immunological

CL097 is an effective agonist of TLR7 and TLR8. CL097 induces pro-inflammatory cytokines in macrophages and NADPH oxidase priming, thereby increasing the fMLF-stimulated ROS production.

Sodium Hydrogen Sulfide (hydrate) is, like nitric oxide, an important gaseous mediator that has significant effects on the immunological, neurological, cardiovascular and pulmonary systems of mammals. Sodium Hydrogen Sulfide (hydrate) is an H2S donor commonly used in cellular and whole animal experimental systems. For example, it has been used to suggest that H2S promotes neutrophil migration, reduces airway inflammation, and protects neurites, heart, and intestine from chemical or ischemic-reperfusion damage.

Tyramine hydrochloride is a biogenic trace amine that is generated via the decarboxylation of the amino acid tyrosine, exhibiting neuromodulatory properties as well as cardiovascular and immunological effects.

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.

VUF10460, a non-imidazole histamine H4 receptor agonist, [58C8-51-20-3] is structurally classified under the chlorobenzylpiperazine ethers with the IUPAC designation (2-[(2-chlorophenyl)methyl]-1-piperazinyl)(1H-indol-3-yl)methanone. It is typically utilized in pharmacological research and exhibits specificity for the H4 subtype, making it a valuable tool in immunological studies.

Tacalcitol (1,24(R)-Dihydroxyvitamin D3; 1.alpha.,24R-Dihydroxyvitamin D3) promotes normal bone development by regulating calcium and modulates immunological and inflammatory processes.

SM360320 (CL-087) is an effective and selective agonist of TLR7. SM360320 inhibits HCV replication in hepatocytes via a type I IFN-independent mechanism in addition to its IFN-mediated activity. SM360320 can be used for research on acting as an immunological adjuv

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.

AYK004-C1 is a TLR agonist used in the formulation of immunological adjuvants.

Monophosphoryl lipid A (free acid) acts as an agonist for toll-like receptor 4. It is employed in immunological and vaccine research.

AYK004-B1, a TLR7 agonist (EC50=0.2265 nM), can be utilized in the formulation of immunological adjuvants.

DHT KLH is a coupling compound for immunological studies, consisting of dihydrotestosterone (DHT) antigen bound to a hemocyanin (KLH) adjuvant, a commonly used carrier protein that enhances the immunogenicity of the antigen. It is widely used to prepare specific antibodies for the study of androgen receptor-associated immune responses.

Ginkgolide A (BN-52020) is a highly active PAF antagonist cage molecule isolated from Ginkgo biloba leaves, showing potential in various inflammatory and immunological disorders.

N-Retinoylleucine has less toxicity and has similar immunological effects as retinoic acid.

Dehydro warfarin, a metabolite of (±)-warfarin, is formed by rat liver microsomes from (±)-warfarin.

1,3,4,6-Tetra-O-acetyl-2-azido-2-deoxy-α-D-mannopyranose is an analog of N-acetylmannosamine (ManNAc) and a building block. It has been used as a precursor in the synthesis of differently substituted trimers of the group A [N. meningitidis] capsular polysaccharide repeating unit for immunological experiments. It has also been used in the synthesis of fluorescent probes for lysosomal labeling.

NTPDase-IN-2 (compound 5g) selectively inhibits NTPDase-2 and NTPDase-8 with IC50 values of 0.04 µM and 2.27 µM, respectively, and exhibits non-competitive inhibition toward h-NTPDase-1 and h-NTPDase-2, with a Km of 74 µM for h-NTPDase-2. This compound is applicable in researching cancer, immunological disorders, and bacterial infections [1].

STING Agonist-13, a stimulator of interferon genes (STING) agonist, enhances cancer immunity through STING-mediated immune activation. It activates STING downstream signaling to promote type I interferon immune responses, significantly reduces tumor volume, and exhibits immunological memory-derived cancer inhibition [1].

STING modulator-5 (compound 38), a STING modulator, exhibits a pIC50 value of 9.5 and antagonizes peripheral blood mononuclear cells (PBMC) with a pIC50 value of 8.1. Additionally, it acts as an antagonist of THP-1 cells, making it applicable in immunological disease research [1].

CL845, a STING (stimulator of interferon genes) agonist analog to CL656, is instrumental in synthesizing conjugatable PRR (pattern recognition receptor) ligands aimed at targeting STING. It holds potential applications in researching cancers, immunological disorders, or infections [1].

Imsamotide (IDO194-214), an Indoleamine 2,3-Dioxygenase (IDO) peptide characterized by the sequence DTLLKALLEIASCLEKALQVF (IDO194-214), functions as both an immunological agent for active immunization and an antineoplastic agent [1] [2].

Mofebutazone inhibits the immunological release of prostaglandins as well as leukotrienes.

Odulimomab (anti-LFA1), an anti-LFA-1 monoclonal antibody, inhibits T lymphocyte proliferation and provides protection against ischemia and reperfusion injury. It is utilized in researching transplant rejection and immunological diseases [1] [2].

PI5P4Kα-IN-1 (Compound 13) is a phosphatidylinositol 5-phosphate 4-kinase (PI5P4K) inhibitor with IC50 values of 2 μM for PI5P4Kα and 9.4 μM for PI5P4Kβ, potentially applicable in cancer, metabolic, and immunological disorder studies [1].