immune responses

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

Lipopolysaccharides (LPS) derived from Escherichia coli 055:B5, are a unique component of the cell wall of Gram-negative bacteria. They are composed of three regions: lipid A, oligosaccharide core, and O-specific polysaccharide (O-antigen). Lipopolysaccharides help maintain the integrity of the cell outer membrane and protect bacteria from damage by bile salts and lipid antibiotics. Lipopolysaccharides are highly immunogenic antigens that can enhance immune responses and can be used to construct inflammatory models.

Bindarit (AF2838)is an aryl hydrocarbon receptor (AHR) antagonist with IC50 of 39.9 nM in the human glioblastoma U87 cell line. BAY-218 inhibition of AhR stimulates pro-inflammatory monocyte and T cell responses in vitro and drives anti-tumor immune responses, leading to reduced tumor growth in vivo.

Dazostinag disodium (TAK-676) is a synthetic novel interferon gene (STING) agonist that triggers STING signaling pathway activation and type I interferon activation. Dazostinag disodium (TAK-676) is also a highly effective immune system modulator with complete resolution and lasting memory of T cell immunity and the ability to promote lasting interferon-dependent anti-tumor immune responses.

Cot inhibitor-1 is a selective inhibitor of Cot protein kinase (also known as Tpl2 or MAP3K8) (IC50 at 28 nM). Cot inhibitor-1 inhibited TNF-alpha production in human whole blood with IC50 of 5.7 nM. Cot is involved in a variety of cellular signaling pathways, particularly those involved in inflammation and immune responses. Cot inactivate-1 inhibits Cot activity and may have potential therapeutic effects on rheumatoid arthritis, inflammatory bowel disease and some types of cancer.

TASP 0277308 is a selective and potent inhibitor of sphingosine 1-phosphate receptor 1 ( S1P1) with immunomodulatory and anticancer activity that inhibits S1P- as well as VEGF-induced cellular responses and blocks VEGF-induced tube formation. TASP 0277308 is used in the study of immune and cardiovascular disorders.

STING agonist-30 is a potent activator of STING-dependent immune responses, demonstrating broad-spectrum antiviral effects against viruses such as HSV (Herpes Simplex Virus), rotavirus, and SARS-CoV-2 (Severe Acute Respiratory Syndrome Coronavirus 2).

Hydrocortisone (Cortisol) is a glucocorticoid hormone secreted by the adrenocortex. Hydrocortisone agonizes the glucocorticoid receptor, which promotes proteolytic metabolism, gluconeogenesis, capillary wall stabilization, and renal calcium excretion, as well as suppressing immune and inflammatory responses.

Inosine pranobex (Delimmun) has a number of immunomodulatory effects, including inducing T-lymphocyte differentiation, augmenting macrophage and NK cell functions, and stimulating IL-2 production. Through these effects and others, isoprinosine shows antiviral activity and has applications against subacute sclerosing panencephalitis. It also restores depressed immune responses in Y patients after irradiation and reduces the incidence of infection in leukemia patients undergoing chemotherapy. It is most commonly used to treat the rare measles complication subacute sclerosing panencephalitis in conjunction with intrathecal interferon therapy.

3-Indoleacrylic acid is a metabolite of tryptophan produced by Peptostreptococcus species. 3-Indoleacrylic acid has a beneficial effect on intestinal epithelial barrier function and mitigates inflammatory responses by immune cells.

Transglutaminase (TG) is a thiolase that induces intermolecular cross-linking of proteins, by catalysing the formation of isopeptide bonds between the γ-carboxamide group of glutamine residues and the primary ε-amine group of other compounds. The enzyme plays a role in a variety of physiological processes including coagulation, antimicrobial immune responses and photosynthesis.

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 TFA is the trifluoroacetate form of MC-Val-Cit-PAB-Amide-TLR7 agonist 4. MC-Val-Cit-PAB-Amide-TLR7 agonist 4 is a HER2-TLR7 and HER2- TLR8 immune agonist complexes with potential antitumor activity by activating the TLR7 and TLR8 signaling pathways and enhancing immune responses.

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.

Simeprevir (TMC435) is a potent HCV NS3 4A protease inhibitor, and inhibits HCV replication with EC50 of 8 nM.

1-Kestose shows significant anti-hydroxyl radical potential. 1-Kestose can promote intestinal Lactobacillus number, and influence the microorganisms as well as the intestinal and systemic immune responses.

BMS-986449 is a CELMoD-type molecular gel that remodels the function of regulatory T cells (Treg) and enhances their anti-tumor immune responses by directing the E3 ubiquitin ligase, Cereblon, to target the degradation of IKZF2 (Helios) and IKZF4 (Eos). BMS-986449 has potential application in the study of advanced solid tumors.

BBIQ is a powerful vaccine adjuvant that enhances innate immune responses and a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC50 of  59.1 nM for human TLR7.

3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid) is a bile acid metabolite that inhibits TH17 cell differentiation by directly binding to the transcription factor RORγt with a Kd of 1.13 μM.

Dusquetide TFA is a kind of innate defense regulator (IDR).Dusquetide TFA has been shown to be active in reducing inflammation and increasing clearance of bacterial infections.Dusquetide TFA regulates innate immune responses to PAMPs and DAMPs in combinat

3M-011, a potent dual toll-like receptor TLR7 8 agonist and cytokine inducer, serves as a powerful adjuvant to radiotherapy, eliciting significant local and systemic immune responses. Additionally, it effectively inhibits H3N2 influenza viral replication in the nasal cavity and exhibits strong antitumor activity[1][2][3].

Leukotriene B4 (LTB4) is a compound derived from arachidonic acid via the 5-lipoxygenase pathway that mediates certain inflammatory and immune responses. Leukotriene B4 induces neutrophil extracellular traps that impede the clearance of Pneumocystis japonicus.

RC529-MDP is an immunological adjuvant that couples Toll-like receptors (TLR4a) and NOD-like receptors (NOD2a) to enhance the innate immune response through the TLR4 and NOD2 signaling pathways. In mouse models, RC529-MDP induces high levels of the cytokine interleukin-related factor (IL-6), highlighting its immunostimulatory activity. Additionally, when injected into mice models with ovalbumin (OVA), RC529-MDP elevates OVA-specific antibody responses, T cell responses, and the proportion of memory T cells.

TLR7 8 agonist 11 (compound 30) serves as a powerful agonist for hTLR7 and hTLR8, exhibiting EC50 values of 31.1 nM and 13.1 nM, respectively. This compound is crucial in the functioning of both adaptive and innate immune responses.

AJI-214 functions as a dual-target inhibitor that specifically blocks Aurora kinase A and JAK2. By directly inhibiting Aurora kinase A, AJI-214 prevents mitotic progression and cell polarity in T cells while concurrently suppressing JAK2 activation to reduce STAT3 phosphorylation. This inhibition decreases the differentiation of TH1 and TH17 cells. AJI-214 is utilized in research focused on the modulation of immune responses and the prevention of graft-versus-host disease (GVHD).