nf-κb inhibition

N,N-Dimethylacetamide (DMAc) is a drug excipient with blood-brain barrier permeability and anti-inflammatory activity, acting through inhibition of the NF-κB signaling pathway. N,N-Dimethylacetamide can reduce endotoxin-induced inflammatory responses in vivo.

1. Linalool (Linalol), a natural compound of the essential oils, has been shown to have antinociceptive, antimicrobial, and anti-inflammatory properties. 2. Linalool was protected against LPS/GalN-induced liver injury through induction of antioxidant defense via Nrf2 activating and reduction inflammatory response via NF-κB inhibition. 3. Linalool biosynthesis and accumulation might be involved in plant defense against bacterial and fungal pathogens and be associated with field resistance to citrus canker. 4. Linalool significantly increased the expression of antioxidant enzymes regulated by Nrf-2 and diminished lung tissue levels of several pro-inflammatory cytokines, including tumor necrosis factor α (TNF-α) and interleukin (IL)-6.

HOIPIN-8 is a potent inhibitor of the linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. As a derivative of HOIPIN-1, it exhibits 255-fold greater inhibition of both petit-LUBAC and TNF-α-mediated NF-κB activation compared to HOIPIN-1. HOIPIN-8 is a promising tool to explore cellular functions of LUBAC.

ethyl 2-[3,5-bis(trifluoromethyl)phenyl]-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxylate is a synthetic compound belonging to the curcumin family. It is involved in the regulation of immune response and inflammation through inhibition of the NF-κB signaling pathway, in the regulation of antioxidant response through activation of the Nrf2 signaling pathway, and in the regulation of cell survival and proliferation through inhibition of the Akt signaling pathway.

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

ST 2825 is a specific MyD88 dimerization inhibitor that blocks IL-1β-mediated activation of NF-κB transcriptional activity.

Vamorolone (VBP15) is an orally active dissociative steroidal anti-inflammatory drug and membrane-stabilizer. Vamorolone improves muscular dystrophy without side effects. Vamorolone displays effective NF-κB inhibition and substantially decreases hormonal effects.

COX-2-IN-48 (5-25) serves as an inhibitor of COX-2, exhibiting an IC50 of 51.7 nM against human COX-2. It displays anti-inflammatory and analgesic effects in various rodent models through inhibition of the NF-κB pathway. COX-2-IN-48 (5-25) inhibits the degradation of IκB, phosphorylation and nuclear translocation of NF-κB p65, and the expression of COX-2 and iNOS.

COX-2-IN-51 (E25) is a potent COX-2 inhibitor with an IC50 of 70.7 nM. It significantly suppresses LPS-induced release of NO and PGE2, the expression of COX-2 and iNOS, and the activation of the NF-κB pathway. Displaying anti-inflammatory and analgesic effects in various mouse models through NF-κB pathway inhibition, COX-2-IN-51 has lower gastrointestinal side effects compared to Indomethacin.

Fosfenopril (Fosinoprilat) is a potent angiotensin-converting enzyme (ACE) inhibitor that mitigates lipopolysaccharide-induced inflammation in monocytes through the suppression of TLR4/NF-κB signaling pathways, and Fosfenopril is utilized in cardiovascular and anti-inflammatory research to investigate molecular mechanisms of ACE inhibition.

NLRP3-IN-78 (compound 21) is an NLRP3 inhibitor with a 46.72% inhibition rate of GSDMD-induced pyroptosis at 5 μM. It binds to the NLRP3 protein and prevents GSDMD-NT oligomerization. Additionally, NLRP3-IN-78 inhibits GSDMD cleavage and upstream NF-κB signaling, demonstrating anti-inflammatory activity.

SMU-L11 is a specific TLR7 agonist (EC50=0.024 μM) that recruits the MyD88 adaptor protein, activating downstream NF-κB and MAPK signaling pathways. In mouse models, SMU-L11 significantly enhances immune cell activation and boosts CD4+ T and CD8+ T cell proliferation, leading to direct tumor cell destruction and inhibition of tumor growth. This compound has applications in cancer research and potential in studying immune system disorders.

