TNF Receptor Inhibitor

Dichotomine C ((R)-(-)-Dichotomine C) is a β-carboline-type alkaloid with antiallergic effects. Dichotomine C inhibits the release of β-hexosaminidase in RBL-2H3 cells with an IC₅₀ of 62 μM. Dichotomine C inhibits the releases of antigen-IgE-mediated TNF-α and IL-4 in RBL-2H3 cells with IC₅₀s of 19 μM and 15 μM, respectively. Dichotomine C can be used for the study of type I allergic reactions.

DN203316 (PPARδ agonist 11) is a potent, selective, orally active PPARδ agonist (EC₅₀ = 20 nM) with high selectivity over PPARα and PPARγ. DN203316 suppresses NF-κB-mediated inflammatory signaling, inhibits ferroptosis by upregulating xCT and GPX4, and attenuates STING-TBK1-IRF3-driven fibrogenic responses. DN203316 is useful for research on inflammatory disorders, metabolic dysfunction-associated steatohepatitis (MASH), and liver fibrosis.

2-O-Methylatromentin is an anti-neuroinflammatory agent. 2-O-Methylatromentin shows inhibitory activity on the production of pro-inflammatory cytokines TNF-α, IL-6 and IL-1β in Lipopolysaccharides (HY-D1056) (LPS) -induced BV-2 microglial cells. 2-O-Methylatromentin can be used for the study of neuroinflammatory related diseases.

Fosimdesonide, a small molecule of adalimumab fosimdesonide, is a potent immunomodulator. Fosimdesonide shows anti-inflammatory activity.

CSF1R-IN-27 is a CSF1R inhibitor with oral effectiveness, kinome-wide selective profile, low cellular cytotoxicity, and CSF1R IC₅₀ values of 19 nM, 88 nM, 173 nM, 797 nM, 1448 nM, and >3000 nM. CSF1R-IN-27 suppresses M-CSF-induced phosphorylation of CSF1R, AKT, and ERK in macrophages, and inhibits hepatic p-CSF1R/p-AKT/p-ERK signaling. CSF1R-IN-27 reduces serum transaminase levels, improves hepatic histopathology, alleviates inflammatory cell infiltration, and decreases circulating TNF-α and IL-6 levels. CSF1R-IN-27 can be used for the research of acute liver injury.

Spirohypertone B is a potent Tumor necrosis factor-α (TNF-α) inhibitor. Spirohypertone B protects L929 cells from death induced by co-incubation with TNF-α and Actinomycin D (HY-17559).

NLRP3-IN-96 is a blood-brain barrier-penetrant NLRP3 inhibitor with a human K_d value of 556 nM. NLRP3-IN-96 inhibits NLRP3 inflammasome activation, suppresses IL-1β release and reduces NLRP3 expression, and inhibits TNF-α production through an NLRP3-independent pathway. NLRP3-IN-96 can be used for research on neuropathic pain.

MR2938 is a potent AChE inhibitor, with an IC₅₀ of 5.04 μM. MR2938 also suppresses NO production obviously (IC₅₀ = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research.

RNP-11 is a selective COX-2 inhibitor with an IC₅₀ of 42.85 μg/mL against human COX-2, and also acts as a bactericide and anti-inflammatory agent. RNP-11 inhibits the production of pro-inflammatory cytokines (IL-6, TNF-α, IL-1β, disrupts bacterial cell membranes and induces bacterial cell death. RNP-11 exhibits activity against strains of Staphylococcus and Enterococcus, including Methicillin (HY-121544)-resistant Staphylococcus aureus and Vancomycin (HY-B0671)-resistant Enterococcus faecium. RNP-11 reduces the load of Staphylococcus aureus, exerting dual effects of pathogen clearance and inflammatory response alleviation in a mouse skin infection model,. RNP-11 can be used in research related to infections caused by Staphylococcus, Staphylococcus aureus and Enterococcus faecium.

1-(3-Carboxypropyl)-3,7-dimethylxanthine is the major circulating oxidative carboxylation metabolite of Pentoxifylline (HY-B0715). 1-(3-Carboxypropyl)-3,7-dimethylxanthine protects fibrosarcoma cells against the cytotoxic effect of TNF-α.

