nf-?b

AP-1 NF-κB activation inhibitor 1 is a potent inhibitor of AP-1 and NF-κB mediated transcriptional activation (IC50 = 1 μM), without blocking basal transcription driven by the β-actin promoter. It has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells [1].

BOT-64 is an IKK-2 inhibitor which targets the Ser177 and or Ser181 residues in the kinase's activation loop domain.BOT-64 is a cell-permeable benzoxathiole compound

NF-κB-IN-1 (1,6-Heptadiene-3,5-dione, 1,7-bis(3,4-dimethoxyphenyl)-4-[(4-hydroxy-3-methoxyphenyl)methylene]-, (1E,6E)-) is a potent NF-κB signaling pathway inhibitor. It is a 4-arylidene crucumin analogue. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells.

The NF-κB Activation Inhibitor III, controls the biological activity of NF-κB. It is primarily used for Inflammation/Immunology applications.

NF-κB-IN-9, a nuclear factor kappa B (NF-κB) targeting sonosensitizer with excitation and emission wavelengths (λex/λem) of 489/628 nm, features dual resveratrol units that strongly inhibit NF-κB signaling. This compound demonstrates notable anti-tumor properties and pronounced sonocytotoxicity against cancer cells, maintaining biosafety in xenograft mouse models.

NF-κB-IN-2 inhibits canonical NF-κB signaling induced by TNF-α in PC-3 cells.

NF-κB PON1-IN-1 (Compound 16) is an inhibitor of the NF-κB PON1 pathway, exhibiting antioxidant activity (IC50: 45.76 μM) and hepatoprotective properties.

Akt NF-κB MAPK-IN-1 (compound 2m) is a potent, orally active inhibitor of NO with an IC50 of 7.70 μM and low toxicity, exhibiting anti-inflammatory effects by blocking the Akt NF-κB and MAPK signaling pathways [1].

NF-κB-IN-10 (compound E1) is an NF-κB inhibitor that mitigates heart failure symptoms by modulating the Nrf2 NF-κB signaling pathway, alleviating oxidative stress and inflammation. It suppresses LPS-induced NO production and downregulates iNOS and COX-2 expression in RAW264.7 cells, showing potential for cardiovascular disease research [1].

NF-κB-IN-8 is a competitive antagonist of LPS for MD-2 binding, and it impedes the expression of inflammatory factors by engaging MD-2. Additionally, it inhibits ALP activity and is usable in inflammation research, including acute lung injury (ALI) [1].

NF-κB-IN-4 (compound 17) is a potent inhibitor of the NF-κB pathway that can cross the blood-brain barrier (BBB). It exhibits potential anti-neuroinflammatory activity with low toxicity, making it suitable for researching neuroinflammation-related diseases. NF-κB-IN-4 can block IκBα activation and phosphorylation, reduce NLRP3 expression, and thereby inhibit NF-κB activation [1].

TLR4 NF-κB MAPK-IN-1 is a novel antineuroinflammatory agent inhibiting the TLR4 NF-κB MAPK pathways.

NF-κB-IN-13 (compound 12) significantly inhibits LPS-induced NF-κB activation and NO synthesis in RAW264.7 macrophages, demonstrating anti-inflammatory properties [1].

NF-κB-IN-5 (compound 4d) is an orally active NF-κB inhibitor that interacts directly with NF-κB, and exhibits antitumor activity against human cancer cell lines, with IC50 values of 5.35, 2.81, 2.83, 2.02, and 3.90 μM for HCT116, U87-MG, HepG2, BGC823, and PC9, respectively.

NF-κB/MAPK-IN-1 is a potent dual inhibitor of the NF-κB and MAPK pathways with potential anti-inflammatory activity, inhibition of NO production, and inhibition of LPS-induced activation of iNOS, COX-2, ERΚ and P38. NF-κB/MAPK-IN-1 is used for the prevention and treatment of rheumatoid arthritis (RA).