ROR1-IN-3 (Compound 24d) is a potent and highly selective inhibitor of the ROR1 kinase, with an IC50 of 17.6 nM. It demonstrates significant antitumor activity and ROR1 inhibition both in vitro and in vivo, exhibiting strong antiproliferative effects. ROR1-IN-3 induces apoptosis in cancer cell lines and inhibits downstream AKT/mTOR and NF-κB signaling pathways. This compound is applicable for antitumor research.

ACHP (IKK-2 Inhibitor VIII) is a novel selective and potent IKK inhibitor with inhibitory effects on IKK-α and IKK-β. ACHP has anti-HIV-1 activity and inhibits HIV-1 long terminal repeat (LTR)-driven gene expression through inhibition of NF-κB activation, inhibits TNF-α-induced NF-κB (p65) recruitment to the HIV-1 LTR, and inhibits TNF-α-induced NF-κB (p65) recruitment to the HIV-1 LTR. ACHKP has anti-HIV-1 activity and inhibits TNF-α-induced recruitment of NF-κB (p65) to the HIV-1 LTR.

S-Nitroso-N-acetylcysteine inhibits proliferation and survival of multiple MM cells. It acts by the S-nitrosylation-dependent inhibition of STAT3 and NF-κB.

SP-100030 is a dual inhibitor of NF-κB and activator protein-1 (AP-1), demonstrating potent inhibition with IC50 values of 50 nM for both. It effectively reduces the production of IL-2, IL-8, and TNF-alpha in Jurkat and other T cell lines. Additionally, SP-100030 has been shown to decrease the severity of murine collagen-induced arthritis (CIA).

SRTCX1003, a SIRT1 activator, suppresses inflammatory responses through promotion of p65 deacetylation and inhibition of NF-κB activity.

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.

Ladarixin (DF 2156A free base) is an orally active, non-competitive CXCR1/CXCR2 allosteric inhibitor that suppresses AKT, NF-κB, and angiogenesis, thereby slowing the progression of experimental human melanoma. It may be employed in research concerning COPD, asthma, and melanoma.

20(S)-Ginsenoside Rg3 (Rg3) possess an ability to inhibit the lung metastasis of tumor cells via inhibition of the adhesion and invasion of tumor cells. It inhibits the proliferation of human umbilical vein endothelial cells(HUVEC) and has anti-angiogenesis activities.

The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 μM compared to 20 μM by resveratrol.

Curcumenol ((+)-Curcumenol), one of the major components of Zedoary turmeric oil, is an antibiotic drug which has anti-Y, anti-inflammation activity. Curcumenol may be safely used without inducing metabolic drug-drug interaction through P450 inhibition.

C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid present in Saccharomyces cerevisiae, wheat grains, and the mammalian epidermal stratum corneum, composed of a phytosphingosine backbone amide-linked to a C18 fatty acid chain, C18 Phytoceramide regulates apoptosis, cell differentiation, smooth muscle cell proliferation, and mitochondrial respiratory chain activity while inhibiting IL-4, TNF-α, c-Jun, and NF-κB expression in histone-stimulated murine skin tissue, supporting its use in dermatological, inflammatory, and cosmetic skin barrier research.

Potent inhibitor of NF-κB activation (IC50 = 85 nM); decreases IκBα phosphorylation. Attenuates LPS-induced nitric oxide production and expression of TNF-α, IL-6 and MCP. Suppresses proliferation of HeLa and HCT116 cells. Anti-inflammatory and antitumor. Hu et al (2007) Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases. Chem.Biol. 14 764 PMID:17656313 |Johnson et al (2012) Myxobacteria versus sponge-derived alkaloids: the bengamide family identified as potent immune modulating agents by scrutiny of LC-MS/ELSD libraries. Bioorg.Med.Chem. 20 4348 PMID:22705020 |Kinder et al (2001) Synthesis and antitumor activity of ester-modified analogues of bengamide B. J.Med.Chem. 44 3692 PMID:11606134