tnf-α-in-1

TNF-α-IN-1 is a TNF-α inhibitor.

TNF-α IL-1β-IN-1 (compound 11a) is an anti-inflammatory agent that effectively reduces the expression of TNF-α and IL-1β, inhibits oxidative stress and myocardial cell apoptosis, and demonstrates significant activity against septic myocardial injury. Additionally, it improves myocardial blood flow in vivo.

TNF-α-IN-11 (Compound 10) is a TNF-α inhibitor with a dissociation constant (K D) of 12.06 μM. It impedes TNF-α-induced caspase activation and the NF-κB signaling pathway by binding to TNF-α, suppressing the phosphorylation of IκBα and the nuclear migration of NF-κB p65. This compound is utilized in the study of TNF-α-mediated autoimmune diseases [1].

TNF-α-IN-10 (compound 8a) is an inhibitor of IL-6 and TNF-α, exhibiting anti-inflammatory activity [1].

TNF-α-IN-12, a TNF-α inhibitor with an IC50 of 0.1 μM, can reduce TNF-α blood levels [1].

TNF-α-IN-13, a potent inhibitor of TNFα, exhibits an IC 50 of less than 0.6 μM and possesses antiinflammatory properties (WO2001072735A2; example 6) [1].

TNF-α-IN-14, a potent TNFα inhibitor, exhibits a selective inhibition profile with an IC50 of 1.1 µM and demonstrates antiinflammatory properties (WO2001072735A2; compound 12) [1].

TNF-α-IN-15, a TNF-α inhibitor, effectively reduces TNF-α blood levels [1].

TNF-α-IN-16, a potent TNFα inhibitor, exhibits an IC50 of less than 0.6 μM and possesses anti-inflammatory properties (WO2001072735A2; example 18) [1].

TNF-α-IN-18 (Compound 61) is a small molecule inhibitor of tumor necrosis factor-alpha (TNF-α) that operates with a IC50 of 1.8µM. TNF-α-IN-18 effectively blocks the nuclear translocation of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB), thereby suppressing the downstream TNF signaling pathway; TNF-α-IN-18 exhibits minimal cytotoxicity in mouse fibroblast LM cells with a CC50 greater than 50 µM. TNF-α-IN-18has been shown to alleviate sepsis induced by TNF or lipopolysaccharide in mouse models, and provides significant protection against the development and progression of rheumatoid arthritis in murine models.

Cot inhibitor-1 hydrochloride is an inhibitor of tumor progression loci-2 kinase (IC50 = 28 nM) and inhibits the production of TNF-α in human whole blood (IC50 = 5.7 nM).

LTβR-IN-1 is a potent and selective lymphin β receptor (LTβR) inhibitor with a selective inhibitory effect on the nuclear translocation of p52 of TNF12A, without affecting the nuclear translocation of p65 mediated by the TNF-α receptor. It inhibits p52 nuclear translocation stimulated by TWEAK or Anti-LTβR with an IC50 of 10 μM and regulates the NF-kB signaling pathway in a ligand-independent manner.

Vialinin A (Terrestrin A), a p-terphenyl compound, exhibits antioxidant properties and acts as a potent inhibitor of TNF-α, USP4, USP5, and sentrin SUMO-specific protease 1 (SENP1). Its efficacy in autoimmune diseases and cancer research is noteworthy, highlighting its potential therapeutic applications.

CU-115 is a selective and potent TLR8 antagonist with IC50 of 1.04 µM and =>50 µM for TLR8 and TLR7, respectively. CU-115 decreases production of TNF-α and IL-1β activated by R-848 in THP-1 cells.

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.

Fumaric acid (2-Butenedioic acid) attenuates the eotaxin-1 expression in TNF-α-stimulated fibroblasts by suppressing p38 MAPK-dependent NF-κB signaling. Fumaric acid has recently been identified as an oncometabolite or an endogenous, cancer-causing metabolite. High levels of this organic acid can be found in tumors or biofluids surrounding tumors. Its oncogenic action appears due to its ability to inhibit prolyl hydroxylase-containing enzymes.

5,6-Benzoflavone (β-Naphthoflavone) is an exogenous ligand for the aryl hydrocarbon receptor, which disrupts zinc homeostasis in human hepatocellular carcinoma HepG2 cells. 5,6-Benzoflavone (β-Naphthoflavone) possesses anti-inflammatory and antioxidant activities, inhibits LPS-induced inflammation through the AKT/Nrf-2/HO-1-NF-kappaB signaling axis, inhibits TNF-α-induced ICAM-1 and VCAM-1 expression, which can be used to study neurodegenerative diseases.

MG-T-19, a TIM-3 inhibitor (KD=0.26 μM), significantly inhibited the interaction of TIM-3 with PtdSer, CEACAM1, and Gal-9, and increased the production of TNF-α and IFN-γ in PBMCs, which reactivated the tumor-attacking ability of T cells.

1. β-Anhydroicaritin exhibits immunosuppressive effect on the mouse macrophages stimulated by LPS. 2. β-Anhydroicaritin phytosomes can inhibit enhanced bone turnover induced by ovariectomy, improve BMD the biomechanical properties of vertebrae, without any stimulation on uterus. 3. β-Anhydroicaritin possesses significant protective effects on the zymosan-induced peritonitis mice, which might be associated with the regulation of Ca(2+); influx in macrophages and iNOS expression.

SKF-86002 is an effective inhibitor of p38 MAP kinase (IC50: 0.5-1 uM); inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50: 1 μM).

4-Deoxypyridoxine (4-DPD) is a vitamin B6 antimetabolite with diverse biological activities. It inhibits transport of pyridoxine , pyridoxal, and pyridoxamine in and reduces growth of S. carlsbergensis cells. 4-DPD inhibits sphingosine-1-phosphate (S1P) lyase and reduces cyclic stretch-induced apoptosis in alveolar epithelial MLE-12 cells. 4-DPD (5 mg, i.p.) reduces lysyl oxidase activity by 26% and reduces collagen and elastin crosslinking, resulting in limb abnormalities in chick embryos. It decreases latency to first seizure in mice (ED50 = 1 mmol kg) and increases the occurrence and duration of myoclonic responses in baboons with photosensitive epilepsy. 4-DPD reduces TNF-α and IL-6 production in mice infected with T. spiralis.

EJMC-1 is an inhibitor of TNF-α with an IC50 value of 42 μM and can be used in studies about auto-inflammatory diseases.

Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) and it also can potently inhibit the release of TNF-α in vitro, ex vivo, and in vivo with IC50s of 144 ng mL in vitro and 81.7 ng mL ex vivo, respectively[1].

Manumycin A is an antibiotic with anticancer activity and is a mammalian thioredoxin reductase-1 (TrxR-1) inhibitor.Manumycin A inhibits the production of IL-1β, IL-6, and IL-8 in TNF alpha-stimulated THP-1 cells and peripheral blood mononuclear cells in a dose-dependent manner, inducing apoptosis.