NF-κB

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1013 Bortezomib (PS-341) <1 mg/mL 76 mg/mL '<1 mg/mL
S2824 TPCA-1 <1 mg/mL 56 mg/mL ''<1 mg/mL
S4902 QNZ (EVP4593) <1 mg/mL 5 mg/mL <1 mg/mL
S1623 Acetylcysteine(N-acetylcysteine) 33 mg/mL 33 mg/mL ''''33 mg/mL
S1848 Curcumin <1 mg/mL 73 mg/mL ''<1 mg/mL
S3256 Tectochrysin -1 mg/mL 7 mg/mL ''-1 mg/mL
S3261 Myrislignan -1 mg/mL 100 mg/mL ''-1 mg/mL
S3299 Demethyleneberberine -1 mg/mL 3 mg/mL ''-1 mg/mL
S3293 Gardenoside -1 mg/mL 81 mg/mL ''-1 mg/mL
S0949 Cucurbitacin IIb ' mg/mL
S8587 Withaferin A <1 mg/mL 94 mg/mL ''4 mg/mL
S0507 CBL0137 <1 mg/mL 15 mg/mL '''8 mg/mL
S6671 SN50 100 mg/mL 100 mg/mL 100 mg/mL
S8941 NIK SMI1 <1 mg/mL 73 mg/mL '<1 mg/mL
S6714 INH14 <1 mg/mL 48 mg/mL 18 mg/mL
S4073 Sodium 4-Aminosalicylate 42 mg/mL 42 mg/mL <1 mg/mL
S7351 JSH-23 <1 mg/mL 48 mg/mL 20 mg/mL
S1576 Sulfasalazine <1 mg/mL 80 mg/mL ''''<1 mg/mL
S7414 Caffeic Acid Phenethyl Ester <1 mg/mL 57 mg/mL 57 mg/mL
S3137 Sodium salicylate 32 mg/mL 32 mg/mL <1 mg/mL
S3939 4'-Methoxyresveratrol <1 mg/mL 48 mg/mL 48 mg/mL
S4798 Benfotiamine <1 mg/mL 0.01 mg/mL '<1 mg/mL
S8279 Shikonin <1 mg/mL 57 mg/mL 23 mg/mL
S7672 Omaveloxolone (RTA-408) <1 mg/mL 100 mg/mL '''20 mg/mL
S3998 (+)-α-Lipoic acid -1 mg/mL 41 mg/mL -1 mg/mL
S5144 Neferine -1 mg/mL 100 mg/mL -1 mg/mL
S9208 Ginsenoside Rb3 -1 mg/mL 100 mg/mL -1 mg/mL
S3633 Pyrrolidinedithiocarbamate ammonium 32 mg/mL 32 mg/mL 32 mg/mL
S9244 8-O-acetyl shanzhiside methyl ester -1 mg/mL 90 mg/mL -1 mg/mL
S8642 GSK'963 <1 mg/mL 46 mg/mL ''46 mg/mL
S2261 Andrographolide <1 mg/mL 70 mg/mL <1 mg/mL
S2382 Evodiamine <1 mg/mL <1 mg/mL <1 mg/mL
S4937 4'-Hydroxychalcone -1 mg/mL 44 mg/mL -1 mg/mL
S9295 Dauricine -1 mg/mL 100 mg/mL -1 mg/mL
S5343 Vanillic acid -1 mg/mL 33 mg/mL -1 mg/mL
S2290 Dihydroartemisinin (DHA) <1 mg/mL 56 mg/mL 11 mg/mL
S9193 Aristolochic acid A -1 mg/mL 6 mg/mL -1 mg/mL
S7445 E3330 <1 mg/mL 75 mg/mL '75 mg/mL
S2313 Indole-3-carbinol 7 mg/mL 29 mg/mL 29 mg/mL