Akt NF-κB JNK-IN-1 (Compound 2i) is an inhibitor of the Akt, NF-κB, and JNK signaling pathways, demonstrating inhibition of nitric oxide production (IC50: 3.15 μM) and exhibiting anti-inflammatory effects.

NF-κB-IN-12 (compound 3h) is a potent NF-κB inhibitor with an IC50 of 1.02 μM, suitable for research in acute lung injury [1].

NF-κB-IN-11 (Compound 3i) is an inhibitor of NF-κB, effectively blocking TNF-α-induced NF-κB pathway activation and nuclear translocation of NF-κB, alongside reducing expression levels of phospho-IKK, IκBα, and NF-κB p65. Demonstrating anti-inflammatory properties, it mitigates dextran sulfate sodium-induced colitis in mice and exhibits a maximum tolerated dose (MTD) exceeding 1852 mg kg in acute toxicity assays when administered orally (p.o.) [1].

NF-κB-IN-6 (Compound 3d) is an anti-inflammatory agent that suppresses the NF-κB signaling pathway, thereby reducing iNOS and COX-2 protein expression. It inhibits NO production in LPS-induced RAW264.7 cells with an IC50 of 23.1 μM[1].

NF-κB-IN-3 (Compound 2) is an NF-κB inhibitor with an IC50 of 0.70 μM, and it can be used as an anti-tumour agent.

Dihydroartemisinin (Artenimol) is a metabolite of artemisinin.

Oxaprozin (Oxaprozinum) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of oxaprozin is as a Cyclooxygenase Inhibitor. The chemical classification of oxaprozin is Nonsteroidal Anti-inflammatory Compounds.

Caffeic Acid Phenethyl Ester (Phenylethyl Caffeate) (CAPE) inhibits the activation of nuclear transcription factor NF-kappa B and may suppress p70S6K and Akt-driven signaling pathways, with antineoplastic, cytoprotective and immunomodulating activities. CAPE is the phenethyl alcohol ester of caffeic acid and a bioactive component of honeybee hive propolis. In addition, CAPE inhibits PDGF-induced proliferation of vascular smooth muscle cells through the activation of p38 mitogen-activated protein kinase (MAPK) and hypoxia-inducible factor (HIF)-1alpha and subsequent induction of heme oxygenase-1 (HO-1).

Baicalin (Baicalein 7-O-β-D-glucuronide) is a prolyl endopeptidase inhibitor isolated from scutellaria baicalensis, with antioxidant, anti-tumor, anti-HIV properties.

Ginsenoside Re (Ginsenoside B2) may have properties that inhibit or prevent the growth of tumors.

Urolithin B is one of the gut microbial metabolites of ellagitannins and is found in diverse plant foods, including pomegranates, berries, walnuts, tropical fruits, and medicinal herbs. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. Urolithin B has anti-inflammatory and antioxidant effects.

(-)-Bornyl acetate (L-(-)-Bornyl acetate) is a less active enantiomer of (+)-Bornyl acetate. Isolated from hyssop oil, it possesses antifungal, highly active whitening, and antioxidant properties, and it has potential applications in cosmeceutical materials. It downregulates proinflammatory cytokines in vitro and in vivo, reduces the number of total cells, neutrophils, and macrophages in BALF, attenuates histologic lung alterations, decreases the wet-to-dry weight ratio in BALF, and inhibits the activation of NF-kappa-B inhibitor alpha, extracellular regulated protein kinases, c-JunN-terminal kinase, and p38 mitogen-activated protein kinase.

Cecropin B acetate induces NF-κB activation and suppresses CYP3A29 by disrupting the association of the PXR/retinoid X receptor alpha (RXR-α) complex with DNA sequences. Cecropin B acetate exhibits strong antimicrobial activity.

β-NF-JQ1 is a PROTAC that recruits aryl hydrocarbon receptor E3 (AhR E3) ligase to target proteins. Using β-NF as an AhR ligand, it targets bromodomain (BRD)-containing proteins and induces AhR and BRD protein interactions. β-NF-JQ1 exhibits potent anticancer activity associated with protein knockdown activity.

