NF-κB

Signaling Pathway Map

Research Area

Inhibitory Selectivity

NF-κB Products

Catalog No. Information Product Use Citations Product Validations
S1013

Bortezomib (PS-341)

Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.

S4902

QNZ (EVP4593)

QNZ (EVP4593) shows potent inhibitory activity toward both NF-κB activation and TNF-α production with IC50 of 11 nM and 7 nM in Jurkat T cells, respectively.

S1623

Acetylcysteine(N-acetylcysteine)

Acetylcysteine(N-acetyl-l-cysteine) is a ROS(reactive oxygen species) inhibitor that antagonizes the activity of proteasome inhibitors. It is also a tumor necrosis factor production inhibitor. Acetylcysteine(N-acetyl-l-cysteine) suppresses TNF-induced NF-κB activation through inhibition of IκB kinases. Acetylcysteine(N-acetyl-l-cysteine) induces apoptosis via the mitochondria-dependent pathway. Acetylcysteine(N-acetyl-l-cysteine) inhibits ferroptosis and virus replication.Solutions of Acetylcysteine are best fresh-prepared.

S1848

Curcumin

Curcumin is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM) and Histone deacetylase; activates Nrf2 pathway and supresses the activation of transcription factor NF-κB.

S4073

Sodium 4-Aminosalicylate

Sodium 4-Aminosalicylate is an antibiotic used to treat tuberculosis via NF-κB inhibition and free radical scavenging.

S6671New

SN50

SN50, a cell-permeable NF-κB inhibitory peptide, is composed of the signal peptide of Kaposi fibroblast growth factor.SN50 inhibits the activation of NF-κB and attenuates ventilator-induced lung injury.

S8941New

NIK SMI1

NIK SMI1 is a highly potent and selective NF-κB-inducing kinase (NIK) inhibitor with Ki of 0.23 nM for NIK-catalyzed hydrolysis of ATP to ADP.

S6714New

INH14

INH14 is an inhibitor of TLR2-mediated NF-kB activation with IC50 values of 8.975 μM and 3.598 μM for IKKα and IKKβ, respectively.

S7351

JSH-23

JSH-23 is an inhibitor of NF-κB transcriptional activity with IC50 of 7.1 μM in RAW 264.7 cell line.

S7414

Caffeic Acid Phenethyl Ester

Caffeic acid phenethyl ester is a potent and specific inhibitor of NF-κB activation, and also displays antioxidant, immunomodulatory and antiinflammatory activities.

S3137

Sodium salicylate

Sodium salicylate is used in medicine as an analgesic and antipyretic.

S3939

4'-Methoxyresveratrol

4-Methoxyresveratrol is a stibenoid found in the Chinese herb Gnetum cleistostachyum. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation.

S4798

Benfotiamine

Benfotiamine is a synthetic S-acyl derivative of thiamine (vitamin B1) and has been investigated for the treatment and prevention of Diabetic Nephropathy and Diabetes Mellitus, Type 2. Benfotiamine suppresses oxidative stress-induced NF-κB activation and prevents the bacterial endotoxin-induced inflammation.

S7672

Omaveloxolone (RTA-408)

Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.

S3998

(+)-α-Lipoic acid

R(+)-α-lipoic acid, a physiological form of thioctic acid, is a strong antioxidant that relieves diabetic neuropathic symptoms. It shows superior antioxidative effects to its racemate. α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation.

S5144

Neferine

Neferine, a natural component of Nelumbo nucifera, has antitumor efficiency in cancer. Neferine((-)-Neferine) is a unique bis-benzylisoquinoline alkaloid that possesses a number of therapeutic effects such as anti-cancer, anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.

S9208

Ginsenoside Rb3

Ginsenoside Rb3, extracted from the plant Panax ginseng, plays important roles in cardiovascular diseases, including myocardial ischemia-reperfusion (I/R) injury. Ginsenoside Rb3 (0.1-10 μM) is tested for inhibition of tumor necrosis factor-α (TNF)-induced nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) luciferase reporter activity using a human kidney 293T cell-based assay. Ginsenoside Rb3 shows the significant activity with an IC50 of 8.2 μM. Ginsenoside Rb3 also inhibits the induction of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) messenger Ribonucleic acid (mRNA) in a dose-dependent manner after HepG2 cells have been treated with TNF-α (10 ng/mL).

