TNF-α

Lenalidomide is a derivative of thalidomide. In vitro, lenalidomide has three main activities: direct anti-tumor effect, inhibition of the micro environment support for tumor cells, and immunomodulatory role. It induces tumor cell apoptosis directly and indirectly by inhibition of bone marrow stromal cell support, by anti-angiogenic and anti-osteoclastogenic effects, and by immunomodulatory activity.

Pomalidomide is a derivative of thalidomide and acts as an immunomodulator.

Thalidomide can directly inhibit angiogenesis induced by bFGF or VEGF in vivo.

Necrostatin-1 is an ATP-competitive, allosteric inhibitor of receptor-interacting protein kinase 1 (RIPK1) (EC50 = 182 nM).

GW4869 is a cell permeable, selective inhibitor of N-SMase (neutral sphingomyelinase).

Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor.

KR-33493 is a potent inhibitor of Fas-mediated cell death (FAF1).

C87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.

DCVC inhibits pathogen-stimulated TNF-α in human extra placental membranes in vitro.

QNZ inhibits the activation of the transcription factor NF-κB and has been used to investigate NF-κB signaling.

Necrostatin 2 is a potent necroptosis inhibitor with EC50 of 50 nM.

Necrostatin 2 is a potent necroptosis inhibitor with EC50 of 50 nM.

Necrostatin 2 is a potent necroptosis inhibitor with EC50 of 50 nM.

Ginsenoside Rc, isolated from Panax ginseng, may exert various activities including anti-cancer, anti-inflammatory, antiobesity, and anti-diabetic effects.

Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinflammatory and antioxidant properties. Homoplantaginin could inhibit TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.

Cynaropicrin is a sesquiterpene lactone originally isolated from artichoke (C. scolymus) that has diverse biological activities. It inhibits the growth of SKOV3, LOX-IMVI, A549, MCF-7, HCT15, and PC-3 cancer cells (IC50s = 1.1-8.7 μg/ml).

Ro 08-2750 is a potent and selective Nerve growth factor (NGF) inhibitor that binds the NGF dimer (KD ~ 1 μM).

C25-140, a first-in-class, fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity.

DRI-C21045 is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 ?M.

SPD304 is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor.

TNF-α-IN-1 is a TNF-α inhibitor extracted from patent US20030096841A1, compound example I-7.

R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.

Dexanabinol exhibits not only the antioxidant and neuroprotective activities in brain but also anti-inflammatory activity by inhibiting NF-κB and decreasing cytokines such as TNFα and interleukin-6, which could ensure the integrity of BBB and reduce cell apoptosis and death.

Roquinimex (Linomide; PNU212616; ABR212616) is a quinoline derivative immunostimulant which increases NK cell activity and macrophage cytotoxicity; inhibits angiogenesis and reduces the secretion of TNF alpha.

Gamma-glutamylcysteine (TFA) ((γ-glutamylcysteine (TFA)), an intermediate in glutathione (GSH) synthesis, is a dipeptide served as an essential cofactor for the antioxidant enzyme glutathione peroxidase (GPx).

(Rac)-Benpyrine, a racemate of Benpyrine, is a potent and orally active TNF-α inhibitor. (Rac)-Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.

Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.

UCB-9260, an orally active compound, inhibits TNF signaling by stabilising an asymmetric form of the trimer. UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar Kd of 13?nM.

Sinensetin is a methylated flavone found in certain citrus fruits. pocess potent antiangiogenesis and anti-inflammatory, sinensetin enhances adipogenesis and lipolysis.

CPI-1189 (REN 1654, REN 1189) is the proapoptotic cytokine tumor necrosis factor (TNF) alpha inhibitor.

Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue that exhibits potent anti-inflammatory activity. It exerts its effects by blocking mitogen-activated protein kinase (MAPK) signaling and inhibiting the nuclear translocation of the NF-κB subunit p65, thereby suppressing key inflammatory pathways. Additionally, compound 5a27 reduces neutrophil infiltration and the production of pro-inflammatory cytokines. In vivo, it significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI), highlighting its potential as a therapeutic candidate for inflammatory and respiratory disorders.

HS-276 is an orally bioavailable, potent, and highly selective inhibitor of transforming growth factor-β–activated kinase 1 (TAK1), with a Kᵢ of 2.5 nM. It exhibits strong inhibition of TAK1 and moderate activity against a panel of other kinases, including CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with respective IC₅₀ values ranging from 8.25 to 5585 nM. HS-276 is a valuable tool for investigating TAK1-mediated signaling pathways and holds therapeutic potential for inflammatory conditions such as rheumatoid arthritis (RA).

AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes.

Muscone, a TNF receptor inhibitor, is derived from the traditional Chinese medicine musk. It effectively inhibits NF-κB signaling and NLRP3 inflammasome activation, resulting in a significant reduction of inflammatory cytokines such as IL-1β, TNF-α, and IL-6. This compound is valuable in research focused on inflammation, cardiac function restoration, and improving survival rates in various pathological conditions.