S9040 Maslinic acid -1 mg/mL 95 mg/mL -1 mg/mL
S7273 SC75741 <1 mg/mL 35 mg/mL '<1 mg/mL
S3760 Stachydrine hydrochloride -1 mg/mL 35 mg/mL -1 mg/mL
S3770 Sodium Aescinate -1 mg/mL 10 mg/mL -1 mg/mL
S3771 Stachydrine -1 mg/mL 28 mg/mL -1 mg/mL
S3773 Tyrosol -1 mg/mL 27 mg/mL -1 mg/mL
S8483 CBL0137 HCl (CBL-0137 HCl) 24 mg/mL 38 mg/mL '<1 mg/mL
S9374 2',5'-Dihydroxyacetophenone -1 mg/mL 30 mg/mL ''-1 mg/mL
S9388 (+)-Praeruptorin A -1 mg/mL 77 mg/mL -1 mg/mL
S9075 Mulberroside A -1 mg/mL 100 mg/mL -1 mg/mL
S2321 Magnolol <1 mg/mL 53 mg/mL 53 mg/mL
S7637 DTP3 100 mg/mL 100 mg/mL ''100 mg/mL
S3874 Curcumenol -1 mg/mL 46 mg/mL -1 mg/mL
S1825 Erdosteine <1 mg/mL 50 mg/mL 10 mg/mL
S3880 Schisantherin A -1 mg/mL 100 mg/mL -1 mg/mL
S8341 TAK-243 (MLN7243) <1 mg/mL 100 mg/mL '25 mg/mL
S9417 Homoplantaginin -1 mg/mL 92 mg/mL -1 mg/mL
S4763 4-Hydroxychalcone -1 mg/mL 44 mg/mL '-1 mg/mL
S9106 Eleutheroside E -1 mg/mL 100 mg/mL -1 mg/mL
S3808 Mangiferin -1 mg/mL 84 mg/mL -1 mg/mL
S5579 Chelidonic acid -1 mg/mL 4 mg/mL -1 mg/mL
S2341 (-)-Parthenolide <1 mg/mL 49 mg/mL 49 mg/mL
S3604 Triptolide (PG490) <1 mg/mL 72 mg/mL <1 mg/mL
S3607 Sarsasapogenin <1 mg/mL <1 mg/mL 5 mg/mL
S3811 Ginsenoside Re -1 mg/mL 100 mg/mL -1 mg/mL
S3138 Methylthiouracil <1 mg/mL 28 mg/mL '''<1 mg/mL
S3899 Hederagenin -1 mg/mL 94 mg/mL -1 mg/mL
S9502 Madecassic acid -1 mg/mL 100 mg/mL -1 mg/mL
S5453 Hyperoside 1 mg/mL 92 mg/mL 1 mg/mL
S3867 (E)-Cardamonin -1 mg/mL 54 mg/mL -1 mg/mL
S3872 Guaiacol -1 mg/mL 24 mg/mL -1 mg/mL
S4712 Diethylmaleate ' mg/mL
S9170 Engeletin -1 mg/mL 86 mg/mL -1 mg/mL
S3923 Ginsenoside Rg1 -1 mg/mL 100 mg/mL -1 mg/mL
S3924 Ginsenoside Rb1 -1 mg/mL 100 mg/mL -1 mg/mL
S3223 L-Quebrachitol -1 mg/mL 100 mg/mL '''-1 mg/mL
S3603 Betulinic acid <1 mg/mL 20 mg/mL 10 mg/mL
S3298 Caulophylline (N-Methylcytisine) -1 mg/mL 100 mg/mL ''-1 mg/mL
S5804 N-Acetylcysteine amide 32 mg/mL 32 mg/mL ''13 mg/mL
S9184 Forsythoside B -1 mg/mL 100 mg/mL -1 mg/mL
S2371 Vanillylacetone 10 mg/mL 38 mg/mL 38 mg/mL

