inflammatory factors

Naphazoline hydrochloride (Naphazoline HCl) is an adrenergic vasoconstrictor agent used as a decongestant.

Hydrangenol is a natural product and can be isolated from Hydrangea serrata leaves. Hydrangenol is an antiphotoaging compound with oral activity. Hydrangenol can reduce MMP and inflammatory cytokine expression and increase moisturizing factors and antioxidant genes level, result in preventing wrinkle formation.

Ciclopirox (HOE296b) exerts its action by binding to and chelating trivalent cations, such as Fe3+ and Al3+, thereby inhibiting the availability of essential co-factors for enzymes. Ciclopirox is a synthetic, broad-spectrum antifungal agent with additional antibacterial and anti-inflammatory activities. This may lead to a loss of activity of enzymes that are essential for cellular metabolism, the organization of cell wall structure and other crucial cell functions. In addition, ciclopirox exerts its anti-inflammatory activity by inhibiting 5-lipoxygenase and cyclooxygenase (COX).

Isotretinoin (13-cis-Retinoic acid) binds to and activates nuclear retinoic acid receptors (RARs), which act as transcription factors that promote cell differentiation and apoptosis. This naturally occurring retinoic acid has potential antineoplastic activity, exhibits immunomodulatory and anti-inflammatory responses, and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization.

Allicin exerts antioxidant, bactericidal, anti-cancer, anti-inflammatory activities, it exerts an inhibitory immunomodulatory effect on intestinal epithelial cells. Allicin could significantly inhibit vascular smooth muscle cells' proliferation and migration induced by insulin, which may be related to the inhibition of the activation of ERK signal path. Allicin is beneficial in reducing blood cholesterol, triglycerides levels and systolic blood pressure in hypercholesterolemic rats, it may beneficially affect two risk factors for atherosclerosis-hyperlipidemia and hypertension.

2',3'-cGAMP is an endogenous cyclic dinucleotide (CDN) produced by cGAS (cGAMP synthase) in response to double-stranded DNA in the cytoplasm. It acts as a STING activator and ligand, inducing interferons (IFNs) via the TBK1/IRF3 pathway and pro-inflammatory factors via the NF-κB pathway.

AZ12601011 is an orally active, selective and potent TGFBR1 kinase inhibitor.AZ12601011 inhibits the release of inflammatory factors, interleukin (IL)-1β, IL-6 and tumor necrosis factor-α, and inhibits the growth of breast tumors.AZ12601011 directly binds to TGF-βR1 and blocks downstream Smad3 activation, which can be used to prevent renal fibrosis.

Thalifendine is one of the main products of Berberine demethylation catalyzed by CYP51 (secreted by intestinal flora), which has anti-inflammatory effects, reduces intestinal inflammation, improves intestinal barrier function, and reduces the production of inflammatory factors.

SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively. SB-657510 plays an anti-inflammatory role by inhibiting UII-induced inflammatory mediators, such as adhesion molecules, in human vascular endothelial cells and upregulation of cytokines and tissue factors. SB 657510 has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models.

Triphenyl phosphate is an organophosphorus flame retardant and endocrine disruptor that activates MAO-A/ROS/NF-κB pathways, disrupting placental tryptophan metabolism and inducing abnormal neurobehavioral effects. It also promotes oxidative stress via inflammatory mediators including NF-κB, IL-6, and TNF-α.

X-17 is a potent Vanin-1 inhibitor known for its anti-inflammatory and antioxidant properties. It reduces the expression of inflammatory factors and inhibits myeloperoxidase activity, while enhancing colonic glutathione reserves and restoring the intestinal barrier.

IAV replication-IN-1 (compound 3h) can reduce the upregulation of inflammatory factors and apoptosis caused by IAV infection and alleviate lung damage resulting from IAV infection.

FKK6 is a selective agonist of the pregnane X receptor (PXR) with an EC50 of 1.2 µM. It demonstrates strong affinity for plasma proteins and exhibits favorable metabolic characteristics in human microsomes. FKK6 inhibits the PXR-related NF-κB signaling pathway, reducing the expression of inflammatory factors and showing anti-inflammatory activity in a mouse model of DSS-induced colitis.

SI-W052 is an orally active, brain-penetrant, and selective small molecule inhibitor that targets mTOR and TEX264. It activates autophagy by inhibiting mTOR phosphorylation, enhances TEX264 expression to promote endoplasmic reticulum renewal, and suppresses the release of LPS-induced inflammatory factors (TNF-α, IL-6). SI-W052 shows potential for research into neuroinflammation associated with Alzheimer's disease (AD).

SIK2-IN-3 is an orally active selective inhibitor of SIK1/2 with IC50 values of 0.128/0.084 μM. It hinders the phosphorylation of CRTC3 and suppresses the production of pro-inflammatory factors in myeloid cells. Additionally, SIK2-IN-3 alleviates systemic and tissue inflammatory responses in a mouse anti-CD40 colitis model.

β2AR agonist 4 (compound A19) is an effective selective agonist for the β2-adrenoceptor (β2-Adrenoceptor), exhibiting an EC50 of 3.7 pM. In a rat model with COPD, β2AR agonist 4 reduces the elevation of inflammatory factors and leukocytes, thereby improving lung function.

Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC50: 0.55 μM), effectively blocking HIF-1 signaling and promoting the degradation of HIF-1α. It inhibits synovial invasion and migration, as well as angiogenesis. In mouse inflammation models, Anti-inflammatory agent 79 effectively reduces foot swelling and arthritis and lowers levels of inflammatory factors and angiogenesis in vivo.

Anti-inflammatory agent 88 (compound 6) is a carbazole derivative found in marine Streptomyces with anti-inflammatory properties. It exerts its effects by inhibiting pro-inflammatory factors and enhancing the expression of anti-inflammatory factors within the Myd88/Nf-κB pathway. This compound holds potential for the development of anti-inflammatory drugs.

TBK1degrader-4 (Compound 30) is a molecular glue degrader targeting TBK1. It effectively inhibits cyst growth, reduces inflammation, and lowers levels of pro-inflammatory factors such as Ccl2, IFNβ, and IL-6. TBK1degrader-4 shows potential for research in autosomal dominant polycystic kidney disease (ADPKD).

PPARδ agonist12 (compound 25) is a PPARδ agonist that inhibits the production of inflammatory factors and nitric oxide. Additionally, PPARδ agonist12 effectively prevents macrophage infiltration into inflamed areas, making it useful for inflammation research.

HTS05585 (Compound Hit-1) is a selective inhibitor of macrophage migration inhibitory factor (MIF) with a Kd value of 0.29 μM determined by microscale thermophoresis (MST) and confirmed through isothermal titration calorimetry (ITC) at 0.32 μM. It suppresses the release of pro-inflammatory factors (TNF-α, IL-6, IL-1β) in macrophages induced by LPS, making it a promising candidate for the study of inflammatory diseases such as sepsis.

RJG-2036 is a potent covalent inhibitor of human prostaglandin reductase 2 (PTGR2) with an IC50 of 100 nM. It effectively inhibits NADPH-dependent reduction reactions, significantly reducing the secretion of inflammatory factors such as TNF-α and the release of various pro-inflammatory eicosanoids in LPS-stimulated THP-1 macrophages. RJG-2036 shows promise for research in inflammatory diseases.

endo-S-cGAFMP (Compound 3) is a STING agonist that enhances both innate and adaptive immune responses by activating the cGAS-STING pathway, leading to the production of interferon regulatory factors and pro-inflammatory cytokines. It exhibits strong immunostimulatory activity in THP1 monocytes and RAW macrophages, with EC50 values of 2.45 μM and 5.54 μM, respectively. endo-S-cGAFMP also demonstrates significant antitumor activity and holds potential as an immunotherapy agent for cancer, particularly in studies involving systemic administration.

CW8001 is a covalent Exportin-1 (XPO1) inhibitor with an EC50 value of 1 nM for inhibiting T cell activation. It prevents the nuclear localization of NFAT transcription factors, thereby suppressing the expression of inflammatory cytokines like IL-2. CW8001 shows potential for research in T cell-driven immune diseases such as graft-versus-host disease (GVHD).