-
Cancer Sci, 2023, 10.1111/cas.15994
|
|
S6557 |
ML355
|
ML355 is a potent and selective inhibitor of human 12-Lipoxygenase with an IC50 of 290 nM and shows excellent selectivity over related lipoxygenases and cyclooxygenases. |
-
Vaccines (Basel), 2023, 11(2)205
-
Vaccines (Basel), 2023, 11(2)205
-
Redox Biol, 2022, 55:102421
|
|
S2277 |
Caffeic Acid
|
Caffeic acid is a hydroxycinnamic acid, a naturally occurring organic compound. Caffeic acid is an inhibitor of both TRPV1 ion channel and 5-Lipoxygenase (5-LO). |
-
Molecules, 2021, 26(5)1210
-
J Nutr Biochem, 2015, 26(11):1379-84
-
Sci Rep, 2015, 5:12580
|
|
S1137 |
Malotilate
|
Malotilate (NKK105) is a drug used for the treatment of liver cirrhosis. Malotilate is a liver protein metabolism improved compound, which selectively inhibit the 5-lipoxygenase. |
-
J Cachexia Sarcopenia Muscle, 2022, 13(6):3062-3077
-
J Cachexia Sarcopenia Muscle, 2022, 13(6):3062-3077
|
|
S6956 |
PD146176
|
PD146176 (NSC168807) is a potent inhibitor of 15-lipoxygenase (15-LO) with Ki of 197 nM for rabbit reticulocyte 15-LO. |
-
Br J Cancer, 2023, 129(4):601-611
-
Br J Cancer, 2023, 129(4):601-611
|
|
S3168 |
cis-Resveratrol
|
cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. |
-
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
|
|
S9024 |
AKBA (3-O-Acetyl-11-keto-β-boswellic acid)
|
AKBA (3-O-Acetyl-11-keto-β-boswellic acid), the major active ingredient of the gum resin from Boswellia serrata and Boswellia carteri Birdw., exerts anti-inflammatory therapeutic effects and noncompetitively inhibits 5-lipoxygenase, topoisomerase, and leukocyte elastase. |
-
Nat Cancer, 2022, 3(5):629-648
|
|
S9421 |
Demethylnobiletin
|
Demethylnobiletin (5-Demethylnobiletin) is a unique flavonoid found in citrus fruits with potential chemopreventive effects against human cancers.5-Demethylnobiletin is a direct inhibitor of 5-LOX with IC50 of 0.1 μM, without affecting the expression of COX-2. 5-Demethylnobiletin has anti-inflammatory activity, inhibits leukotriene B 4(LTB4) formation in rat neutrophils and elastase release in human neutrophils with IC50 of 0.35 μM. |
-
Front Oncol, 2023, 13:1143664
|
|
S4711 |
Esculetin
|
Esculetin (Cichorigenin, Aesculetin) is a coumarin derivative found in various natural plant products with various biological and pharmaceutical properties including anti-edema, anti-inflammatory and anti-tumour effects. It inhibits lipoxygenases (LOs). |
-
Cancer Lett, 2021, S0304-3835(21)00436-5
|
|
S3984 |
Nordihydroguaiaretic acid (NDGA)
|
Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. |
|
|
E2671 |
SR 2640 hydrochloride
|
SR2640 hydrochloride is a potent and selective competitive leukotriene D4/E4 antagonist. |
|
|
S0759 |
FPL 62064
|
FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and prostaglandin synthetase (cyclooxygenase, COX) with IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and seminal vesicle prostaglandin synthetase, respectively. FPL 62064 has potent anti-inflammatory activity. |
|
|
S3387 |
ML351
|
ML351 is a selective inhibitor of 15-Lipoxygenase-1 (15-LOX-1 or 12/15-LOX) with IC50 of 200 nM. |
|
|
E0335 |
4-MMPB
|
4-MMPB, a selective inhibitor of 15-lipoxygenase (15-LO) with an IC50 of 18 μM, shows IC50s of 19.5 μM and 19.1 μM for soybean 15-lipoxygenase (SLO) and human 15-lipoxygenase-1 (15-LOX-1), respectively. |
|
|
S5122 |
Abietic Acid
|
Abietic acid (Sylvic acid, Abietate, Rosin Acid), an abietane diterpenoid, inhibited soybean 5-lipoxygenase with an IC50 of 29.5 ± 1.29 μM. |