S3633

Pyrrolidinedithiocarbamate ammonium

Ammonium pyrrolidine dithiocarbamate (PDTC) is a potent nuclear factor-κB (NF-κB) inhibitor that inhibits IκB phosphorylation, blocks NF-κB translocation to the nucleus and reduces the expression of downstream cytokines.

S3816

Dehydroevodiamine

Dehydroevodiamine, a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.

S9244

8-O-acetyl shanzhiside methyl ester

8-O-acetyl shanzhiside methyl ester, isolated from the leaves of Lamiophlomis rotata Kudo, promotes angiogenesis, which leads to the improvement of functional outcome after stroke.8-O-Acetyl shanzhiside methyl ester can inhibts NF-κB

S8484

GSK2982772

GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase (RIPK1) inhibitor with the IC50 value of 16 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses.

S8642

GSK'963

GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase (RIPK1) with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.

S8261

GSK583

GSK583 is a highly potent and selective inhibitor of RIP2 kinase with an IC50 of 5 nM.

S2261

Andrographolide

Andrographolide is a labdane diterpenoid that is the main bioactive component of the medicinal plant Andrographis paniculata.

S2382

Evodiamine

Evodiamine (Isoevodiamine), an alkaloid extract from the fruit of Evodiae Fructus exhibits antitumor activities against the human tumor cells. It is shown to inhibit NF-kB activation through suppression of IkB kinase activity.

S4937

4'-Hydroxychalcone

4'-Hydroxychalcone, found in herbs and spices and tea, is a member of the class of compounds known as retrochalcones. It has diverse biological activities, inhibiting TNFα-induced NF-κB pathway activation in a dose-dependent manner and activating BMP signaling.

S9295

Dauricine

Dauricine, a plant metabolite isolated from the Asian vine Menispermum dauricum, plays a variety of biological roles in the human body, from inhibiting cancer cell growth to blocking cardiac transmembrane Na+, K+, and Ca2+ ion currents.Dauricine induces apoptosis, inhibits proliferation and invasion through inhibiting NF‐κB signaling pathway in colon cancer cells.

S5343

Vanillic acid

Vanillic acid is a flavoring agent which is also an intermediate in the production of vanillin from ferulic acid. Vanillic acid inhibits NF-κB activation. Anti-inflammatory, antibacterial, and chemopreventive effects.

S9193

Aristolochic acid A

Aristolochic acid A is a carcinogenic, mutagenic, and nephrotoxic agent extracted from the flowering plant family Aristolochiaceae.Aristolochic acid A significantly reduces both activator protein 1 (AP-1) and nuclear factor-κB (NF-κB) activities.

S2313

Indole-3-carbinol

Indole-3-carbinol is produced by the breakdown of the glucosinolate glucobrassicin, which can be found at relatively high levels in cruciferous vegetables. Indole-3-carbinol suppresses NF-κB and IκBα kinase activation.

S9040

Maslinic acid

Maslinic Acid, a Natural Triterpene, exerts a wide range of biological activities, i.e. antitumor, antidiabetic, antioxidant, cardioprotective, neuroprotective, antiparasitic and growth-stimulating. MA significantly suppresses the DNA-binding activity of NF-κB p65 in LPS-induced RAW 264.7 cells.

S7273

SC75741

SC75741 is a potent NF-κB inhibitor with EC50 of 200 nM.

S3760

Stachydrine hydrochloride

Stachydrine is isolated from seed husk and the pulp of the fruit of C. Leonurus, and many other Asian plants and fruits. It has potent anti-metastatic activity and cardioprotective effects. Stachydrine hydrochloride is the major active constituent of Herba Leonuri, which is a potential therapy for cardiovascular diseases. Stachydrine can inhibit the NF-κB signal pathway. Anti-hypertrophic activities.

