L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype[1].
Benmelstobart is an IgG1κ antibody targeting PD-L1/CD274, derived from mice[1].
Ebastine-d5 (LAS-W 090-d5) is the deuterium labeled Ebastine. Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research[1][2].
Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis.
Balsalazide-d4 is deuterium labeled Balsalazide. Balsalazide could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
PD-1/PD-L1-IN-33 (Compound N11) is a PD-1/PD-L1 inhibitor. PD-1/PD-L1-IN-33 inhibits PD-1 and PD-L1 interaction with an IC50: 6.3 nM. PD-1/PD-L1-IN-33 promotes T-cell proliferation, activation, and infiltration into tumor spheres. PD-1/PD-L1-IN-33 has immunomodulatory and anticancer activity[1].
Astemizole, a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has anticholinergic and antipruritic effects[1][2].
Roxatidine acetate is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine acetate has antisecretory potency against gastric acid secretion. Roxatidine acetate can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine acetate has antitumor activity[1][2][3].
Opucolimab is an anti-PD-L1 recombinant human monoclonal antibody. Opucolimab can be used to synthesis antibody drug conjugates. Opucolimab can be used for the research of advanced solid tumors[1].
Izokibep (ABY-035) is a selective and antibody mimetic interleukin 17A (IL-17A) inhibitor with high potency and long half-life. Izokibep can be used for the research of ankylosing spondylitis, atherosclerosis and skin disease[1].
Theophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) monohydrate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) monohydrate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) monohydrate induces apoptosis. Theophylline (1,3-Dimethylxanthine) monohydrate can be used for asthma and chronic obstructive pulmonary disease (COPD) research[1][2][3][4][5].
Factor B-IN-2 (Example 1 target compound) is a potent complement factor B inhibitor, with an IC50 of 1.5 μM. Factor B-IN-2 can be used for the research of diseases related to inflammation and immunity[1].
CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3+ T lymphocytes into the Pan02 tumor tissues[1].
Eltrombopag methyl ester is a derivative of Eltrombopag, which is a thrombopoietin (Tpo) receptor agonist, which can promote platelet production and is used in research related to specific types of thrombocytopenia[1].
GSK1795091 (CRX-601), an immunologic stimulator, is a synthetic TLR4 agonist. Antitumor activity. GSK1795091 can be used as a vaccine adjuvant to enhance both mucosal and systemic immunity to influenza virus vaccines[1][2].
TLR8 agonist 2 is a potent and selective TLR8 agonist with an EC50 of 3 nM for human TLR8. TLR8 agonist 2 shows less active against human TLR7 (EC50 of 33.33 μM)[1].
CXCR4 antagonist 8 (Compound 3) is a CXCR4 antagonist with an IC50 of 57 nM. CXCR4 antagonist 8 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 0.24 nM. CXCR4 antagonist 8 inhibits CXLC12/CXCR4 mediated cell migration[1].
Dectrekumab (QAX576) is a humanized monoclonal antibody that targets IL-13. Dectrekumab significantly improves intraepithelial esophageal eosinophil counts and dysregulated esophageal disease-related transcripts with Eosinophilic esophagitis (EoE) in a sustained manner and can be used for inflammation and immunology related research[1].
Doxepin D3 Hydrochloride is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant used as a sedative. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2[1][2].
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively[1].
COX-2-IN-18 (Compound 3) is a potent inhibitor of COX-2. COX-2-IN-18 possesses good COX-2 inhibitory activity (IC50 = 0.775 μM) compared to the reference drug, Celecoxib (IC50 = 0.153 μM). COX-2-IN-18 has the potential for the research of cancer diseases[1].
Olamkicept (FE 999301) is a selective inhibitor of the soluble interleukin 6 (sIL-6R)/IL-6 complex. Olamkicept is a soluble gp130-Fc-fusion-protein and anti-inflammatory agent[1][2].
Tagraxofusp (SL-401) is a potent IL-3 receptor inhibitor to inhibits plasmacytoid dendritic cells (pDCs) growth in multiple myeloma (MM) bone marrow (BM) microenvironment. Tagraxofusp has synergistic effect with Bortezomib (HY-10227) and Pomalidomide (HY-10984) to suppress multiple myeloma (MM)[1].
Roburic acid, a tetracyclic triterpenoid found in Gentiana macrophylla, acts as an inhibitor of COX, with IC50s of 5 and 9 μM for COX-1 and COX-2, respectively[1].
Plozalizumab (MLN-1202) is a specific humanized anti-CCR2 antibody. Plozalizumab can be used for malignant melanoma research[1].
COX-2-IN-11 (compound 7b2) is a potent and selective inhibitor of COX-2. COX-2-IN-11 has the potential for the research of inflammation diseases[1].
PD-1/PD-L1-IN-21 (Example 22) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-21 blocks PD-1/PD-L1 with the IC50 of 4.99 μM. PD-1/PD-L1-IN-21 can be used for the research of cancers, infectious diseases and autoimmune diseases[1].
TLR7 agonist 8 (compound IIb-34) is an TLR7 agonist with an EC50 value of ~4 nM[1].
(±)-Catechin (rel-Cianidanol) is the racemate of Catechin. (±)-Catechin has two steric forms of (+)-Catechin and its enantiomer (-)-Catechin. (+)-Catechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM. Anticancer, anti-obesity, antidiabetic, anticardiovascular, anti-infectious, hepatoprotective, and neuroprotective effects[1].
TLR8 agonist 2 hydrochloride is a potent and selective TLR8 agonist with an EC50 of 3 nM for human TLR8. TLR8 agonist 2 hydrochloride shows less active against human TLR7 (EC50 of 33.33 μM)[1].