|
|
E0320New |
Atuliflapon (AZD5718)
|
Atuliflapon (AZD5718) is an oral inhibitor of (FLAP) 5-lipoxygenase activating protein with an IC50 of 2.0 nM. It has the potential to treat coronary artery disease. |
|
|
S5520 |
Phenidone
|
Phenidone (1-phenyl-3-pyrazolidinone), a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), is an organic compound that is primarily used as a photographic developer. |
|
|
S9378 |
4',5-Dihydroxyflavone
|
4',5-Dihydroxyflavone inhibits soybean LOX-1 and yeast α-glucosidase. |
|
|
E0226 |
Chebulagic acid
|
Chebulagic acid, isolated form Terminalia chebula Retz, is a reversible and non-competitive inhibitor of maltase with a Ki value of 6.6 μM. Chebulagic acid shows potent anti-inflammatory effects in LPS-stimulated RAW 264.7 cells. Chebulagic acid also shows potent COX–LOX dual inhibition activity with IC50 values of 15 μM, 0.92 μM and 2.1 μM for COX-1, COX-2 and 5-LOX respectively.
|
|
|
S3255 |
Pectolinarigenin
|
Pectolinarigenin, an active anti-inflammatory ingredient in Cirsium chanroenicum, is a dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). |
|
|
S6228 |
Indole-2-carboxylic acid
|
Indole-2-carboxylic acid is a strong inhibitor of lipid peroxidation. |
|
|
S3283 |
Marmesin
|
Marmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) is a natural coumarin with COX-2 and 5-LOX dual inhibitory activity. |
|
|
S1396 |
Resveratrol
|
Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis. |
- Biochem Biophys Res Commun, 2024, 723:150186
- J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
- Cell Death Dis, 2023, 14(6):367
|
|
S8011 |
U73122
|
U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca2+ increases in platelets and PMN. U73122 potently inhibits human 5-lipoxygenase (5-LO). |
- Nat Commun, 2024, 15(1):1300
- Autophagy, 2024, 10.1080/15548627.2024.2395797
- Cell Rep, 2024, 43(3):113929
|
|
S1443 |
Zileuton
|
Zileuton is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma. Zileuton induces apoptosis while inhibits ferroptosis. |
- Nat Commun, 2024, 15(1):8663
- J Transl Med, 2023, 21(1):923
- Cancer Sci, 2023, 10.1111/cas.15994
|
|
S6557 |
ML355
|
ML355 is a potent and selective inhibitor of human 12-Lipoxygenase with an IC50 of 290 nM and shows excellent selectivity over related lipoxygenases and cyclooxygenases. |
- Vaccines (Basel), 2023, 11(2)205
- Vaccines (Basel), 2023, 11(2)205
- Redox Biol, 2022, 55:102421
|
|
S2277 |
Caffeic Acid
|
Caffeic acid is a hydroxycinnamic acid, a naturally occurring organic compound. Caffeic acid is an inhibitor of both TRPV1 ion channel and 5-Lipoxygenase (5-LO). |
- Molecules, 2021, 26(5)1210
- J Nutr Biochem, 2015, 26(11):1379-84
- Sci Rep, 2015, 5:12580
|
|
S1137 |
Malotilate
|
Malotilate (NKK105) is a drug used for the treatment of liver cirrhosis. Malotilate is a liver protein metabolism improved compound, which selectively inhibit the 5-lipoxygenase. |
- J Cachexia Sarcopenia Muscle, 2022, 13(6):3062-3077
- J Cachexia Sarcopenia Muscle, 2022, 13(6):3062-3077
|
|
S6956 |
PD146176
|
PD146176 (NSC168807) is a potent inhibitor of 15-lipoxygenase (15-LO) with Ki of 197 nM for rabbit reticulocyte 15-LO. |
- Br J Cancer, 2023, 129(4):601-611
- Br J Cancer, 2023, 129(4):601-611
|
|
S3168 |
cis-Resveratrol
|
cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. |
- J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
|
|
S9024 |
