neuroinflammatory

TQS (4-Naphthalen-1-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide) is a positive allosteric modulator of α7 nACh receptors.

Neuroinflammatory-IN-2 (compound 7i) is a potent anti-neuroinflammatory agent, capable of acting on MAO-B (IC50: 10.30 μM). Neuroinflammatory-IN-2 inhibits 96.33% of Aβ1-42 aggregation at 25 μM. Neuroinflammatory-IN-2 exhibits neuroprotective activity in H2O2-induced PC-12 cell injury. Neuroinflammatory-IN-2 can be used to study Alzheimer's disease.

Neuroinflammatory-IN-3 is a tubulin inhibitor that serves as both an anti-neuroinflammatory agent and a potent antitumor agent by inhibiting tubulin polymerization.

Neuroinflammatory-IN-1 (Compound 5) is an anti-neuroinflammatory agent that inhibits nitric oxide (NO) production with an IC50 of 65.4 μM [1].

MW01-2-151SRM is a novel small molecule inhibitor of microglia activation that crosses the blood-brain barrier, has anti-neuroinflammatory effects, attenuates the up-regulation of glial cytokines in models of neuroinflammation, and can be used in studies of traumatic brain injury, Alzheimer's disease, and alginate toxicity.

MAO-B-IN-8 is a highly potent and reversible inhibitor of monoamine oxidase-B (MAO-B), also inhibiting microglial production of neuroinflammatory mediators. This compound is specifically designed for research on neurodegenerative diseases [1].

CB1 antagonist 1 is a CB1 receptor antagonist, used in the research of obesity and metabolic syndrome, neuroinflammatory disorders, cognitive disorders, and gastrointestinal disorders, psychosis, and cardiovascular.

RV01 is a novel quinoline-substituted analogue of resveratrol that inhibits DNA damage, reduces ethanol-induced acetaldehyde dehydrogenase (ALDH2) mRNA expression, and has hydroxyl radical scavenging activity. rV01 reduces iNOS expression and has anti-neuroinflammatory effects. rV01 reduces tumor necrosis factor-a (TNF-a) and interleukin-6 (IL-6) mRNA levels and secretion. RV01 reduced tumor necrosis factor-a (TNF-a) and interleukin-6 (IL-6) mRNA levels and secretion, inhibited lps-induced ROS production and nicotinamide adenine dinucleotide phosphate (NADPH) oxidase activation, decreased toll-like receptor 4 (TLR4) protein expression, and inhibited lps-induced activation of mitogen-activated protein kinase (MAPK) and nuclear transcription factor-кB (NF-кB) signaling pathways.

Neuroprotective agent 5 (compound 28) acts as a brain-penetrating agent with anti-neuroinflammatory, antioxidant, and neuroprotective properties. It exhibits potent inhibition of nitric oxide (NO) with an EC50 of 0.49 μM and suppresses the release of pro-inflammatory mediators PGE2 and TNF-α. Additionally, it downregulates the expression of iNOS and COX-2 proteins, facilitating the polarization of BV-2 cells from a pro-inflammatory M1 phenotype to an anti-inflammatory M2 phenotype. Neuroprotective agent 5 also dose-dependently inhibits acetylcholinesterase (AChE) activity and the aggregation of Aβ42. This compound is useful for research into Alzheimer's disease.

Anti-neuroinflammation agent 2 (compound 4) exhibits both anti-neuroinflammatory and antibacterial properties, with an IC50 value of 3.06 µM for TNF-α, an IC50 value of 4.31 µM for IL-6, and an EC50 value range of 0.87 to 3.16 µM for Gram-positive bacteria.

FGA139 is an inhibitor of cysteine proteases, specifically targeting cathepsin B and L with IC50 values of 4.98 μM and 3.14 μM, respectively. It reduces the production of NO in LPS-induced RAW264.7 cells and lowers TNFα levels in microglia, demonstrating antioxidant and anti-inflammatory properties. Additionally, FGA139 enhances the secretion of neuroprotective metabolites such as purines and linoleic acid in LPS-stimulated microglia. This compound is applicable in the study of neuroinflammatory diseases.

Aβ1–42 aggregation inhibitor 2 (compound 7c) is a potent inhibitor of Aβ1-42 aggregation, playing a significant role in Alzheimer's disease research. It exhibits excellent antioxidant properties, metal ion chelation ability, reduces oxidative stress, and demonstrates neuroprotective and anti-neuroinflammatory activities.

