inos-in-6

iNOs-IN-6 is an anti-inflammatory agent known for inhibiting the expression of NF-κB, iNOS, and MAPK with an IC50 ranging from 0.2 to 0.62 μM. Additionally, it decreases the levels of pro-inflammatory mediators, such as IL-6, TNF-α, and IL-1β, with an IC50 ranging from 0.4 to 0.69 μM.

CU-T12-9 is a potent TLR1/2 agonist(EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay). It acts by activating the NFkB pathway, upregulating proinflammatory cytokines, and enhancing TLR1 and TLR2 dimerization.CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.

Sabialimon P (compound 16), with an IC50 of 18.12 μM, functions as a NO release inhibitor and exhibits anti-inflammatory properties. It effectively diminishes the secretion of TNF-α, iNOS, IL-6, and NF-κB, and suppresses the expression of COX-2 and NF-κB/p65 in LPS-induced RAW264.7 cells.

PDE1-IN-9 (Compound 7a) is a selective inhibitor of phosphodiesterase 1 (PDE1), targeting PDE1C with an IC50 value of 11 nM. It effectively reduces the mRNA expression of IL-1β, IL-6, TNF-α, and iNOS, while also inhibiting the production of nitric oxide (NO) and reactive oxygen species (ROS). Additionally, PDE1-IN-9 demonstrates good metabolic stability in rat liver microsomes.

COX-2/15-LOX-IN-6 (Compound 5l) is a dual inhibitor of COX-2 and 15-LOX with IC50 values of 0.201 μM and 11.723 μM, respectively. In serum, it suppresses the expression of PGE, TNF-α, IL-6, and iNOS, and demonstrates anti-inflammatory activity in a carrageenan-induced rat edema model.

STAT1/3-IN-1 (Compound 6k) is an inhibitor of STAT1/3 phosphorylation. It prevents the phosphorylation and nuclear translocation of STAT1/3. Additionally, STAT1/3-IN-1 inhibits the inflammatory enzymes iNOS and COX-2. This compound exhibits anti-inflammatory properties by reducing pro-inflammatory cytokines, such as IL-1β, IL-6, and TNF-α, without significant cytotoxicity.

NLRP3-IN-76 is an orally active NLRP3 inhibitor that suppresses the production of NO and reduces the mRNA levels of pro-inflammatory cytokines (iNOS, IL-6, IL-1β, and TNFα). It exerts anti-inflammatory effects by inhibiting the activation of the NLRP3 inflammasome and the NF-κB signaling pathway. Furthermore, NLRP3-IN-76 can ameliorate DSS-induced colitis and is applicable for studying inflammatory bowel disease (IBD).

FGT-4 is a chimeric molecule targeting folate receptor β (FR-β) and functions as a TLR7 agonist. It enhances the secretion of iNOS and the pro-inflammatory cytokine IL-6 associated with M1 macrophages and promotes the proliferation of cytotoxic CD8+ T cells. FGT-4 demonstrates antitumor activity in the 4T1 breast cancer mouse model and is applicable for cancer immunotherapy research.

BS-153 is a novel synthetic oxazolidinone drug that exhibits anti-inflammatory effects by blocking the activation of the NF-κB/PKCθ pathway. It can suppress the expression levels of iNOS, COX-2, and pro-inflammatory cytokines (TNF-α, IL-1β, and IL-6) in LPS-stimulated RAW264.7 cells.

PDE1-IN-9 (Compound 7a) hydrochloride is a selective inhibitor of phosphodiesterase 1 (PDE1), with an IC50 of 11 nM for inhibiting PDE1C. It reduces the mRNA expression of IL-1β, IL-6, TNF-α, and iNOS and inhibits the production of nitric oxide (NO) and reactive oxygen species (ROS). Additionally, PDE1-IN-9 hydrochloride exhibits good metabolic stability in rat liver microsomes.

1. Negletein (7-O-Methylbaicalein) has anti-inflammatory and immunomodulatory activities via inhibition of TNF-α, iNOS and IL-1β. 2. Negletein as a neuroprotectant enhances the action of nerve growth factor and induces neurite outgrowth in PC12 cells. 3. Negletein shows a comparable redox-active potential, and it (50 μM, 4 h) can activate Nrf2. 4. Negletein shows significant antimicrobial activity. 5. Negletein has anti-hypoxia activity, it can significantly prolong the survival time of hypoxic mice.6. Negletein has anti- Alzheimer's disease activity, it inhibits the iron-dependent formation of ROS and also blocks the iron-induced oligomerization of amyloid beta 42 in vitro. 7. Negletein (IC50: 3.89 +/- 0.39 microM) exhibits potent inhibitory activity against nuclear factor of activated T cells (NFAT) transcription factor.

6-Formylpterin (Pterin-6-aldehyde) is an inhibitor of Xanthine Oxidase (Ki ~0.6 nM) with potent neuroprotective effects against transient IRI in gerbils.6-Formylpterin induces intracellular ROS generation in HL-60 cells as well as apoptosis ( 6-Formylpterin inhibits the expression of iNOS, produces hydrogen peroxide intracellularly and restores the impaired bactericidal activity of human neutrophils.

Rhein-13C4 is intended for use as an internal standard for the quantification of rhein by GC- or LC-MS. Rhein is an anti-inflammatory anthraquinone found in rhubarb and is the bioactive derivative of its prodrug diacerein . At 10 μM, rhein inhibits IL-1β signaling, suppressing signaling through NF-κB, and reduces the expression of the matrix metalloproteases MMP-1 and MMP-13.1 It inhibits IKKβ (IC50 = 11.8 μM), decreasing iNOS and IL-6 expression in LPS-stimulated macrophages but paradoxically increasing TNF-α, IL-1β, and HMBG1 expression.2 Rhein shows efficacy against pancreatic fibrosis, chronic pancreatitis, and hyperglycemia-induced pancreatic β-cell apoptosis.3,4 It also inhibits angiogenesis of breast cancer cells under normoxic and hypoxic conditions.5

NF-κB-IN-6 (Compound 3d) is an anti-inflammatory agent that suppresses the NF-κB signaling pathway, thereby reducing iNOS and COX-2 protein expression. It inhibits NO production in LPS-induced RAW264.7 cells with an IC50 of 23.1 μM[1].

α7 nAchR-JAK2-STAT3 agonist 1 is a potent inhibitor of the α7 nAchR-JAK2-STAT3 pathway that acts on nitric oxide (NO) (IC50: 0.32 μM). It has demonstrated positive effects on iNOS, IL-1β, and IL-1β in murine macrophages RAW264.7, and inhibited the expression of iNOS, IL-1β, and IL-6 in mouse macrophages. Additionally, α7 nAchR-JAK2-STAT3 agonist 1 suppressed LPS-induced NO release, NF-κB activation, and cytokine production, making it useful for studying sepsis.

iNOs-IN-1 (YPW) is a potent inhibitor of inducible nitric oxide synthase (iNOS) with anti-inflammatory effects, significantly inhibiting IL-6 and iNOS expression in a dose-dependent manner in murine macrophages, and also inhibiting LPS-induced NO generation.

COX-2-IN-10 is a potent COX-2 inhibitor that exhibits inhibitory effects on the production of IL-6, TNF-α, and IL-1β, and inhibits PGE2 production in a concentration-dependent manner with an IC50 value of 2.54 μM. Additionally, COX-2-IN-10 inhibits the expression of iNOS and COX-2 at both mRNA and protein levels.

1. Schisandrol B (Besigomsin) may exert neuroprotective effects by attenuating the microglia-mediated neuroinflammatory response via inhibiting the TLR4-mediated NF-κB and MAPKs signaling pathways. 2. Schisandrol B has anti-inflammatory property, potentially result from the inhibition of COX-2, iNOS, IL-6, TNF-α and NO through the down-regulation of RIP2 and NF-κB activation. 3. Schisandrol B induces marked protective effects against hepatic and renal injury induced by CCl(4) exposure through differential regulation of the MAPK signal transduction pathway. 4. Schisandrol B significantly inhibits cell proliferation in a dose-dependent manner, due to cell cycle arrest in the G1 phase with the downregulation of cyclin D1 expression and Retinoblastoma (RB) phosphorylation.

Anemarsaponin B has anti-inflammatory effect in LPS-treated RAW 264.7macrophages, the effect is associated with the inhibition of NF-κB transcriptional activity, possibly via the p38 MAP kinase pathway. Anemarsaponin B can inhibit PAF-induced rabbit platelet aggregation in vitro.

6(5H)-Phenanthridinone is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2. It decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells. 6(5H)-Phenanthridinone reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes. In vivo, 6(5H)-phenanthridinone reduces spinal cord expression of inducible nitric oxide synthase (iNOS), IL-1β, TNF-α, IL-2, and IFN-γ and reduces disease score in a rat model of experimental autoimmune encephalomyelitis (EAE). It also decreases serum levels of lactate dehydrogenase as well as hepatic lipid peroxidation, oxidative DNA damage, and PARP levels.

PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor with an IC50 of 15 nM, exhibiting anti-inflammatory properties through the inhibition of iNOS, TNF-α, IL-1α, IL-1β, and IL-6 expression induced by LPS. It has demonstrated efficacy in mitigating inflammatory bowel disease (IBD) symptoms in a dextran sodium sulfate (DSS)-induced colitis mouse model, suggesting its potential utility for IBD research [1].

Anti-inflammatory agent 54 (compound 9c), a Coixol derivative, exhibits anti-inflammatory properties by inhibiting the NF-κB pathway and reducing the expression of pro-inflammatory cytokines such as iNOS, TNF-α, IL-6, and IL-1β. It effectively suppresses LPS-induced nitric oxide (NO) production in RAW264.7 macrophages with an IC50 of 2.4 μM and demonstrates in vivo efficacy in a mouse auricular edema model [1].

Compound 9j (anti-inflammatory agent 55), a Coixol derivative, exhibits anti-inflammatory properties by inhibiting the NF-κB pathway and reducing the expression of iNOS, TNF-α, IL-6, and IL-1β. It notably suppresses LPS-induced nitric oxide (NO) production in RAW264.7 macrophages with an IC50 of 0.8 μM and demonstrates anti-inflammatory effects in vivo using a mouse auricular edema model [1].

Z21115 is an orally effective phosphodiesterase 4 (PDE4) inhibitor that can inhibit PDE4D7 with an IC50 of 10.5 nM. It suppresses the expression of IL-6, TNF-α, and iNOS induced by Lipopolysaccharide. In a DSS-induced mouse colitis model, Z21115 demonstrates anti-inflammatory activity without significant toxicity at doses up to 1 g/kg.