S3770

Sodium Aescinate

Sodium aescinate (SA) is a widely-applied triterpene saponin product derived from horse chestnut seeds, possessing vasoactive and organ-protective activities with oral or injection administration in the clinic. Sodium aescinate is a triterpene saponin derived from Aesculus hippocastanum seeds, with anti-inflammatory and antioxidant activities. Sodium aescinate inhibits hepatocellular carcinoma growth by targeting CARMA3/NF-κB pathway.

S3771

Stachydrine

Stachydrine, also known as N,N-dimethylproline or proline betaine, is a quaternary ammonium derivative of proline that occurs widely in Medicago species. It is an osmoprotective compound found in urine. Stachydrine is a major constituent of Chinese herb leonurus heterophyllus sweet used to promote blood circulation and dispel blood stasis. Stachydrine can inhibit the NF-κB signal pathway.

S3773

Tyrosol

Tyrosol is an antioxidant that is naturally present in several foods such as wines and green tea and is present most abundantly in olives. Tyrosol is a derivative of phenethyl alcohol. Tyrosol attenuates pro-inflammatory cytokines from cultured astrocytes and NF-κB activation. Anti-oxidative and anti-inflammatory effects.

S8483

CBL0137 HCl (CBL-0137 HCl)

CBL0137(CBL-0137) activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex).

S9388

(+)-Praeruptorin A

Praeruptorin A is a coumarin compound naturally occurring in the roots of Peucedanum praeruptorum Dunn., a commonly used traditional Chinese medicine for the treatment of certain respiratory diseases and hypertension. (+)-Praeruptorin A is one of enantiomers that shows more potent relaxant effects than (−)-praeruptorin A in rat aorta rings and may be an activator of eNOS.

S2321

Magnolol

Magnolol is a bioactive lignin found in the bark of the Houpu magnolia (Magnolia officinalis) which shows antifungal properties. It can block TNF-α-induced NF-KB activation.

S3874

Curcumenol

Curcumenol, a sesquiterpene isolated from Curcuma zedoaria, is known to possess a variety of health and medicinal values which includes neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. It inhibits NF-κB activation by suppressing the nuclear translocation of the NF-κB p65 subunit and blocking IκBα phosphorylation and degradation.

S1825

Erdosteine

Erdosteine is a mucolytic which is used in treatment of excessive viscous mucus. Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation.

S3880

Schisantherin A

Schisantherin A, also known as Gomisin C, is a dibenzocyclooctadiene that exhibits anti-tussive, sedative, anti-inflammatory, anti-osteoporotic, neuroprotective, cognition enhancing, and cardioprotective activities. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.

S8341

TAK-243 (MLN7243)

TAK-243 (MLN7243) is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE) with an IC50 of 1 ± 0.2 nM in the UBCH10 E2 thioester assay. It has minimal inhibitory activity in a panel of kinase and receptor assays, as well as on human carbonic anhydrase type I and type II. TAK-243 (MLN7243) induces ER stress, abrogates NFκB pathway activation and promotes apoptosis.

S4763

4-Hydroxychalcone

4-Hydroxychalcone is a chalcone metabolite with diverse biological activities. It inhibits TNFα-induced NF-κB pathway activation in a dose-dependent manner and also activates BMP signaling.

S9106

Eleutheroside E

Eleutheroside E, a principal component of Eleutherococcus senticosus (ES), has anti-inflammatory effects by inhibiting NF-κB and protecting against myocardial infarction.

S3808

Mangiferin

Mangiferin is a bioactive compound that demonstrates many health perspectives and has been used to prepare medicinal and food supplements. Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50.

S2341

(-)-Parthenolide

(-)-Parthenolide, an inhibitor of the Nuclear Factor-κB Pathway, specifically depletes HDAC1 protein without affecting other class I/II HDACs; Also promotes the ubiquitination of MDM2 and activates p53 cellular functions.

S3604

Triptolide (PG490)

Triptolide is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein.

S3811

Ginsenoside Re

Ginsenoside Re (Ginsenoside B2), an extract from Panax notoginseng, is a major ginsenoside in ginseng and belongs to 20(S)-protopanaxatriol group. It has diverse in vitro and in vivo effects, including vasorelaxant, antioxidant, antihyperlipidemic, and angiogenic actions. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB.

S3138

Methylthiouracil

Methylthiouracil is an antithyroid preparation. Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.

