pro-inflammatory cytokine

ML604086 suppresses CCL1 mediated chemotaxis and enhances intracellular Ca2 concentrations. ML604086 is a selective inhibitor of CCR8. It also inhibiting CCL1 binding to CCR8 on circulating T-cells.

6-OAU (GTPL5846)(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.

(±)-Lisofylline is an enantiomer-specific, alkyl-substituted methylxanthine, which has specific and potent activity in down-regulating leukocyte activation. (±)-Lisofylline is an anti-inflammatory agent.

7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) exhibits anti-inflammatory, antibacterial, and antifungal activities, along with moderate antitrypanosomal activity, having an MIC value of 19.0 µg/mL.

Oxidopamine hydrobromide (6-OHDA hydrobromide) is a widely used neurotoxin and an antagonist of the neurotransmitter dopamine. It selectively destroys dopaminergic neurons, promotes COX-2 activation, induces PGE2 synthesis, and stimulates the secretion of the pro-inflammatory cytokine IL-1β. It is commonly used to establish animal models of Parkinson’s disease (PD).

Cadonilimab (AK104) is a tetravalent PD-1/CTLA-4 bispecific humanised antibody that activates T cells by enhancing IL-2 and IFN-γ secretion while reducing pro-inflammatory cytokine secretion (e.g., IL-6, IL-8). It offers low toxicity and high affinity, making it suitable for metastatic cervical, gastric, hepatic, and pulmonary cancers, pancreatic cancer, and oesophageal squamous cell carcinoma.

Cynandione A, an acetophenone derived from Cynanchum wilfordii, has anti-inflammatory activity and significantly reduces pro-inflammatory cytokine overexpression via macrophage α7 nAChR activation and subsequent IL-10 expression.

Nisin Z has anti-inflammatory activity and reduces pro-inflammatory cytokine release by inhibiting activation of the ERK1/2 and p38 mitogen-activated protein kinase (MAPK) signaling pathways, attenuating lipopolysaccharide-induced mastitis through inhibition of the ERK1/2 and p38 mitogen-activated protein kinase signaling pathways.

SIRT5 inhibitor 6 is a novel and potent Sirtuin 5 inhibitor with an IC50 = 310 nM for the treatment of sepsis-associated acute kidney injury (AKI) that modulates protein succinylation and pro-inflammatory cytokine release in the kidney and attenuates renal dysfunction and pathologic injury.

SIRT5 inhibitor 7 (compound 58), a substrate-competitive and selective SIRT5 inhibitor with IC 50 = 310 nM, significantly attenuated renal dysfunction and pathological damage in lipopolysaccharide (LPS)- and cecum ligation/perforation (CLP)-induced septic AKI mice, and modulated proteinsuccinimidylation and proinflammatory cytokine release and pro-inflammatory cytokine release in the kidneys of acute kidney injury (AKI) mice.

Triamcinolone (Aristocort) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B.

GSK-5498A is a selective blocker of CARC (IC50, 1 μM). It inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.

LP99 is an epigenetic probe. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells. LP99 is an effective and selective inhibitor of the BRD7 and BRD9 bromodomains (Kd: 99 nM against BRD9).

STAT3-IN-31 (compound K2071), derived from STATtic, acts as an inhibitor of both STAT3 and mitotic processes. This compound interrupts mitotic progression and impacts the formation of the mitotic spindle. Additionally, STAT3-IN-31 hampers migration in glioblastoma cells, suppresses cellular proliferation within tumor spheroids, induces senescence in glioblastoma, and inhibits the growth of Temozolomide-resistant cells while reducing the secretion of the pro-inflammatory cytokine monocyte chemoattractant protein (MCP-1).

NOD1-RIPK2-IN-1 (Compound 37) is an inhibitor of the NOD1-RIPK2 signaling pathway, displaying potent IC50 values of 42 nM and 1.52 nM against NOD1 and RIPK2, respectively. This compound effectively reduces the secretion of the pro-inflammatory cytokine IL-8, making it valuable for research in inflammation and immune disorders.

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.

PDE4B-IN-6 (Compound 4i) is a potent and highly selective inhibitor of phosphodiesterase 4B (PDE4B) with an IC50 of 7.42 nM. As a roflumilast analogue, it exhibits significantly higher selectivity for PDE4B over PDE4A (IC50 = 1540 nM, ~195-fold) and PDE4C (IC50 = 1260 nM, ~169-fold). PDE4B-IN-6 exerts anti-inflammatory effects by elevating intracellular cAMP levels and suppressing the expression of the pro-inflammatory cytokine TNF-α. Additionally, it demonstrates good antioxidant properties and low cytotoxicity, making it suitable for research on chronic obstructive pulmonary disease (COPD) and related inflammatory conditions.

Anti-inflammatory agent 5w is a investigational anti-inflammatory compound, its activity was tested by pro-inflammatory cytokine production. Consistent with results observed in HaCaT keratinocytes, ELISA analysis showed that Anti-inflammatory agent 5w significantly suppressed IL-6 secretion induced by 24-hour LPS stimulation. This inhibition was dependent on concentration and was already evident after a 3-hour pretreatment, with near-complete suppression at 1 μM, bringing IL-6 levels close to those seen in untreated control cells

LMP-420 is a selective inhibitor of tumor necrosis factor-α (TNF-α). It reduces the release of pro-inflammatory cytokines, such as IL-1β and IL-2, while inducing the expression of anti-inflammatory cytokine IL-10, and anti-apoptotic molecules SOCS-1 and Mn-SOD. LMP-420 also downregulates chemokines like IP-10 and MCP-1, which decreases immune cell infiltration. This compound shows potential for research into type 1 diabetes, inflammatory diseases such as colitis, and HIV-mycobacterium tuberculosis co-infection.

KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a Ki of 138 nM. It shows no activity on μ and δ opioid receptors or the σ1 receptor, and exhibits very low affinity for the σ2 receptor (Ki = 2.8 μM). This compound significantly reduces the secretion of pro-inflammatory cytokines, such as IL-6, TNF-α, and IFN-γ, while increasing the secretion of the anti-inflammatory cytokine IL-10. Additionally, KOR agonist 7 decreases the expression of pro-inflammatory M1 macrophage marker (CD80) and increases the expression of anti-inflammatory M2 macrophage marker (CD163). It can be utilized for pain relief and immunomodulation.

DRAK1/2-IN-2 (Compound Y17) is an inhibitor of DRAK1/2, with IC50 values of 353.2 nM for DRAK2 and 507.4 nM for DRAK1. This compound enhances mitochondrial membrane potential and glucose-stimulated insulin secretion (GSIS). It also combats lipotoxicity-induced apoptosis and significantly suppresses the secretion of the pro-inflammatory cytokine IL-1β, providing anti-inflammatory effects. Additionally, DRAK1/2-IN-2 significantly reduces blood glucose levels in mice and is applicable in diabetes research.

Cot-IN-4 (compound 32) is a potent inhibitor of cancer Osaka thyroid (COT) kinase, with an IC50 value of 6 nM. It effectively inhibits the phosphorylation of ERK (IC50: 60 nM) and suppresses the release of TNFα (IC50: 60 nM). Additionally, Cot-IN-4 reduces the production of the pro-inflammatory cytokine IL-1β in macrophages stimulated by uric acid (IC50: 0.2 μM). This compound is applicable for research in inflammatory diseases.

TLR7/8 agonist 14 is a dual-target agonist of TLR7 and TLR8, with EC50 values of 75 μM for TLR7 and 96 μM for TLR8. This compound enhances the secretion of pro-inflammatory cytokines TNF-α, IL-1β, IL-8, and IFN-γ, while also increasing cytokine secretion and CD86 expression levels. TLR7/8 agonist 14 is applicable in colorectal cancer research.

Betamethasonesuccinate (NSSL-BMS) is a nanoformulation capable of crossing the blood-brain barrier, created by encapsulating Betamethasone hemisuccinate in PEGylated liposomes. By leveraging the enhanced permeability and retention effect of liposomes, Betamethasone succinate effectively delivers potent glucocorticoids to inflammatory sites. It inhibits the secretion of pro-inflammatory cytokines, such as TNF-α and IL-6, while maintaining the levels of the anti-inflammatory cytokine TGF-β. This compound is useful for researching arthritis and cerebral malaria.