NF-κB製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1013

Bortezomib (PS-341)

Bortezomib (PS-341, LDP-341, MLM341) 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.

S2824

TPCA-1

TPCA-1 is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1. TPCA-1 is also an inhibitor of STAT3 and enhances apoptosis.

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,NAC) 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 (Diferuloylmethane) 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 (HDAC); activates Nrf2 pathway and supresses the activation of transcription factor NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.

S3256

Tectochrysin

Tectochrysin (Techtochrysin, NSC 80687) is one of the major flavonoids of Alpinia oxyphylla Miquel. Tectochrysin significantly increases the expression of DR3, DR4 and Fas and inhibits activity of NF-κB. Tectochrysin induces apoptotic cell death.

S3261

Myrislignan

Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan inhibits interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α). Myrislignan significantly inhibits the expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) dose-dependently in LPS-stimulated macrophage cells. Myrislignan inhibits the NF-κB signalling pathway activation.

S3299

Demethyleneberberine

Demethyleneberberine (DMB), a component of Cortex Phellodendri Chinensis (CPC), significantly alleviates the weight loss and diminishes myeloperoxidase (MPO) activity, while significantly reduces the production of pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), and inhibits the activation of NF-κB signaling pathway. Demethyleneberberine (DMB) potentially ameliorates NAFLD (Non-alcoholic fatty liver disease) by activating AMPK pathways.

S3293

Gardenoside

Gardenoside is a natural compound extracted from Gardenia fruits, with hepatoprotective properties. Gardenoside inhibits TNF-α, IL-1β, IL-6 and NFκB activation. Gardenoside also has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. Gardenoside suppresses the pain in rats model of chronic constriction injury by regulating the P2X3 and P2X7 receptors.

S0949

Cucurbitacin IIb

Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis.

S8587

Withaferin A

Withaferin A potently inhibits NF-κB activation by preventing the tumor necrosis factor-induced activation of IκB kinase β via a thioalkylation-sensitive redox mechanism. Withaferin A binds to the intermediate filament (IF) protein, vimentin with antitumor and antiangiogenesis activity. Withaferin A is a steroidal lactone isolated from Withania somnifera.

S0507

CBL0137

CBL0137 is an inhibitor of the histone chaperone FACT (facilitates chromatin transcription) that simultaneously suppresses NF-κB and activates p53 with EC50 of 0.47 μM and 0.37 μM, respectively.

S6671

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.

S8941

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.

S6714

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.

S4073

Sodium 4-Aminosalicylate

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

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.

S1576

Sulfasalazine

Sulfasalazine (Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.

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.

S4798

Benfotiamine

Benfotiamine (S-Benzoylthiamine O-monophosphate) 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.

S8279

Shikonin

Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.

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.

S5144

Neferine

Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine induces autophagy-dependent cell death in apoptosis-resistant cancers. Neferine possesses a number of therapeutic effects such as 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 (DHED), 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.

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.

S8642

GSK'963

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

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.

S5771

sulforaphane

Sulforaphane is a naturally occurring isothiocyanate derived from the consumption of cruciferous vegetables, such as broccoli, cabbage, and kale. It is an inducer of Nrf2. Sulforaphane is also an inhibitor of histone deacetylase (HDAC) and NF-κB. Sulforaphane increases heme oxygenase-1 (HO-1) and reduces the levels of reactive oxygen species (ROS). Sulforaphane induces cell cycle arrest and apoptosis.

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.

S5343

Vanillic acid

Vanillic acid (4-hydroxy-3-methoxybenzoic acid) is a flavoring agent which is also an intermediate in the production of vanillin from ferulic acid.

S2290

Dihydroartemisinin (DHA)

Dihydroartemisinin (DHA) is a semi-synthetic derivative of artemisinin and isolated from the traditional Chinese herb Artemisia annua. Dihydroartemisinin induces autophagy and apoptosis by suppressing NF-κB activation.

S9193

Aristolochic acid A

Aristolochic acid A is a carcinogenic, mutagenic, and nephrotoxic agent extracted from the flowering plant family Aristolochiaceae.

S7445

E3330

E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.

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.

S7273

SC75741

SC75741 is a potent NF-κB inhibitor with EC50 of 200 nM. SC75741 efficiently blocks influenza virus propagation.

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.

S3770

Sodium Aescinate

Sodium Aescinate (SA, Escin Sodium Salt) 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.

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.

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.

S8483

CBL0137 HCl (CBL-0137 HCl)

CBL0137 (Curaxin 137) 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).

S9374

2',5'-Dihydroxyacetophenone

2',5'-Dihydroxyacetophenone is a mixture of dihydroxyacetophenone isomers is used in food flavouring. 2',5'-Dihydroxyacetophenone significantly inhibits NO production via the suppression of iNOS expression. 2',5'-Dihydroxyacetophenone significantly decreases levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways.