S3899

Hederagenin

Hederagenin is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo.

S5453

Hyperoside

Hyperoside, a naturally occuring flavonoid compound, exerts multiple bioactivities, including myocardial protection, anti-redox, and anti-inflammatory activities.Hyperoside can inhibit activation of the NF-κB signaling pathway.

S3867

(E)-Cardamonin

Cardamonin is a naturally occurring chalcone with strong anti-inflammatory activity. It is a novel TRPA1 antagonist with IC50 of 454 nM and also a NF-kB inhibitor.

S3872

Guaiacol

Guaiacol is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a precursor to various flavorants, such as eugenoland vanillin. Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.

S4712

Diethylmaleate

Diethylmaleate is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NF-kB.

S9170

Engeletin

Engeletin, a bioactive flavonoid, has multiple biological activities such as anti-diabetic and anti-inflammatory effects. engeletin againsts LPS-stimulated endometritis in mice via negative regulation of pro-inflammatory mediators via the TLR4-regulated NF-κB pathway.

S3923

Ginsenoside Rg1

Ginsenoside Rg1, one of the major active components of ginseng, is identified as a protopanaxatriol-type and has pharmacological actions such as neuroprotective and anti-tumor effects on various cancer types. Ginsenoside Rg1 reduces cerebral Aβ levels and NF-κB nuclear translocation.

S3924

Ginsenoside Rb1

Ginsenoside Rb1 is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65.

S3603

Betulinic acid

Betulinic acid, a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Betulinic acid acts as a new activator of NF-kB.Phase 1/2.

S5804

N-Acetylcysteine amide

N-acetylcysteine amide is a membrane penetrating antioxidant with anti-inflamatory activity through regulation of activation of NF-κB and HIF-1α as well as modulation of ROS.

S2371

Vanillylacetone

Vanillylacetone is similar in chemical structure to other flavor chemicals such as vanillin and eugenol and is used as a flavor additive in spice oils and in perfumery to introduce spicy aromas. Vanillylacetone (Zingerone) alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways. Zingerone acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells.

Catalog No. Information Product Use Citations Product Validations
S1013

Bortezomib (PS-341)

Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.

S4902

QNZ (EVP4593)

QNZ (EVP4593) shows potent inhibitory activity toward both NF-κB activation and TNF-α production with IC50 of 11 nM and 7 nM in Jurkat T cells, respectively.

S1623

Acetylcysteine(N-acetylcysteine)

Acetylcysteine(N-acetyl-l-cysteine) is a ROS(reactive oxygen species) inhibitor that antagonizes the activity of proteasome inhibitors. It is also a tumor necrosis factor production inhibitor. Acetylcysteine(N-acetyl-l-cysteine) suppresses TNF-induced NF-κB activation through inhibition of IκB kinases. Acetylcysteine(N-acetyl-l-cysteine) induces apoptosis via the mitochondria-dependent pathway. Acetylcysteine(N-acetyl-l-cysteine) inhibits ferroptosis and virus replication.Solutions of Acetylcysteine are best fresh-prepared.

S1848

Curcumin

Curcumin is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM) and Histone deacetylase; activates Nrf2 pathway and supresses the activation of transcription factor NF-κB.

S4073

Sodium 4-Aminosalicylate

Sodium 4-Aminosalicylate is an antibiotic used to treat tuberculosis via NF-κB inhibition and free radical scavenging.

S6671New

SN50

SN50, a cell-permeable NF-κB inhibitory peptide, is composed of the signal peptide of Kaposi fibroblast growth factor.SN50 inhibits the activation of NF-κB and attenuates ventilator-induced lung injury.

S8941New

NIK SMI1

NIK SMI1 is a highly potent and selective NF-κB-inducing kinase (NIK) inhibitor with Ki of 0.23 nM for NIK-catalyzed hydrolysis of ATP to ADP.

S6714New

INH14

INH14 is an inhibitor of TLR2-mediated NF-kB activation with IC50 values of 8.975 μM and 3.598 μM for IKKα and IKKβ, respectively.

S7351

JSH-23

JSH-23 is an inhibitor of NF-κB transcriptional activity with IC50 of 7.1 μM in RAW 264.7 cell line.

