Telazorlimab (GBR-830) is a humanized monoclonal antibody against OX40 costimulatory receptor on activated T cells. Telazorlimab can be used for the research of autoimmune diseases[1].
SCH28080 inhibits gastric H+/K+-ATPase by K+-competitive binding, with an IC50 value of 20 nM in rabbit microsomal membranes[1]. Antisecretory and cytoprotective activities[2].
OVA-E1 peptide TFA, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes[1].
NLRP3-IN-21 (compound L38) is a NLRP3 inflammasome inhibitor with inflammatory properties. NLRP3-IN-21 inhibits NLRP3 inflammasome activation and pyroptosis by suppressing gasdermin D cleavage, ASC oligomerization, and NLRP3 inflammasome assembly[1].
Trans substituted cephalosporin is an effective NDM-1 inhibitor，with an IC50 value of 0.13 μM.
Y 9000 is an orally active anti-allergic agent [1].
Alcaftadine-D3 (R89674-D3) is a deuterium labeled Alcaftadine. Alcaftadine (HY-17039) is a H1 histamine receptor antagonist[1].
Foralumab (NI-0401) is a potent, orally active humanized monoclonal antibody targeting the CD3. Foralumab modulates immune responses by human cells in NSG mice that were reconstituted with human hematopoietic stem cells[1].
AZD9898 is an orally active leukotriene-C4 synthetase (LTC4S, glutathione S-transferase II) inhibitor, with an IC50 of 0.28 nM. AZD9898 mitigates the GABA binding and hepatic toxicity signal. AZD9898 has the potential to treat asthma[1].
Vidofludimus(4SC-101; SC12267) is a novel immunosuppressive drug that inhibits DHODH; inhibits IL-17 secretion in vitro independently of effects on lymphocyte proliferation.IC50 value:Target: DHODH inhibitorin vitro: 4SC-101 is a potent inhibitor of human DHODH, inhibits lymphocyte proliferation, and uniquely blocks phytohemagglutinin-stimulated IL-17 production by lymphocytes [2].in vivo: In vivo Vido treatment alone most effectively reduced macroscopic and histological pathology and the numbers of CD3+ T cells. In contrast, similarly reduced nuclear signal transducer and activator of transcription 3 (STAT3) binding and IL-17 levels were observed from animals treated with Vido alone and Vido + Uri. Vido improves TNBS-induced colonic inflammation by a unique dual mode of action [1]. Oral administration of 4SC-101 effectively improved both chronic DSS and acute TNBS colitis in mice. In these colitis models the overall efficacy profile of 4SC-101 was similar to that of dexamethasone [2].
BPU-11 is a hyperpolarization-activated cyclic nucleotide-gated (HCN) C-linker pocket (CLP) HCN4 CLP ligand. BPU-11 can be used for the research of congenital immune disease[1].
Methyl arachidate (Methyl eicosanoate), a natural compound, is a leukotriene A4 hydrolase (LTA4H) inhibitor[1].
ShK-Dap22 is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 is a selective Kv1.3 channel blocker with IC50s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively[1].
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties[1][2]. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca2+, and markedly decreases iNOS protein expression[3].
Tofacitinib-d3 (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
GLPG1690 is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and Ki of 15 nM.
Navafenterol (AZD-8871) saccharinate is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile[1].
MMP13-IN-31f is a highly potent, selective, orally bioavailable MMP-13 inhibitor with IC50 of 0.036 nM; exhibits 5,000-fold selectivity for MMP-13 over MMP-2, >1,500-fold selectivity over MMP-10, and >27,000-fold selectivity over MMP-1, 3, 7, 8, 9, 14, and TACE; prevents IL-1/OSM induced in vitro degradation of BNC (70.8% inhibition of cartilage degradation at 1 µM).
Carmine (Carmine red), a "semi-synthetic" dye, is a complex of aluminum and the natural dye Cochineal (Carminic acid). Cochineal is isolated from the native Mexican and South American insect. Carmine is a widely used "natural" food additive. Carmine provokes both an immediate hypersensitivity and a delayed systemic response with cutaneous expression[1][2].
Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM.
CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3.
Lymecycline is a tetracycline derivative, with broad-spectrum antibacterial activity and also has anti-inflammatory property.
Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl- competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain[1][2].
3'-Sialyllactose (3'-SL) sodium is a prebiotic, maintains immune homeostasis and exerts anti-inflammatory and anti-arthritic effects. 3'-Sialyllactose sodium is an ordinary carbohydrate with the lowest toxicity rating, it can be used for the research of inflammation[1][2][3].
Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen[1].
Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering with the activity of DNA polymerase[1].Aphidicolin is an antibiotic produced by the mold Cephalosporium aphidicola. Aphidicolin is a potent inhibitor of cellular deoxyribonucleic acid synthesis and inhibits the growth of herpes simplex virus[2].Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line[3].
Nangibotide is a TREM-1 receptor inhibitor that can modulate innate immune response. Nangibotide can reduce systemic and in situ inflammatory reaction in rodent models of myocardial ischaemia‐reperfusion[1].
N-(3-Oxodecanoyl)-L-homoserine lactone (3-Oxo-C10-HSL) is a bacterial quorum sensing signal autoinducer molecule[1].
sPLA2 inhibitor 1, a D-tyrosine derivative, is an orally active, potent secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 29 nM for human nonpancreatic secretory PLA2 isoform IIa (hnpsPLA2-IIa). sPLA2 inhibitor 1 has anti-inflammatory activity[1].
CID-1067700 is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.