Xanthine oxidase-IN-6 (Compound 6c) is a potent, orally active, mixed-type xanthine oxidase (XOD) inhibitor with an IC₅₀ value of 1.37 µM. Xanthine oxidase-IN-6 shows strong anti-hyperuricemia and renal protective activity.

KSI-028 is a STING inhibitor. KSI-028 disrupts STING-mediated signal transduction, reduces IFN-β and pro-inflammatory cytokine (IL-6, IL-1β and TNF-α) production. KSI-028 inhibits the phosphorylation of STING, TBK1, IRF3, and STAT1. KSI-028 attenuates renal and hepatic injury in a Cisplatin (HY-17394)-induced acute kidney injury mouse model.

JAK-IN-39 (compound 11) is a JAK inhibitor that suppresses JAK1, JAK2, JAK3 with IC₅₀ values of 0.05, 1.18, and 0.03 nM, respectively. JAK-IN-39 can inhibit the viability of TF-1 cells and also suppress the production of lymphocyte TNFα and INFγ in vitro.

AD-35 is an orally active, blood-brain barrier-permeable acetylcholinesterase inhibitor with an IC₅₀ of 793 nM. AD-35 inhibits metal-induced amyloid-β aggregation and disassembles preformed amyloid-β aggregates. In rat models of cognitive impairment, AD-35 attenuates Aβ_25-35-induced astrocyte activation, TNF-α and IL-1β release, inhibits ERK phosphorylation, and alleviates learning and memory deficits. AD-35 can be used for research on Alzheimer's disease.

β-Bisabolol is a potent anti-inflammatory agent that can be found in cotton gin trash. β-Bisabolol inhibits the production of nitric oxide (NO), pGE₂, TNF-α, IL-6, and IL-8 in LPS (HY-D1056)-stimulated macrophages and fibroblast cells. β-Bisabolol can be used for the research on inflammatory conditions.

Dendrocandin U is a bibenzyl compound found in Dendrobium officinale that exhibits anti-inflammatory activity and α-glucosidase inhibitory effect (IC₅₀ = 9.46 mM). Dendrocandin U inhibits the expression of TLR4 and MyD88 in the TLR4/MyD88/NF-kB pathway, suppresses the phosphorylation of NF-kB p65 and I-kBα, and blocks the nuclear translocation of NF-kB p65. Dendrocandin U inhibits M1 polarization, NO secretion, and TNF-α release in alveolar macrophages, and reduces inflammatory morphological changes in macrophages. Dendrocandin U promotes neurite outgrowth in PC12 cells. Dendrocandin U can be used for research on inflammation-related diseases and type 2 diabetes.

LC-PDA-01 is a selective peroxiredoxin 1 (PRDX1) activator with an EC₅₀ of 111.8 nM and a human K_D of 123.2 nM. LC-PDA-01 inhibits the expression of pro-inflammatory cytokines IL-1β, IL-6 and TNF-α. LC-PDA-01 can be used in antioxidant/anti-inflammatory research.

ABI793 is a human IgG1 anti-human CD154 (CD40 ligand) monoclonal antibody. ABI793 inhibits immune response by blocking the CD154-CD40 (IC₅₀ = 75 nM) signaling pathway. ABI793 effectively prevents kidney transplant rejection. ABI793 can be used for research on immunological rejection.

LPZ-51 is a Vibrio β-lactam resistance sensor kinase (VbrK) inhibitor with a K_i value of 1.09 μM. LPZ-51 inhibits blaA gene expression at the transcriptional level by blocking the kinase activity of VbrK, reduces β-lactamase synthesis, and does not affect bacterial growth. LPZ-51 acts synergistically with β-lactam antibiotics. LPZ-51 decreases bacterial load, alleviates intestinal inflammation, and improves survival rate in zebrafish infection models. LPZ-51 can be used in studies related to Vibrio parahaemolyticus infection.

FPA154 is a human monoclonal antibody against TNFRSF18/GITR/CD357. FPA154 activates NF-κB via the GITR pathway. FPA154 can be used in solid tumor research. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).