S3871

Muscone

Muscone, a flavouring ingredient, is an organic compound that is the primary contributor to the odor of musk and also a potent anti-inflammatory agent. Muscone significantly downregulats the levels of LPS-induced inflammatory cytokines and inhibits NF-κB and NLRP3 inflammasome activation in BMDMs. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6).

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.

S9075

Mulberroside A

Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.

S2321

Magnolol

Magnolol (NSC 293099) 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.

S7637

DTP3

DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway.

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.

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.

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.

S9417

Homoplantaginin

Homoplantaginin, a main flavonoid from a traditional Chinese medicine Salvia plebeia, has anti-inflammatory and anti-oxidant properties. Homoplantaginin inhibits TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.

S4763

4-Hydroxychalcone

4-Hydroxychalcone (P-Cinnamoylphenol) 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.

S5579

Chelidonic acid

Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) is a secondary metabolite found in several plants with therapeutic potential in allergic disorders in experimental animals. Chelidonic acid inhibits IL-6 production by blocking NF-κB and caspase-1 in HMC-1 cells. Chelidonic acid is also an inhibitor of glutamate decarboxylase with Ki of 1.2 μM.

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 (PG490) 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. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway.

S3607

Sarsasapogenin

Sarsasapogenin (SAR) is a steroidal sapogenin. It can provoke the generation of reactive oxygen species and activate unfolded protein response (UPR) signaling pathways. SAR potently inhibits NF-κB and MAPK activation, as well as IRAK1, TAK1, and IκBα phosphorylation in LPS-stimulated macrophages.

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 (NSC-193526, NSC-9378) 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 (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) 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.

S9502

Madecassic acid

Madecassic acid, a natural triterpene first isolated from C. asiatica, has diverse anti-inflammatory and anti-diabetic effects, blocking NF-κB activation in macrophages and causing by iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 inhibition.

S5453

Hyperoside

Hyperoside (Hyperin, Quercetin 3-galactoside), a naturally occuring flavonoid compound, exerts multiple bioactivities, including myocardial protection, anti-redox, and anti-inflammatory activities.

S3867

(E)-Cardamonin

(E)-Cardamonin (Alpinetin chalcone, cardamomin) 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 (O-methoxyphenol, 2-hydroxyanisole, O-methylcatechol) 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.

S4712

Diethylmaleate

Diethylmaleate (Diethyl ester, Maleic acid diethyl ester) 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.

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 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions.

S3223

L-Quebrachitol

L-Quebrachitol (L-QCT), a natural product isolated from many plants, promotes proliferation and cell DNA synthesis. L-Quebrachitol upregulates bone morphogenetic protein-2 (BMP-2) and runt-related transcription factor-2 (Runx2) and regulatory genes associated with mitogen-activated protein kinase (MAPK) and Wnt/β-catenin signaling pathway, while down-regulating the receptor activator of the nuclear factor-κB(NF-κB) ligand (RANKL) mRNA level.

S3603

Betulinic acid

Betulinic acid (ALS-357), 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.

S3298

Caulophylline (N-Methylcytisine)

Caulophylline (N-Methylcytisine, Caulophyllin, NMC) is a tricyclic quinolizidine alkaloid with anti-inflammatory activities. Caulophylline binds to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia with Kd of 50 nM. Caulophylline significantly reduces myeloperoxidase (MPO) activity, blocks the activation of NF-κB by inhibiting IκB and IKK phosphorylation.

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.

S9184

Forsythoside B

Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant. Forsythoside B has potent neuroprotective effects and has anti-inflammation, antioxidant, and antisepsis properties. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.

S2371

Vanillylacetone

Vanillylacetone (NSC 15335) 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.

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S1013

Bortezomib (PS-341)

Bortezomib (PS-341, LDP-341, MLM341) 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.

S2824

TPCA-1

TPCA-1 is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1. TPCA-1 is also an inhibitor of STAT3 and enhances apoptosis.

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,NAC) 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 (Diferuloylmethane) 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 (HDAC); activates Nrf2 pathway and supresses the activation of transcription factor NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.