S7414

Caffeic Acid Phenethyl Ester

Caffeic acid phenethyl ester is a potent and specific inhibitor of NF-κB activation, and also displays antioxidant, immunomodulatory and antiinflammatory activities.

S3137

Sodium salicylate

Sodium salicylate is used in medicine as an analgesic and antipyretic.

S3939

4'-Methoxyresveratrol

4-Methoxyresveratrol is a stibenoid found in the Chinese herb Gnetum cleistostachyum. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation.

S4798

Benfotiamine

Benfotiamine is a synthetic S-acyl derivative of thiamine (vitamin B1) and has been investigated for the treatment and prevention of Diabetic Nephropathy and Diabetes Mellitus, Type 2. Benfotiamine suppresses oxidative stress-induced NF-κB activation and prevents the bacterial endotoxin-induced inflammation.

S7672

Omaveloxolone (RTA-408)

Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.

S3998

(+)-α-Lipoic acid

R(+)-α-lipoic acid, a physiological form of thioctic acid, is a strong antioxidant that relieves diabetic neuropathic symptoms. It shows superior antioxidative effects to its racemate. α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation.

S5144

Neferine

Neferine, a natural component of Nelumbo nucifera, has antitumor efficiency in cancer. Neferine((-)-Neferine) is a unique bis-benzylisoquinoline alkaloid that possesses a number of therapeutic effects such as anti-cancer, anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.

S9208

Ginsenoside Rb3

Ginsenoside Rb3, extracted from the plant Panax ginseng, plays important roles in cardiovascular diseases, including myocardial ischemia-reperfusion (I/R) injury. Ginsenoside Rb3 (0.1-10 μM) is tested for inhibition of tumor necrosis factor-α (TNF)-induced nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) luciferase reporter activity using a human kidney 293T cell-based assay. Ginsenoside Rb3 shows the significant activity with an IC50 of 8.2 μM. Ginsenoside Rb3 also inhibits the induction of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) messenger Ribonucleic acid (mRNA) in a dose-dependent manner after HepG2 cells have been treated with TNF-α (10 ng/mL).

S3633

Pyrrolidinedithiocarbamate ammonium

Ammonium pyrrolidine dithiocarbamate (PDTC) is a potent nuclear factor-κB (NF-κB) inhibitor that inhibits IκB phosphorylation, blocks NF-κB translocation to the nucleus and reduces the expression of downstream cytokines.

S3816

Dehydroevodiamine

Dehydroevodiamine, a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.

S9244

8-O-acetyl shanzhiside methyl ester

8-O-acetyl shanzhiside methyl ester, isolated from the leaves of Lamiophlomis rotata Kudo, promotes angiogenesis, which leads to the improvement of functional outcome after stroke.8-O-Acetyl shanzhiside methyl ester can inhibts NF-κB

S8484

GSK2982772

GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase (RIPK1) inhibitor with the IC50 value of 16 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses.

S8642

GSK'963

GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase (RIPK1) with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.

S8261

GSK583

GSK583 is a highly potent and selective inhibitor of RIP2 kinase with an IC50 of 5 nM.

S2261

Andrographolide

Andrographolide is a labdane diterpenoid that is the main bioactive component of the medicinal plant Andrographis paniculata.

S2382

Evodiamine

Evodiamine (Isoevodiamine), an alkaloid extract from the fruit of Evodiae Fructus exhibits antitumor activities against the human tumor cells. It is shown to inhibit NF-kB activation through suppression of IkB kinase activity.

S4937

4'-Hydroxychalcone

4'-Hydroxychalcone, found in herbs and spices and tea, is a member of the class of compounds known as retrochalcones. It has diverse biological activities, inhibiting TNFα-induced NF-κB pathway activation in a dose-dependent manner and activating BMP signaling.

S9295

Dauricine

Dauricine, a plant metabolite isolated from the Asian vine Menispermum dauricum, plays a variety of biological roles in the human body, from inhibiting cancer cell growth to blocking cardiac transmembrane Na+, K+, and Ca2+ ion currents.Dauricine induces apoptosis, inhibits proliferation and invasion through inhibiting NF‐κB signaling pathway in colon cancer cells.

