NF-κB

Phorbol 12-myristate 13-acetate (PMA) belongs to the phorbol ester group of natural products and is an activator of PKC, SphK, and NF-κB. Phorbol 12-myristate 13-acetate induces THP1 cell differentiation.

Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.

Specnuezhenide (Nuezhenide) significantly protects human neuroblastoma SH-SY5Y cells from 6-hydroxydopamine-induced neurotoxicity.Nuezhenide is the main inhibitory compound of fruits, it shows a clear inhibitory effect to the seeds of wheat and Chinese cabbage.

1. Sanggenon C (Sanggenone C) inhibits tumor cellular proteasomal activity and cell viability, via induction of cell cycle arrest and cell death , inhibiting the proteasome function. 2. Sanggenon C and O inhibited NO production and iNOS expression by suppressing NF-κB activity and IκBα activation; inhibited TNF-alpha -stimulated PMN-HSC adhesion and expression of VCAM-1 by suppressing the activation of NF-kappaB.

CBL0137 hydrochloride (Curaxin-137 hydrochloride) activates p53 and inhibits NF-kB (EC50: 0.37 0.47 μM) in the cell-based p53 and NF-kB reporter assays, respectively. It also suppresses histone chaperone FACT.

Kurarinone, a flavanoid derived from shrub Sophora flavescens,Kurarinone exhibits anti-tumor, estrogenic, and anti-inflammatory activities, it also shows strong inhibitory effect on immune responses. Kurarinone may ameliorate chronic inflammatory skin diseases through the suppression of pathogenic CD4(+) T-cell differentiation and the overall immune response.

Stachydrine Hydrochloride is an effective component that mainly extracted from the leaf of Leonurussibiricus.

Sodium Houttuyfonate (Houttuynin sodium bisulfite), the active compound of the Houttuynia plant, is mainly used for treating purulent skin infections, respiratory tract infections, including pneumonia in elderly patients, and chronic bronchitis.

Dihydroartemisinin (Artenimol) is a metabolite of artemisinin.

Sodium houttuyfonate is anti-pseudomonas agents, inhibits virulence-related motility of Pseudomonas.

Picroside II (Vanilloyl catalpol) is the main active ingredient in iridoid glycosides. It has antioxidant, anti-inflammatory, immune regulatory, anti-virus and other pharmacological activities.

Aucubin (Rhinanthin) is an iridoid glycoside with anti-inflammatory, anti-microbial, anti-algesic as well as anti-tumor activities.

Guaiacol (2-Methoxyphenol) is a precursor to various flavorants, such as eugenol and vanillin. Its derivatives are used medicinally as an expectorant, antiseptic, and local anesthetic. It also can be used as an indicator in chemical reactions that produce oxygen. When oxygen binds to it, the complex turns yellowish brown and absorbs light maximally at about 470 nm.

Triacetylresveratrol (Acetyl-trans-resveratrol) has anti-cancer activity,it inhibits the phosphorylation of STAT3 and NFκB, down-regulates Mcl-1, and up-regulates Bim and Puma in pancreatic cancer cells.

Diallyl disulfide has antitumor effect, the effect can be enhanced by miR-200b and miR-22.

Glucosamine (Chitosamine) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. Supplemental glucosamine may help to rebuild cartilage and treat arthritis.

Sarsasapogenin (Parigenin) is a steroidal sapogenin, that is the aglycosidic portion of a plant saponin. It is named after sarsaparilla (Smilax sp.), a family of climbing plants found in subtropical regions. It was one of the first sapogenins to be identified, and the first spirostan steroid to be identified as such.

Eleutheroside E has anti-inflammatory effects by inhibiting NF-κB activities. Eleutheroside E significantly decreases the inflammatory cell infiltration, pannus formation, cartilage damage, bone erosion of CIA mice, the generation of TNF-α and IL-6, the m

Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antidiarrhoeic, antilipolytic, antispasmodic and anti-tumor properties. Zingerone(Gingerone) alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways. Zingerone(Gingerone) acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells.

Vanillic Acid (Acide vanillique) is used as a condiment in food,which used in wine and vinegar. It is an intermediate in the production of vanillin from ferulic acid.

Bergenin (Bengenin) is a polyphenol, which is an effective antinarcotic agent with antioxidant action.

5-Aminosalicylic Acid (5-ASA) is an anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE.

Indole-3-carbinol (I3C), a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activation.

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

BI-69A11 ((E)-3-(1H-Benzo[d]imidazol-2-yl)-1-(6-chloro-2-hydroxy-4-phenylquinolin-3-yl)prop-2-en-1-one) is a dual AKT and NFkB pathway inhibitor. It enhances the susceptibility of colon cancer cells to mda-7/IL-24-induced growth inhibition by targeting Akt.

Chrysotoxine (Phenol, 4-[2-(3,4-dimethoxyphenyl)ethyl]-2,6-dimethoxy-) inhibits 6-hydroxydopamine induced apoptosis in SH-SY5Y cells via NF-κB modulation and mitochondria protection.