AKBA (3-O-Acetyl-11-keto-β-boswellic acid)
|
AKBA (3-O-Acetyl-11-keto-β-boswellic acid), the major active ingredient of the gum resin from Boswellia serrata and Boswellia carteri Birdw., exerts anti-inflammatory therapeutic effects and noncompetitively inhibits 5-lipoxygenase, topoisomerase, and leukocyte elastase. |
- Nat Cancer, 2022, 3(5):629-648
|
|
S9421 |
Demethylnobiletin
|
Demethylnobiletin (5-Demethylnobiletin) is a unique flavonoid found in citrus fruits with potential chemopreventive effects against human cancers.5-Demethylnobiletin is a direct inhibitor of 5-LOX with IC50 of 0.1 μM, without affecting the expression of COX-2. 5-Demethylnobiletin has anti-inflammatory activity, inhibits leukotriene B 4(LTB4) formation in rat neutrophils and elastase release in human neutrophils with IC50 of 0.35 μM. |
- Front Oncol, 2023, 13:1143664
|
|
S4711 |
Esculetin
|
Esculetin (Cichorigenin, Aesculetin) is a coumarin derivative found in various natural plant products with various biological and pharmaceutical properties including anti-edema, anti-inflammatory and anti-tumour effects. It inhibits lipoxygenases (LOs). |
- Cancer Lett, 2021, S0304-3835(21)00436-5
|
|
S3984 |
Nordihydroguaiaretic acid (NDGA)
|
Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. |
|
|
S0759 |
FPL 62064
|
FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and prostaglandin synthetase (cyclooxygenase, COX) with IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and seminal vesicle prostaglandin synthetase, respectively. FPL 62064 has potent anti-inflammatory activity. |
|
|
S3387 |
ML351
|
ML351 is a selective inhibitor of 15-Lipoxygenase-1 (15-LOX-1 or 12/15-LOX) with IC50 of 200 nM. |
|
|
E0335 |
4-MMPB
|
4-MMPB, a selective inhibitor of 15-lipoxygenase (15-LO) with an IC50 of 18 μM, shows IC50s of 19.5 μM and 19.1 μM for soybean 15-lipoxygenase (SLO) and human 15-lipoxygenase-1 (15-LOX-1), respectively. |
|
|
S5122 |
Abietic Acid
|
Abietic acid (Sylvic acid, Abietate, Rosin Acid), an abietane diterpenoid, inhibited soybean 5-lipoxygenase with an IC50 of 29.5 ± 1.29 μM. |
|
|
E0320New |
Atuliflapon (AZD5718)
|
Atuliflapon (AZD5718) is an oral inhibitor of (FLAP) 5-lipoxygenase activating protein with an IC50 of 2.0 nM. It has the potential to treat coronary artery disease. |
|
|
S5520 |
Phenidone
|
Phenidone (1-phenyl-3-pyrazolidinone), a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), is an organic compound that is primarily used as a photographic developer. |
|
|
S9378 |
4',5-Dihydroxyflavone
|
4',5-Dihydroxyflavone inhibits soybean LOX-1 and yeast α-glucosidase. |
|
|
E0226 |
Chebulagic acid
|
Chebulagic acid, isolated form Terminalia chebula Retz, is a reversible and non-competitive inhibitor of maltase with a Ki value of 6.6 μM. Chebulagic acid shows potent anti-inflammatory effects in LPS-stimulated RAW 264.7 cells. Chebulagic acid also shows potent COX–LOX dual inhibition activity with IC50 values of 15 μM, 0.92 μM and 2.1 μM for COX-1, COX-2 and 5-LOX respectively.
|
|
|
S3255 |
Pectolinarigenin
|
Pectolinarigenin, an active anti-inflammatory ingredient in Cirsium chanroenicum, is a dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). |
|
|
S6228 |
Indole-2-carboxylic acid
|
Indole-2-carboxylic acid is a strong inhibitor of lipid peroxidation. |
|
|
S3283 |
Marmesin
|
Marmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) is a natural coumarin with COX-2 and 5-LOX dual inhibitory activity. |
|
|