S5343

Vanillic acid

Vanillic acid is a flavoring agent which is also an intermediate in the production of vanillin from ferulic acid. Vanillic acid inhibits NF-κB activation. Anti-inflammatory, antibacterial, and chemopreventive effects.

S9193

Aristolochic acid A

Aristolochic acid A is a carcinogenic, mutagenic, and nephrotoxic agent extracted from the flowering plant family Aristolochiaceae.Aristolochic acid A significantly reduces both activator protein 1 (AP-1) and nuclear factor-κB (NF-κB) activities.

S2313

Indole-3-carbinol

Indole-3-carbinol is produced by the breakdown of the glucosinolate glucobrassicin, which can be found at relatively high levels in cruciferous vegetables. Indole-3-carbinol suppresses NF-κB and IκBα kinase activation.

S9040

Maslinic acid

Maslinic Acid, a Natural Triterpene, exerts a wide range of biological activities, i.e. antitumor, antidiabetic, antioxidant, cardioprotective, neuroprotective, antiparasitic and growth-stimulating. MA significantly suppresses the DNA-binding activity of NF-κB p65 in LPS-induced RAW 264.7 cells.

S7273

SC75741

SC75741 is a potent NF-κB inhibitor with EC50 of 200 nM.

S3760

Stachydrine hydrochloride

Stachydrine is isolated from seed husk and the pulp of the fruit of C. Leonurus, and many other Asian plants and fruits. It has potent anti-metastatic activity and cardioprotective effects. Stachydrine hydrochloride is the major active constituent of Herba Leonuri, which is a potential therapy for cardiovascular diseases. Stachydrine can inhibit the NF-κB signal pathway. Anti-hypertrophic activities.

S3770

Sodium Aescinate

Sodium aescinate (SA) is a widely-applied triterpene saponin product derived from horse chestnut seeds, possessing vasoactive and organ-protective activities with oral or injection administration in the clinic. Sodium aescinate is a triterpene saponin derived from Aesculus hippocastanum seeds, with anti-inflammatory and antioxidant activities. Sodium aescinate inhibits hepatocellular carcinoma growth by targeting CARMA3/NF-κB pathway.

S3771

Stachydrine

Stachydrine, also known as N,N-dimethylproline or proline betaine, is a quaternary ammonium derivative of proline that occurs widely in Medicago species. It is an osmoprotective compound found in urine. Stachydrine is a major constituent of Chinese herb leonurus heterophyllus sweet used to promote blood circulation and dispel blood stasis. Stachydrine can inhibit the NF-κB signal pathway.

S3773

Tyrosol

Tyrosol is an antioxidant that is naturally present in several foods such as wines and green tea and is present most abundantly in olives. Tyrosol is a derivative of phenethyl alcohol. Tyrosol attenuates pro-inflammatory cytokines from cultured astrocytes and NF-κB activation. Anti-oxidative and anti-inflammatory effects.

S8483

CBL0137 HCl (CBL-0137 HCl)

CBL0137(CBL-0137) activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex).

S9388

(+)-Praeruptorin A

Praeruptorin A is a coumarin compound naturally occurring in the roots of Peucedanum praeruptorum Dunn., a commonly used traditional Chinese medicine for the treatment of certain respiratory diseases and hypertension. (+)-Praeruptorin A is one of enantiomers that shows more potent relaxant effects than (−)-praeruptorin A in rat aorta rings and may be an activator of eNOS.

S2321

Magnolol

Magnolol is a bioactive lignin found in the bark of the Houpu magnolia (Magnolia officinalis) which shows antifungal properties. It can block TNF-α-induced NF-KB activation.

S3874

Curcumenol

Curcumenol, a sesquiterpene isolated from Curcuma zedoaria, is known to possess a variety of health and medicinal values which includes neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. It inhibits NF-κB activation by suppressing the nuclear translocation of the NF-κB p65 subunit and blocking IκBα phosphorylation and degradation.

S1825

Erdosteine

Erdosteine is a mucolytic which is used in treatment of excessive viscous mucus. Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation.