S3256

Tectochrysin

Tectochrysin (Techtochrysin, NSC 80687) is one of the major flavonoids of Alpinia oxyphylla Miquel. Tectochrysin significantly increases the expression of DR3, DR4 and Fas and inhibits activity of NF-κB. Tectochrysin induces apoptotic cell death.

S3261

Myrislignan

Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan inhibits interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α). Myrislignan significantly inhibits the expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) dose-dependently in LPS-stimulated macrophage cells. Myrislignan inhibits the NF-κB signalling pathway activation.

S3299

Demethyleneberberine

Demethyleneberberine (DMB), a component of Cortex Phellodendri Chinensis (CPC), significantly alleviates the weight loss and diminishes myeloperoxidase (MPO) activity, while significantly reduces the production of pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), and inhibits the activation of NF-κB signaling pathway. Demethyleneberberine (DMB) potentially ameliorates NAFLD (Non-alcoholic fatty liver disease) by activating AMPK pathways.

S3293

Gardenoside

Gardenoside is a natural compound extracted from Gardenia fruits, with hepatoprotective properties. Gardenoside inhibits TNF-α, IL-1β, IL-6 and NFκB activation. Gardenoside also has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. Gardenoside suppresses the pain in rats model of chronic constriction injury by regulating the P2X3 and P2X7 receptors.

S0949

Cucurbitacin IIb

Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis.

S8587

Withaferin A

Withaferin A potently inhibits NF-κB activation by preventing the tumor necrosis factor-induced activation of IκB kinase β via a thioalkylation-sensitive redox mechanism. Withaferin A binds to the intermediate filament (IF) protein, vimentin with antitumor and antiangiogenesis activity. Withaferin A is a steroidal lactone isolated from Withania somnifera.

S0507

CBL0137

CBL0137 is an inhibitor of the histone chaperone FACT (facilitates chromatin transcription) that simultaneously suppresses NF-κB and activates p53 with EC50 of 0.47 μM and 0.37 μM, respectively.

S6671

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.

S8941

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.

S6714

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.

S4073

Sodium 4-Aminosalicylate

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

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.

S1576

Sulfasalazine

Sulfasalazine (Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.

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.

S4798

Benfotiamine

Benfotiamine (S-Benzoylthiamine O-monophosphate) 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.

S8279

Shikonin

Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.

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.

S5144

Neferine

Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine induces autophagy-dependent cell death in apoptosis-resistant cancers. Neferine possesses a number of therapeutic effects such as 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 (DHED), 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.

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.

S8642

GSK'963

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

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.

S5771

sulforaphane

Sulforaphane is a naturally occurring isothiocyanate derived from the consumption of cruciferous vegetables, such as broccoli, cabbage, and kale. It is an inducer of Nrf2. Sulforaphane is also an inhibitor of histone deacetylase (HDAC) and NF-κB. Sulforaphane increases heme oxygenase-1 (HO-1) and reduces the levels of reactive oxygen species (ROS). Sulforaphane induces cell cycle arrest and apoptosis.

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.

S5343

Vanillic acid

Vanillic acid (4-hydroxy-3-methoxybenzoic acid) is a flavoring agent which is also an intermediate in the production of vanillin from ferulic acid.

S2290

Dihydroartemisinin (DHA)

Dihydroartemisinin (DHA) is a semi-synthetic derivative of artemisinin and isolated from the traditional Chinese herb Artemisia annua. Dihydroartemisinin induces autophagy and apoptosis by suppressing NF-κB activation.

S9193

Aristolochic acid A

Aristolochic acid A is a carcinogenic, mutagenic, and nephrotoxic agent extracted from the flowering plant family Aristolochiaceae.

S7445

E3330

E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.

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.

S7273

SC75741

SC75741 is a potent NF-κB inhibitor with EC50 of 200 nM. SC75741 efficiently blocks influenza virus propagation.

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.

S3770

Sodium Aescinate

Sodium Aescinate (SA, Escin Sodium Salt) 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.

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.

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.

S8483

CBL0137 HCl (CBL-0137 HCl)

CBL0137 (Curaxin 137) 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).

