immune

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.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

KA2507 is a potent and selective HDAC6 inibitor with an IC50 of 2.5nM.

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.

Immune cell migration-IN-1 (compound 2) is a potent inhibitor of immune cell migration and has potential research applications for mitigating conditions like dry eye diseases, eczema dermatitis, and psoriasis [1].

Immune cell migration-IN-2 is a potent inhibitor of immune cell migration, exhibiting an EC50 value of 13.5 nM in a T-cell adhesion assay. This compound is utilized in research pertaining to dry-eye and other retinal diseases [1]. As a click chemistry reagent, Immune cell migration-IN-2 possesses an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.

BMS-1 (PD-1 PD-L1 inhibitor 1) is an inhibitor of the PD1-PD-L1 protein-protein interaction. It also acts as an immunomodulator. Programmed death ligand 1 (PD-L1) is a protein in humans that is encoded by the CD274 gene and the upregulation of PD-L1 allows Ys to evade the host immune system. High tumor expression of PD-L1 was associated with increased tumor aggressiveness and a 4.5-fold increased risk of death.

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.

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

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.

D18 is an immune modulator that acts as a dual agonist for TLR7 8 (with EC50 values of 24 nM for hTLR7 and 10 nM for hTLR8, respectively). It enhances the expression of PD-L1 through epigenetic regulation, thereby increasing the sensitivity of tumors to PD-1 PD-L1 blockade. Additionally, D18 functions as a cytotoxin for ADC synthesis, specifically for the ADC HE-S2 [1].

BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) PD-Ll (Programmed death-ligand 1) protein protein interaction.

Sirpiglenastat (DRP-104), a glutamine antagonist and prodrug of DON, exhibits antitumor activity by inhibiting glutamine metabolism and stimulating both the innate and adaptive immune systems.

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.

SR-717 is a cGAMP analog, a non-nucleoside STING agonist that induces a closed activation conformation of STING. SR-717 has antitumor activity and promotes activation of immune cells and cross-presentation of antigens.

Astragaloside IV (AS-IV), an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1 2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine.1 It dose-dependently inhibits human adenovirus type 3 (HAdV-3) in A549 cells (IC50 = 23 μM; LC50 = 865 μM).It inhibits replication of HAdV-3 and decreases HAdV-3-induced apoptosis. It has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems. In particular, it reduces myocardial infarct size in dogs when administered prior to coronary ligation and reduces reperfusion arrhythmias in isolated rat hearts.

Penicillamine (Artamine), possessing antineoplastic properties, induces apoptosis by a p53-mediated mechanism and inhibits angiogenesis by chelating with copper, a cofactor for angiogenesis. Artamine is a beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, Artamine chelates with heavy metals and increases their urinary excretion.

Evodenoson (ATL313) is a potent and selective adenosine A2a receptor (A2aR) agonist for the treatment of eye diseases, tumors, and immune system disorders, and may be used in studies of open-angle glaucoma and blood tumors.

Edralbrutinib (TG-1701) is a potent BTK inhibitor with anticancer activity used in treating tumors, immune system disorders, and blood and lymphatic system disorders. Additionally, Edralbrutinib is studied for its efficacy in membranous glomerulonephritis and optic neuromyelitis optica.

PPTN is a high-affinity, competitive and highly selective antagonist of P2Y14 receptor(KB value of 434 pM), with anti-inflammatory and immune activity.

Tresperimus TFA can be used as an immune agent and can be used to study retinitis.

RS 0481 modulates the immune response and rebuilds lymphocyte populations damaged by tumor growth in animals.

CGS8216 is a benzodiazepine receptor antagonist that shows analgesic activity at high doses.CGS8216 has anxiolytic activity and may be used to study immune system disorders.

AVP-13358 is a CD23 antagonist (immunoglobulin ε-Fc receptor antagonist), an immunoglobulin E inhibitor. AVP-13358 has potent activity against IgE, cytokines and CD23 and is used in the treatment of immune system disorders, infections and otolaryngological disorders.