Polygalasaponin F has anti-neuroinflammatory activity, can inhibit the release of inflammatory cytokines TNF-α and NO induced by lipopolysaccharides (LPS) and reduce the expression of inducible nitric oxide synthases. Polygalasaponin F can significantly i

1. Flavokawain B (Flavokavain B) has potent anti-inflammatory activity, can significantly inhibit production of NO and PGE2 in LPS-induced RAW 264.7 cells. 2. Flavokawain B, the hepatotoxic constituent from kava root, induces GSH-sensitive oxidative stress through modulation of IKK/NF-κB and MAPK signaling pathways. 3. Flavokawain B induces apoptosis, has the potential usefulness of FKB for prevention and treatment of hormone-refractory prostate cancer in an adjuvant setting. 4. Flavokawain B acts through ROS generation and GADD153 up-regulation to regulate the expression of Bcl-2 family members, thereby inducing mitochondrial dysfunction and apoptosis in HCT116 cells.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

1. ISOGINKGETIN (4',4'''-Dimethylamentoflavone), a compound derived from the leaves of Ginkgo biloba, to up-regulate adiponectin secretion with potency comparable to that of rosiglitazone, a known modulator of adiponectin production. 2. Isoginkgetin has anti-tumor activity, the mechanistic basis is splicing inhibition , thus, pre-mRNA splicing inhibitors may represent a novel avenue for development of new anti-cancer agents.3. Isoginkgetin can inhibit tumor cell invasion by regulating phosphatidylinositol 3-kinase/Akt-dependent matrix metalloproteinase-9 expression. 4. Isoginkgetin (0.3mg/kg ip for 3d) can reduce the level of O2·- in plasma and erythroeyte and sometimes increase the activity of SOD in anoxic rats, the action being stronger than aspirin.

Tizoxanide (Desacetyl-nitazoxanide) is a metabolite of lamivudine. Lamivudine (2', 3'-dideoxy-3'-thiacytidine, commonly called 3TC) is a potent nucleoside analog reverse transcriptase inhibitor (nRTI).

Maslinic acid (Crategolic acid) is a DNA polymerase B inhibitor.

CU-CPT9b (TLR8-specific antagonist 1) is an antagonist of toll-like receptor 8 (TLR8; Kd = 21 nM). It inhibits activation of NF- B induced by the TLR8 agonist R-848 in TLR8-overexpressing HEK-Blue cells with an IC50 value of 0.7 nM.

11-Keto-beta-boswellic acid, a novel Nrf2 activator, and a selective 5-lipoxygenase (5-LOX) inhibitor; it exerts dose dependent cardioprotective effect manifested by dose-dependent reduction in serum lactate dehydrogenase

Dri-c21045 showed concentration-dependent inhibition of NF- B activation and all CD40L induced by B cell proliferation. IC50 was 17.1 M and 4.5 M, respectively.Dri-c21045 is an effective selective inhibitor of CD40-CD40L synergistic stimulator protein-pro

1. β,β-Dimethylacrylshikonin (Dimethylacrylshikonin) is a promising agent for developing an improved strategy for radiotherapy against tumors. (a) Injection of Dimethylacrylshikonin combined with IR treatment significantly suppressed tumor growth of the HCT-116 xenograft. (b) Dimethylacrylshikonin significantly suppressed the growth of H(22) transplantable hepatoma, and induced the activation of caspase-3 . (c) Dimethylacrylshikonin inhibited growth of gastric cancer SGC-791 cells by inducing ERK signaling pathway. 2. Dimethylacrylshikonin inhibits the proliferation of MCF-7 cells in vitro by inducing apoptosis through the downregulation of Bcl-2, upregulation of Bax and partial inactivation of the NF-κB pathway.