CHPG hydrochloride is a selective agonist of mGluR5.

Homobutein (3-O-Methylbutein) is a dual inhibitor of HDACs and NF-κB with IC50s of 190 and 38 μM. Homobutein is an iron chelator with anticancer, anti-inflammatory, antiparasite, and antioxidation activities.

GGTI 2147 decreased Rac1 activity, down-regulated p65 expression, and ameliorated OGD/R-induced neuronal apoptosis.

4-methoxylonchocarpin was isolated from the roots of Abrus precatorius as a potent anti-inflammatory compound. 4-methoxylonchocarpin inhibited NF-κB-activated TNF expression by inhibiting the binding of LPS to TLR4 in macrophages and suppressed TNBS-induced colitis in mice.

Methyl chlorogenate is isolated from Eriobotrya japonica which is the inhibitor of NFkappaB.

Cyclo(his-pro) is an endogenous cyclic dipeptide that exerts oxidative damage protection by selectively activating the transcription factor Nrf2 signalling pathway.

IKKγ NBD Inhibitory Peptide acetate is a NEMO-binding domain peptide (NBD peptide) acetate corresponding to the NEMO amino-terminal alpha-helical region. IKKγ NBD Inhibitory Peptide acetate is shown to block TNF-alpha-induced NF-kB activation.

OT-551 HCl is an NF-Κb inhibitor, a disubstituted hydroxylamine with antioxidant properties can be used for the treatment of cataracts and age-related macular degeneration and geographic atrophy (GA).

CLEFMA has anti-proliferative activity. CLEFMA inhibits tumor growth associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects.

Biricodar dicitrate (VX-710) is a potent MDR inhibitor with no anticancer activity and can be used to study prostate cancer.

SN50 acetate is a cell permeable inhibitor of NF-κB translocation.

Hydrangenol is a natural product and can be isolated from Hydrangea serrata leaves. Hydrangenol is an antiphotoaging compound with oral activity. Hydrangenol can reduce MMP and inflammatory cytokine expression and increase moisturizing factors and antioxidant genes level, result in preventing wrinkle formation.

Hentriacontane is a natural product.

CPS-11 (N-(Hydroxymethyl)thalidomide) is a Thalidomide analogue that has significant antitumor activity and exhibits a wider range of activity and highly potent effects on the MM (multiple myeloma) cell line.

HOIPIN-1 (JTP0819958) is a selective and potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) (IC50 >2.8 μM).HOIPIN-1 inhibits LUBAC-mediated NF-kB activation.

Edasalonexent (CAT-1004) is an orally available NF-κB inhibitor for the improvement of Duchenne muscular dystrophy.

DMAPT (Dimethylamino Parthenolide) is a water-soluble analogue of Parthenolide (PTL). It is an orally active NF-κB inhibitor with an LD50 of 1.7 μM on primary acute myeloid leukemia cells.

EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.

DHMEQ racemate is an NF-κB inhibitor. The activity of DHMEQ racemate is lower than (-)-DHMEQ.

LTβR-IN-1 is a potent and selective lymphin β receptor (LTβR) inhibitor. LTβR-IN-1 has a selective inhibitory effect on the nuclear translocation of p52 of TNF12A, and has no obvious effect on the nuclear translocation of p65 mediated by TNF-α receptor, but inhibits the nuclear translocation of p52 stimulated by TWEAK or Anti-LTβR. Translocation with IC50 of 10 μM. LTβR-IN-1 regulates the NF-kB signaling pathway through a ligand-independent manner.

CHPG sodium salt is a selective agonist of mGluR5 and activates the ERK and Akt signaling pathways. CHPG sodium salt can be used in studies about traumatic brain injury.

AP-1/NF-κB activation inhibitor 1 is a potent inhibitor of AP-1 and NF-κB mediated transcriptional activation ( IC 50 =1 μM), does not blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells [1].

Schisantherin A (Wuweizi ester-A) is a dibenzocyclooctadiene lignan isolated from the fruit of Schisandra sphenanthera, has been used as an antitussive, tonic, and sedative agent.

Ethyl gallate (gallic acid ethyl ester) obviously decreases cell proliferation in MDA-MB-231 and MCF-7 cells in a dose- and time-dependent manner, exhibits cytotoxicity in a dose-dependent manner. Ethyl gallate can inhibit the abilities of invasion of breast cancer in vitro by inhibiting the mRNA levels of MMP-9/MMP-2, phosphorylation of Akt and protein expression of NF-κB and inhibits hydrogen peroxide signaling, may represent an alternative class of vasopressors for use in septic shock. Also, Ethyl gallate suppresses proliferation and invasion in human breast cancer cells by modulating the PI3K/Akt pathway, which may contribute to inhibiting their downstream targets such as NF-κB p-65, Bcl-2/Bax, and mRNA levels of MMP-2 and MMP-9 in breast cancer cells, could be used as potential antioxidants with safe therapeutic application in cancer chemotherapy.