S9374

2',5'-Dihydroxyacetophenone

2',5'-Dihydroxyacetophenone is a mixture of dihydroxyacetophenone isomers is used in food flavouring. 2',5'-Dihydroxyacetophenone significantly inhibits NO production via the suppression of iNOS expression. 2',5'-Dihydroxyacetophenone significantly decreases levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways.

S3871

Muscone

Muscone, a flavouring ingredient, is an organic compound that is the primary contributor to the odor of musk and also a potent anti-inflammatory agent. Muscone significantly downregulats the levels of LPS-induced inflammatory cytokines and inhibits NF-κB and NLRP3 inflammasome activation in BMDMs. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6).

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.

S9075

Mulberroside A

Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.

S2321

Magnolol

Magnolol (NSC 293099) 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.

S7637

DTP3

DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway.

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.

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.

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.

S9417

Homoplantaginin

Homoplantaginin, a main flavonoid from a traditional Chinese medicine Salvia plebeia, has anti-inflammatory and anti-oxidant properties. Homoplantaginin inhibits TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.

S4763

4-Hydroxychalcone

4-Hydroxychalcone (P-Cinnamoylphenol) 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.

S5579

Chelidonic acid

Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) is a secondary metabolite found in several plants with therapeutic potential in allergic disorders in experimental animals. Chelidonic acid inhibits IL-6 production by blocking NF-κB and caspase-1 in HMC-1 cells. Chelidonic acid is also an inhibitor of glutamate decarboxylase with Ki of 1.2 μM.

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 (PG490) 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. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway.

S3607

Sarsasapogenin

Sarsasapogenin (SAR) is a steroidal sapogenin. It can provoke the generation of reactive oxygen species and activate unfolded protein response (UPR) signaling pathways. SAR potently inhibits NF-κB and MAPK activation, as well as IRAK1, TAK1, and IκBα phosphorylation in LPS-stimulated macrophages.

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 (NSC-193526, NSC-9378) 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 (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) 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.

S9502

Madecassic acid

Madecassic acid, a natural triterpene first isolated from C. asiatica, has diverse anti-inflammatory and anti-diabetic effects, blocking NF-κB activation in macrophages and causing by iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 inhibition.

S5453

Hyperoside

Hyperoside (Hyperin, Quercetin 3-galactoside), a naturally occuring flavonoid compound, exerts multiple bioactivities, including myocardial protection, anti-redox, and anti-inflammatory activities.

S3867

(E)-Cardamonin

(E)-Cardamonin (Alpinetin chalcone, cardamomin) 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 (O-methoxyphenol, 2-hydroxyanisole, O-methylcatechol) 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.

S4712

Diethylmaleate

Diethylmaleate (Diethyl ester, Maleic acid diethyl ester) 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.

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 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions.

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S3223

L-Quebrachitol

L-Quebrachitol (L-QCT), a natural product isolated from many plants, promotes proliferation and cell DNA synthesis. L-Quebrachitol upregulates bone morphogenetic protein-2 (BMP-2) and runt-related transcription factor-2 (Runx2) and regulatory genes associated with mitogen-activated protein kinase (MAPK) and Wnt/β-catenin signaling pathway, while down-regulating the receptor activator of the nuclear factor-κB(NF-κB) ligand (RANKL) mRNA level.

S3603

Betulinic acid

Betulinic acid (ALS-357), 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.

2020, 873:172981

2020, 10.1093/abbs/gmz148

2020, 1467(1):77-93

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S3298

Caulophylline (N-Methylcytisine)

Caulophylline (N-Methylcytisine, Caulophyllin, NMC) is a tricyclic quinolizidine alkaloid with anti-inflammatory activities. Caulophylline binds to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia with Kd of 50 nM. Caulophylline significantly reduces myeloperoxidase (MPO) activity, blocks the activation of NF-κB by inhibiting IκB and IKK phosphorylation.

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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.

2020, 121:105703

2019, 19(2):258-265

2019, 508(4):1271-1278

S9184

Forsythoside B

Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant. Forsythoside B has potent neuroprotective effects and has anti-inflammation, antioxidant, and antisepsis properties. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.

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S2371

Vanillylacetone

Vanillylacetone (NSC 15335) 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.