S3880

Schisantherin A

Schisantherin A, also known as Gomisin C, is a dibenzocyclooctadiene that exhibits anti-tussive, sedative, anti-inflammatory, anti-osteoporotic, neuroprotective, cognition enhancing, and cardioprotective activities. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.

S8341

TAK-243 (MLN7243)

TAK-243 (MLN7243) is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE) with an IC50 of 1 ± 0.2 nM in the UBCH10 E2 thioester assay. It has minimal inhibitory activity in a panel of kinase and receptor assays, as well as on human carbonic anhydrase type I and type II. TAK-243 (MLN7243) induces ER stress, abrogates NFκB pathway activation and promotes apoptosis.

S4763

4-Hydroxychalcone

4-Hydroxychalcone is a chalcone metabolite with diverse biological activities. It inhibits TNFα-induced NF-κB pathway activation in a dose-dependent manner and also activates BMP signaling.

S9106

Eleutheroside E

Eleutheroside E, a principal component of Eleutherococcus senticosus (ES), has anti-inflammatory effects by inhibiting NF-κB and protecting against myocardial infarction.

S3808

Mangiferin

Mangiferin is a bioactive compound that demonstrates many health perspectives and has been used to prepare medicinal and food supplements. Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50.

S2341

(-)-Parthenolide

(-)-Parthenolide, an inhibitor of the Nuclear Factor-κB Pathway, specifically depletes HDAC1 protein without affecting other class I/II HDACs; Also promotes the ubiquitination of MDM2 and activates p53 cellular functions.

S3604

Triptolide (PG490)

Triptolide is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein.

S3811

Ginsenoside Re

Ginsenoside Re (Ginsenoside B2), an extract from Panax notoginseng, is a major ginsenoside in ginseng and belongs to 20(S)-protopanaxatriol group. It has diverse in vitro and in vivo effects, including vasorelaxant, antioxidant, antihyperlipidemic, and angiogenic actions. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB.

S3138

Methylthiouracil

Methylthiouracil is an antithyroid preparation. Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.

S3899

Hederagenin

Hederagenin is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo.

S5453

Hyperoside

Hyperoside, a naturally occuring flavonoid compound, exerts multiple bioactivities, including myocardial protection, anti-redox, and anti-inflammatory activities.Hyperoside can inhibit activation of the NF-κB signaling pathway.

S3867

(E)-Cardamonin

Cardamonin is a naturally occurring chalcone with strong anti-inflammatory activity. It is a novel TRPA1 antagonist with IC50 of 454 nM and also a NF-kB inhibitor.

S3872

Guaiacol

Guaiacol is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a precursor to various flavorants, such as eugenoland vanillin. Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.

S4712

Diethylmaleate

Diethylmaleate is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NF-kB.

S9170

Engeletin

Engeletin, a bioactive flavonoid, has multiple biological activities such as anti-diabetic and anti-inflammatory effects. engeletin againsts LPS-stimulated endometritis in mice via negative regulation of pro-inflammatory mediators via the TLR4-regulated NF-κB pathway.

S3923

Ginsenoside Rg1

Ginsenoside Rg1, one of the major active components of ginseng, is identified as a protopanaxatriol-type and has pharmacological actions such as neuroprotective and anti-tumor effects on various cancer types. Ginsenoside Rg1 reduces cerebral Aβ levels and NF-κB nuclear translocation.

S3924

Ginsenoside Rb1

Ginsenoside Rb1 is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65.

Catalog No. Information Product Use Citations Product Validations
S3603

Betulinic acid

Betulinic acid, a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Betulinic acid acts as a new activator of NF-kB.Phase 1/2.

Catalog No. Information Product Use Citations Product Validations
S5804

N-Acetylcysteine amide

N-acetylcysteine amide is a membrane penetrating antioxidant with anti-inflamatory activity through regulation of activation of NF-κB and HIF-1α as well as modulation of ROS.

Catalog No. Information Product Use Citations Product Validations
S2371

Vanillylacetone

Vanillylacetone is similar in chemical structure to other flavor chemicals such as vanillin and eugenol and is used as a flavor additive in spice oils and in perfumery to introduce spicy aromas. Vanillylacetone (Zingerone) alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways. Zingerone acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells.