Potent, selective agonist of Mu-opioid receptor. Antinociceptive. Stimulates calcium-activated adenylyl cyclases related cAMP production. Expresses chemokines and chemokine receptors through TGF-beta1. Increases food intake of rats.

3-Hydroxykynurenamine, also known as 3-Hydroxy-L-kynurenamine or 3-HKA, is a biogenic amine produced via an alternative pathway of tryptophan metabolism. In vitro, 3-HKA has an anti-inflammatory profile by inhibiting the IFN-γ mediated STAT1/NF-κΒ pathway in both mouse and human dendritic cells (DCs) with a consequent decrease in the release of pro-inflammatory chemokines and cytokines, most notably TNF, IL-6, and IL12p70. 3-HKA has protective effects in an experimental mouse model of psoriasis by decreasing skin thickness, erythema, scaling and fissuring, reducing TNF, IL-1β, IFN-γ, and IL-17 production, and inhibiting generation of effector CD8+ T cells. Similarly, in a mouse model of nephrotoxic nephritis, besides reducing inflammatory cytokines, 3-HKA improves proteinuria and serum urea nitrogen, overall ameliorating immune-mediated glomerulonephritis and renal dysfunction.This compound is unstable in powder form and other related salt forms are recommended.

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630/624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20/2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

Murabutide, a safe synthetic immunomodulator, diminishes the expression of CD4 and CCR5 receptors and promotes the secretion of high levels of beta-chemokines, thereby enhancing nonspecific resistance to viral infections. It does not impact virus entry, reverse transcriptase activity, or the formation of early proviral DNA in the cytoplasm of infected cells [1].

Antileukinate is a synthetic hexapeptide with an acetylated amino terminus and an amidated carboxyl terminus that inhibits the binding of CXC chemokines to the chemokine receptor CXCR2. It inhibits IL-8 binding to neutrophils (Ki = 2.7-13 μM), prevents neutrophil chemotaxis and β-glucuronidase release, and blocks IL-8-induced skin edema in rabbits. At 53 mg/kg, antileukinate has been shown to protect mice against acute pancreatitis and associated lung injury.

AMG 487 is an effective and selective antagonist of chemokine receptor 3. AMG 487 inhibited CXCR3-mediated cell migration induced by three CXCR3 chemokines, IP-10, ITAC and MIG (IC50: 8, 15 and 36 nM, respectively).

GA-O-02, an 18β-Glycyrrhetinic acid (GA) derivative, functions as a powerful antimicrobial and anti-inflammatory agent. This compound inhibits NO, pro-inflammatory cytokines, and chemokines to exert its anti-inflammatory effects. Additionally, GA-O-02 demonstrates significant antimicrobial activity against Gram-positive bacteria.

PB118 has the capacity to effectively clear Aβ deposits by augmenting phagocytosis, enhance the tubulin/microtubule network through increased acetyl α-tubulin levels, modulate various inflammation-associated cytokines and chemokines, and notably diminish phospho-tau (p-tau) levels linked to Alzheimer's disease (AD). The IC50 of PB118 for HDAC6 is 5.6 nM.

Ergosta-7,22-dien-3-one is a lanosterane that can be isolated from the substrates of Ganoderma taiwanensis.Ergosta-7,22-dien-3-one has pro-inflammatory properties, it stimulates nitric oxide production, induces gene expression, and induces the production of TLRs, cytokines, chemokines, and cellular adhesion molecules.

KS370G (Caffeic Acid Phenethyl Amide) inhibits UUO-induced renal fibrosis marker expression. KS370G is an orally active hypoglycemic and cardioprotective agent that reduces collagen deposition in obstructed kidneys and significantly decreases renal expression of inflammatory chemokines/adhesion molecules and monocyte markers and improves left ventricular hypertrophy and function in the heart of pressure-overloaded mice.KS370G can be used to study renal obstructive nephropathy.

DPP-4-IN-8 (compound 27) is a potent and selective inhibitor of dipeptidyl peptidase 4 (DPP4), with an inhibition constant (Ki) of 0.96 μM. It inhibits the dipeptidase activity of DPP4 in both Caco-2 and HepG-2 cells and dose-dependently reduces the expression of chemokines such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β) [1].

IMMH001, also known as SYL930, is an orally active compound that exhibits potent selectivity as an agonist for the S1P1 receptor, which is the sphingosine-1-phosphate receptor 1. This compound effectively reduces the levels of various chemokines and proinflammatory cytokines, such as IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 finds utility in research focused on rheumatoid arthritis (RA) [1] [2].

Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.

TMC353121 is a respiratory syncytial virus (RSV) fusion inhibitor with anti-RSV activity that inhibits the production of the inflammatory cytokines TNF-α, IL-6, and IL-1β, as well as chemokines, KC, IP-10, MCP, and MIP1-α.

K 76 Carboxylic acid effectively blocks human complement from forming tumor cell chemokines.

GA-O-06, an 18β-Glycyrrhetinic acid derivative, serves as a potent antimicrobial and anti-inflammatory agent. It achieves its anti-inflammatory effects by inhibiting NO, pro-inflammatory cytokines, and chemokines, while demonstrating significant antimicrobial activity against Gram-positive bacteria.

Noricaritin, a flavonoid derived from Epimedium root, induces cell proliferation in lung tissue and inhibits the production of pro-inflammatory cytokines and chemokines in human lung epithelial cells.

Valencene (NSC-148969) is a sesquiterpenoid isolated from Cyperus rotundus and is an aroma component of citrus fruits and citrus-derived odors.ValenceneValencene has anti-allergic, anti-inflammatory, anti-melanogenic, and antioxidant activities. Valencene inhibits the overexpression of Th2 chemokines and pro-inflammatory chemokines by blocking the NF-κB pathway.

Myristicin (Myristicine) is a natural product found in spices and umbelliferous plants. Myristicin has anti-cholinergic, Antibacterial, and hepatoprotective effects, it also has anti-inflammatory properties related with its inhibition of NO, cytokines,chemokines, and growth factors in dsRNA-stimulated macrophages via the calcium pathway. Myristicin can induce Apoptosis as characterised by alterations in the mitochondrial membrane potential, cytochrome c release, Caspase-3 activation, PARP-cleavage and DNA fragmentation.

CCR2 antagonist 4 (Teijin compound 1) is a potent and specific antagonist of CCR2(IC50s of 180 nM), and potently inhibits MCP-1-induced chemotaxis(IC50 of 24 nM).

IDR-1 is an antimicrobial peptide with activity against both Gram-positive and Gram-negative bacteria. This compound modulates innate immunity to counter infections while avoiding evident toxicities. Additionally, IDR-1 exhibits anti-inflammatory and anti-infective properties, increases the levels of monocyte chemokines, and reduces the release of pro-inflammatory cytokines.

Tirotundin is a PPARα/γ dual agonist, it exerts anti-diabetic effect through PPARγ pathway. It shows anti-inflammatory activity, it inhibits inhibit the activation of NF-kappa B, thereby, the synthesis of inflammatory mediators such as cytokines and chemo