AChE-IN-57 (compound 5b(SP-2)) is a potent inhibitor of AChE, capable of improving cognitive deficits. It restores biochemical mediators and suppresses reactive oxygen and nitrogen species associated with neuroinflammatory mechanisms, showing potential for Alzheimer's disease research.

BuChE-IN-10 (compound 7p) is a BuChE inhibitor with eqBuChEIC50 of 4.68 nM and huBuChEIC50 of 9.12 nM. It demonstrates anti-neuroinflammatory properties and exhibits high blood-brain barrier (BBB) permeability.

STAT3-IN-28 (compound 18) is an inhibitor of STAT3. It can suppress the activation of microglia and exhibits anti-neuroinflammatory effects. Additionally, STAT3-IN-28 is capable of crossing the blood-brain barrier.

N4-Acetylcytidine-13C5 is a 13C-labeled version of N4-acetylcytidine (N4A), an endogenous nucleoside metabolite produced from tRNA degradation. It is synthesized by enzymes such as N-acetyltransferase 10. N4-acetylcytidine may play a role in maintaining the activation of the NLRP3 inflammasome by inducing the expression and release of HMGB1. Additionally, it influences the stability and translation efficiency of mRNA, tRNA, and rRNA (e.g., enterovirus71RNA) through modification. This compound is utilized in studies related to cancer, neuroinflammatory diseases, viral infections, and obesity.

G721-0282 is an orally active inhibitor of CHI3L1 that reduces the expression of inflammatory proteins and cytokines. It suppresses the activation of the NF-κB signaling pathway, inhibits neuroinflammation, and decreases anxiety-related behaviors. Additionally, G721-0282 significantly curtails the proliferation of osteosarcoma (OS) cells by inhibiting the STAT3 signaling pathway and induces apoptosis in OS cells by upregulating pro-apoptotic protein levels while downregulating anti-apoptotic protein levels. This compound is useful in the study of neuroinflammatory diseases and cancer.

ARN-6039, an orally available inverse agonist of RORγ, targets Autoimmune Neuroinflammatory Demyelinating Disease. Its efficacy was demonstrated in a RORγ-activated IL-17A Prom/LUCPorter assay in HEK 293 cells (360 nM) and in IL-17 release from CD4+T cell assays (220 nM).

Polygalasaponin F has anti-neuroinflammatory activity, can inhibit the release of inflammatory cytokines TNF-α and NO induced by lipopolysaccharides (LPS) and reduce the expression of inducible nitric oxide synthases. Polygalasaponin F can significantly i

PKM2-IN-3 is a potent PKM2 kinase inhibitor, displaying an IC 50 value of 4.1 μM. The compound effectively suppresses PKM2-mediated glycolysis and NLRP3 activation, thereby exerting an anti-neuroinflammatory effect.

1. beta-Asarone (Cis-Isoelemicin) may be a potential preventive drug for Alzheimer's disease. 2. Beta-Asarone prevents autophagy and synaptic loss by reducing ROCK expression in SAMP8 mice. 3. The co-administration of beta-Asarone(Cis-Isoasarone) and l-dopa may contribute to the treatment of 6-OHDA-induced damage in rats by inhibiting autophagy activity. 4. Beta-Asarone exhibits anti-inflammatory effects by suppressing the production of pro-inflammatory mediators through NF-κB signaling and the JNK pathways in activated microglial cells and might be developed as a promising candidate to treat various neuroinflammatory diseases.

Aurantiamide has anti-cancer, anti-inflammatory and antinociceptive activities, it may suppress the growth of malignant gliomas by blocking autophagic flux.Aurantiamide has an anti-neuroinflammatory effect on LPS stimulation through its inhibition of the

Monoamine Oxidase B inhibitor 1 is a potent, reversible, orally active, and selective monoamine oxidase B (MAO-B) inhibitor (IC50 = 0.02 nM) capable of crossing the blood-brain barrier (BBB). It exhibits antioxidant and anti-neuroinflammatory activities and can be used in the study of Parkinson's disease[1].

MAPK-IN-1 (Compound 2) is an inhibitor of the MAPK signaling pathway with anti-neuroinflammatory and neuroprotective activities, suitable for Alzheimer's disease research. It inhibits AChE with an IC50 of 23.84 μM [1].