1. Schisandrol B (Besigomsin) may exert neuroprotective effects by attenuating the microglia-mediated neuroinflammatory response via inhibiting the TLR4-mediated NF-κB and MAPKs signaling pathways. 2. Schisandrol B has anti-inflammatory property, potentially result from the inhibition of COX-2, iNOS, IL-6, TNF-α and NO through the down-regulation of RIP2 and NF-κB activation. 3. Schisandrol B induces marked protective effects against hepatic and renal injury induced by CCl(4) exposure through differential regulation of the MAPK signal transduction pathway. 4. Schisandrol B significantly inhibits cell proliferation in a dose-dependent manner, due to cell cycle arrest in the G1 phase with the downregulation of cyclin D1 expression and Retinoblastoma (RB) phosphorylation.

BTYNB (MDK6620) is an inhibitor of the oncofetal mRNA-binding protein IMP1 (IC50 = 5 μM for IMP1 binding to c-Myc mRNA). MDK6620 downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB). It disrupts this enhancer function by impairing IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA association

GS143 is a selective IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. It suppresses NF-κB activation and transcription of target genes without inhibiting proteasome activity. GS143 has anti-asthm[atic] properties.

Damascenone is a mixture of E- and Z-isomer damascenones, characteristic compounds with anti-inflammatory properties derived from Epipremnum pinnatum.

NF-κΒ Activator 2 is a potent, orally active compound that efficiently activates NF-κB with an EC50 value of 1.58 μM. By enhancing NF-κB expression and activation, it induces SOD 2 synthesis, rendering it useful for amyotrophic lateral sclerosis (ALS) research [1].

Triamcinolone (Aristocort) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B.

Artemisinin B is a drug which may improve spatial memory in dementia patients and alter the levels of inflammatory cytokines in the hippocampus and the cortex. Artemisinin B may inhibit neuroinflammation and exert neuroprotective effects on cognitive functions by modulating the TLR4-MyD88-NF-κB signaling pathway. Artemisinin B has shown potential in the treatment of neuroinflammatory diseases.

Resveratrol is a potent phenolic antioxidant found in grapes, red wine, and various berries that also has antiproliferative and anti-inflammatory activity. cis-Resveratrol is the double bond isomer of trans-resveratrol, the more often studied and naturally abundant of the two resveratrol isomers. cis-Resveratrol exhibits antioxidant activity in the µM range similar to that observed with trans-resveratrol. It blocks production of reactive oxygen species (ROS) by inhibition of NAD(P)H oxidase and also inhibits production of nitric oxide. At a concentration of 100 µM, cis-resveratrol significantly inhibits the expression of genes related to the Rel/NF-κB/IκB family, adhesion molecules, and acute-phase proteins in LPS and INF-γ-stimulated murine peritoneal macrophages. cis-Resveratrol inhibits uptake of noradrenaline and 5-HT by synaptosomes from rat brain with IC50 values of 79 and 51 µM, respectively. It also inhibits human monoamine oxidase-A (MOA-A) and MOA-B with IC50 values of 25 and 61 µM, respectively, which is similar to, but slightly less effective than, values obtained with trans-resveratrol.

Mollugin (Rubimaillin) may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for a chemotherapeutic agent in OSCCs via the upregulation of the HO-1 and Nrf2 pathways and the downregulation of NF- κ B. Mollugin may be a novel therapeutic candidate for bone loss-associated disorders including osteoporosis, rheumatoid arthritis, and periodontitis. Also, it has anticancer efficacy, can modulate the HER2 pathway in HER2-overexpressing Y cells with a potential role in the treatment and prevention of human breast and ovarian Y with HER2 overexpression.

1. Phellodendrine (Phallodendrin) has anti-nephritic activity, may be due to its ability to inhibit the proliferation or the migration of macrophages and cytotoxic T lymphocytes in the glomeruli.

Nepetoidin B has anti-fungal, anti-bacterial, and antiinflammatory effects, it can inhibit LPS-stimulated NO production possibly via modulation of iNOS mediated by MKP-5/NF-κB pathways in RAW 264.7 cells.