pro-inflammatory cytokine

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).

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.

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.

I942 is a novel, selective ACyclic nucleotide (NCN) EPAC1 agonist that activates exchange proteins to regulate inflammatory gene expression in human umbilical blood tubes and inhibit pro-inflammatory cytokine signaling associated with cardiovascular disease.

AN0128 (CRM-0005) is an anti-inflammatory boron-containing antibacterial agent that inhibits S. aureus, S. epidermidis, P. acnes, B. subtilis, and suppresses pro-inflammatory cytokine production in macrophage cell lines by inhibiting the p38 MAP kinase signaling pathway. It can be used in dermatological research.

Semapimod tetrahydrochloride (CPSI-2364 tetrahydrochloride) is a synthetic ornithine mitogen-activated protein kinase blocker and pro-inflammatory cytokine production inhibitor that interferes with macrophage and microglia function. Sematimod tetrahydrochloride inhibits TLR4 signaling, TNF-α, IL-1β, and IL-6, and is used in the study of Crohn's disease and other inflammatory conditions.

DCVC inhibits pathogen-stimulated TNF-α in human extra placental membranes in vitro.Target: TNF-αin vitro: DCVC inhibits pathogen stimulated cytokine release from tissue punch cultures. DCVC (5-50 μM) significantly inhibits LTA-, LPS-, and GBS-stimulated cytokine release from tissue cultures as early as 4 h (P ≤ 0.05). In contrast, TCA (up to 500 μM) does not inhibit LTA-stimulated cytokine release from tissue punches. DCVC effects on LTA-stimulated and LPS-stimulated TNF-α release from tissue punch cultures of extraplacental membranes. DCVC effects on GBS-stimulated release of pro-inflammatory cytokines from extraplacental membranes in transwell cultures. [1]. Boldenow E, et al. The trichloroethylene metabolite S-(1,2-dichlorovinyl)-l-cysteine but not trichloroacetate inhibits pathogen-stimulated TNF-α in human extraplacental membranes in vitro. Reprod Toxicol. 2015 Apr;52:1-6. [2]. Lash LH, et al. Multigenerational study of chemically induced cytotoxicity and proliferation in cultures of human proximal tubular cells. Int J Mol Sci. 2014 Nov 18;15(11):21348-65. [3]. Yoo HS, et al. Comparative analysis of the relationship between trichloroethylene metabolism and tissue-specific toxicity among inbred mouse strains: kidney effects. J Toxicol Environ Health A. 2015;78(1):32-49.

17-oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-Docosahexaenoic acid is a metabolite of lipoxygenase-mediated oxidation of DHA that is produced endogenously by aspirin-enhanced COX-2 activity. It has been shown to activate Nrf2-dependent antioxidant gene expression, to act as a PPARγ agonist (EC50 = ~200 nM), and to inhibit pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 μM).

Docosapentaenoic acid (DPA) is a ω-3 fatty acid found in fish oils. 17-oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is a metabolite of lipoxygenase-mediated oxidation of DPA that is produced endogenously by aspirin-enhanced COX-2 activity. It has been shown to activate Nrf2-dependent antioxidant gene expression, to act as a PPARγ agonist (EC50 = ~200 nM), and to inhibit pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 μM).

1. Kirenol (Kirel) has anti-oxidant, anti-inflammatory, anti-allergic, and anti-arthritic activities. 2. Kirenol is effective against gram-positive bacteria. 3. Kirenol possesses antitumor action on human chronic myeloid leukemia K562 cells in vitro. 4. Kirenol is capable of promoting osteoblast differentiation in MC3T3-E1 cells through activation of the BMP and Wnt β-catenin signaling pathways. 5. Kirenol treatment reduces pro-inflammatory cytokine secretion, increases anti-inflammatory cytokine production, inhibits cell proliferation and induces apoptosis of CII-specific lymphocytes in vitro.

1. Tetrahydrocoptisine (STYLOPINE) has effective effects in suppressing inflammation. 2. Tetrahydrocoptisine possesses a protective effect on LPS-induced ALI through inhibiting of NF-κB signaling pathways, which may involve the inhibition of pulmonary inflammatory process. 3. Tetrahydrocoptisine has gastroprotective activity, is attributed to reducing NO production and adjusting the pro-inflammatory cytokine, inhibited neutrophil accumulation and NF-κB expression. 4. Tetrahydrocoptisine is an active anti-inflammatory constituent by inhibition of TNF-α, IL-6 and NO production possibly via down-regulation of NF-κB activation, phospho-ERK1 2 and phospho-p38MAPK signal pathways.

LSD1-IN-21 is a potent, blood-brain barrier permeable LSD1 (lysine specific demethylase-1) inhibitor (IC50: 0.956 μM).LSD1-IN-21 significantly reduces the pro-inflammatory cytokine TNF-α and exhibits good anti-cancer and anti-inflammatory effects.

APC-0576 is an (S,S)-isomer which inhibits NF-kappaB-dependent gene activation. APC-0576 may prevent pro-inflammatory cytokine-induced chemokine production in human endothelial cells.

Itolizumab (Anti-Human CD6 Recombinant Antibody) is a recombinant anti-CD6 monoclonal antibody that targets the extracellular SRCR distal domain 1 of CD6, thereby slowing T cell proliferation and inhibiting pro-inflammatory cytokine production. Itolizumab can be used to study conditions such as psoriasis, rheumatoid arthritis (RA), and COVID-19 disease.

Atibuclimab is a chimeric monoclonal antibody targeting CD14, consisting of a mouse variable region and a human IgG4 Fc region. Atibuclimab can be used to treat amyotrophic lateral sclerosis. Atibuclimab reduces LPS-induced disease and inhibits LPS-induced pro-inflammatory cytokine release, delaying the release of anti-inflammatory cytokine soluble TNF receptor type I.

COX-2-IN-33 (compound 5f) is a selective COX-2 inhibitor with an IC50 of 45.5 nM, demonstrating potential as an anti-inflammatory agent by effectively suppressing pro-inflammatory cytokine production in vivo while maintaining gastric safety [1].

SIKs-IN-1 (compound 8h), a pyrimidine-5-carboxamide derivative, functions as an inhibitor of Salt-inducible kinases (SIKs), which play a role in M1 M2 macrophage polarization linked to inflammation. By inhibiting SIK activity, this compound increases anti-inflammatory cytokine IL-10 and decreases pro-inflammatory cytokine IL-12, demonstrating significant anti-inflammatory efficacy in a DSS-induced colitis model [1].