nfκb

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].

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

NF-κB inhibitor is a synthetic peptide corresponding to the nuclear localization sequence (NLS) of NF-κB p105 subunit (also known as p50) appended to a hydrophobic sequence to facilitate import into living cells. It blocks the nuclear import of p105 in cells treated with activators of NF-κB signaling, including LPS and TNF-α. NF-κB control is a peptide that is identical in sequence to NF-κB inhibitor, except two essential, basic residues of the p105 NLS are substituted with non-basic amino acids. It is ineffective at blocking the activation of NF-κB signaling and is used as a negative control peptide.

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 NF-κB/PON1 pathway inhibitor with antioxidant activity (IC50: 45.76 μM) and hepatoprotective activity.

Akt/NF-κB/MAPK-IN-1 (compound 2m) serves as a potent, orally active inhibitor targeting NO with an IC50 of 7.70 μM and demonstrates low toxicity. This compound exerts anti-inflammatory effects by impeding the Akt/NF-κB and MAPK signaling pathways [1].

NF-κB-IN-10 (compound E1) is an inhibitor of NF-κB that mitigates heart failure symptoms through the modulation of 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 research in cardiovascular diseases [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 NF-κB pathway which can cross blood brain barrier (BBB). NF-κB-IN-4 shows potential anti-neuroinflammatory activity with low toxicity which can be used for the research of neuroinflammation related diseases. NF-κB-IN-4 can block the IκBα activation and phosphorylation, reduce NLRP3 expression, therefore inhibiting NF-κB activation [1].

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

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

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-5 (compound 4d) is an orally active NF-κB inhibitor. NF-κB-IN-5 interacts directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines, with IC 50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM for HCT116, U87-MG, HepG2, BGC823, 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).

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-12 (compound 3h) serves as a potent inhibitor of NF-κB, exhibiting an IC50 value of 1.02 μM. It is applicable 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 the nuclear translocation of NF-κB. It also reduces the expression levels of phospho-IKK, IκBα, and NF-κB p65. Demonstrating anti-inflammatory properties, NF-κB-IN-11 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 works by reducing the protein expression of iNOS and COX-2 by suppressing the NF-κB signaling pathway. NF-κB-IN-6 inhibits the production of NO 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 (IC50: 0.70 μM) and can be used as an anti-tumour agent.

Akt/NF-κB/JNK-IN-1 (Compound 2i) is an inhibitor of Akt, NF-κB and JNK signalling pathways.Akt/NF-κB/JNK-IN-1 exhibits an inhibitory effect on nitric oxide production (IC50: 3.15 μM) and shows anti-inflammatory effects.

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.

Cepharanthine (NSC-623442), a biscoclaurine alkaloid, suppresses tumor necrosis factor (TNF)-α-mediated NFκB stimulation, plasma membrane lipid peroxidation and platelet aggregation and inhibits cytokine production.

Myristic acid (Crodacid) , a 14 carbon saturated fatty acid, is a rare molecule in cells and is a substrate of some fatty acid desaturases. This compound has the ability to acylate proteins by covalently binding to the N-terminal glycine residues, in a process called N-terminal myristoylation. Myristoylation of substrate proteins by this fatty acid has the potential to activate and mediate many physiological pathways. Furthermore, saturated fatty acids have been reported to be essential for biological activities of lipopolysaccharides and have demonstrated the ability to induce expression of COX-2 and NFκB (nuclear factor κB) activation.

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.

INI-43, an inhibitor of Nuclear Import-43, shows a significant cytotoxic effect on various cervical and oesophageal cancer cell lines by targeting Kpnβ1 and interferes with the nuclear localization of Kpnβ1 and known Kpnβ1 cargoes, NFAT, NFκB, AP-1 and NF

1. Morusin (Mulberrochromene) possesses antitumor effects of cell lines including HT-29, A549, MCF-7, and MDA-MB-231, through suppressing STAT3 and NFκB attenuation mediated apoptosis induction. 2. Morusin possesses anti-oxidant and anti-inflammatory effects.

Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.

CTP-NBD is a cell-permeable, specific inhibitor of the NFκB peptide, which has been utilized in studies of colitis [1] [2].

GW-870086 is an effective anti-inflammatory agent. GW-870086 also plays a role in a glucocorticoid receptor agonist (pIC50: 10.1 in A549 cells expressing NF-κB).

EGCG Octaacetate, a prodrug of EGCG, is utilized to enhance the stability and bioavailability of EGCG in vivo. It has high efficacy, bioavailability, anti-oxidation, and anti-angiogenesis capacities.

MnTBAP chloride (Mn(III)TBAP) is a cell-permeable superoxide dismutase (SOD) mimetic and peroxynitrite scavenger that reduces the doubling time of SOD-E. coli by a factor of 2. MnTBAP chloride exhibits anti-inflammatory effects through upregulation of BMPR-II and inhibition of NFκB signaling. mnTBAP chloride is a manganese porphyrin complex with antioxidant properties and has potential for use in the study of fibrotic responses in chronic kidney diseases (CKDs).

Coenzyme Q0 (CoQ0), a potent, orally active ubiquinone compound derived from Antrodia cinnamomea, induces apoptosis and autophagy. It suppresses HER-2/AKT/mTOR signaling, enhancing apoptosis and autophagy mechanisms. Additionally, Coenzyme Q0 regulates NFκB/AP-1 activation and promotes Nrf2 stabilization, contributing to the attenuation of inflammation and redox imbalance. It also exhibits anti-angiogenic activity by downregulating MMP-9/NF-κB and upregulating HO-1 signaling.

4-Aaqb, also known as OB-318, is a natural inhibitor of the autophagy pathway, enhancing immune function, suppressing MAPK and NFκB, showing anti-inflammatory, hypoglycemic, vasorelaxative, and antiproliferative activities.

TBK1/IKKε-IN-4, a 6-aminopyrazolopyrimidine derivative, serves as a potent, selective inhibitor for TBK1 and IKKε, demonstrating IC50 values of 13 nM and 59 nM, respectively. This compound exhibits significantly reduced activity, by 100- to 1000-fold, against other protein kinases, such as PDK1, PI3K family members, and mTOR[1].

1. Desmethoxyyangonin (5,6-Dehydrokavain) protects LPS or LPS/D-GalN-induced damages in cell or liver tissues mainly through de-regulating IKK/NFκB and Jak2/STAT3 signaling pathways. 2. The induction of CYP3A23 by dihydromethysticin and Desmethoxy yangonin involves transcription activation, probably through a PXR-independent or PXR-involved indirect mechanism.

gamma-Linolenic acid (gamolenic acid), is an unsaturated fatty acid synthesized from linoleic acid (LA) by the enzyme delta-6-desaturase. Research on hepatocellular cell lines has shown γ-Linolenic Acid to have induced reactive oxygen species generation including lipid peroxidation, cell growth inhibition, and heme oxygenase-1 production for antioxidant protection against oxidative stress. Further experiments have noted that γ-Linolenic acid inhibits inflammatory responses through inactivation of NFκB and activator protein-1 by suppressed oxidative stress.

ML115 is a potent and selective activator of transcription 3 (STAT3), with abn EC50 of 2.0 nM, and is inactive against the related STAT1 and NFκB anti-targets.

HSR1304 (Compound 5d) is a potent inhibitor of NFκB, a multifunctional transcription factor involved in a wide range of human diseases (e.g. cancer, chronic inflammation). HSR1304 has potential for research in cancer diseases.

AK963, also known as 40708899, is a potent PAK1 (p21-activated kinase 1) inhibitor, which suppresses the proliferation of human gastric cancer cells significantly by downregulation of PAK1-NFκB-CyclinB1 pathway.

SN50 TFA is a cell-permeable inhibitor of NF-κB and attenuates alveolar hypercoagulation and fibrinolysis inhibition in acute respiratory distress syndrome mice through inhibiting NF-κB p65 translocation. SN50 TFA can be used in studies about ARDS.