Inflammation/Immunology

Concanavalin A can be coupled to agarose to form Concanavalin A (agarose) (HY-P2149A). Concanavalin A (ConA) is a selective, competitive binding agent that targets specific carbohydrate structures containing glucose and mannose; it acts as a mitogen and exhibits varying degrees of cytotoxicity, hepatotoxicity, and teratogenicity. Concanavalin A is also utilized for in vivo blood glucose monitoring in the context of diabetes.

Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a K_i of 2 μM.

Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC₅₀ for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (K_d=0.1 nM). Doramapimod also inhibits B-Raf with an IC₅₀ of 83 nM.

Pilocarpine Hydrochloride is an orally active, selective M3 muscarinic acetylcholine receptor agonist. Pilocarpine Hydrochloride can induce seizures and is used in research on conditions such as epilepsy, dry mouth (xerostomia), and elevated intraocular pressure.

Nerandomilast (BI 1015550) is an orally active inhibitor of PDE4B with an IC₅₀ value of 7.2 nM. Nerandomilast has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD).

Propranolol is a nonselective and BBB-permeable β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.

Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.

ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-x_L and Bcl-w inhibitor with EC₅₀s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research.

Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.

SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits ¹²⁵I-IL-8 binding to CXCR2 with an IC₅₀ of 22 nM.

Polyinosinic-polycytidylic acid (Poly(I:C)) sodium is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis.

Orforglipron (LY3502970) (Compound 67) is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorates the type 2 diabete.

Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.

Spermine is a natural antioxidant and anti-inflammatory agent. Spermine is known to inhibit some bacterial cultures, especially strains of Staphylococcus aureus. Spermine can reversibly inhibits DNA synthetic response, mixed lymphocyte response and the induction of cytolytic lymphocyte response in primary cultures of murine spleen cells. Spermine is a polyamine nitric oxide donor that can provide nitric oxide to platelets and inhibit platelet activation to a certain extent concentration-dependently. Spermine occurs in mammalian tissues, plants, bacteria, ribosomes and bacteriophage. Spermine inhibits primary human embryo lung fibroblasts in vitro.

Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC₅₀ of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH.

GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC₅₀ of 1.8 nM, and inhibits kinase activity with an IC₅₀ of 1.3 nM. GSK-872 decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.

SIS3 is a potent and selective inhibitor of Smad3 with an IC₅₀ of 3 μM for Smad3 phosphorylation. SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.

Kifunensine, a potent and selective inhibitor of class I α-mannosidases isolated from Actinomycete, prevents α-mannosidases I from trimming mannose residues on glycoproteins. Kifunensine inhibits ERAD.

Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research.

Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice.