Inflammation/Immunology

Lithocholic acid is a toxic secondary bile acid that can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is also a FXR antagonist and a PXR/SXR agonist.

OVA Peptide(257-264) is a class I (Kb)-restricted peptide epitope of OVA, an octameric peptide can be from ovalbumin presented by the class I MHC molecule, H-2Kb.

Sphingosine-1-phosphate (S1P) is an agonist of S1P_1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca²⁺ as an extracellular ligand for G protein-coupled receptors. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids. Sphingosine-1-phosphate stimulates the DNA synthesis, cell proliferation and migration.

Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.

Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC₅₀ values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.

Baicalin, as a flavonoid glycoside, is an allosteric carnitine palmityl transferase 1 (CPT1) activator. Baicalin reduces the expression of NF-κB.

Indolelactic acid (Indole-3-lactic acid) is a tryptophan (Trp) catabolite in Azotobacter vinelandii cultures. Indolelactic acid has anti-inflammation and potential anti-viral activity.

Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the K_Ds of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the K_Ds of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research.

Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₅₀=1.13 μM).

Papain is a cysteine protease of the peptidase C1 family. Papain enhances red cell agglutination by anti-D and anti-A, and increases red cell sensitivity to K cell-mediated lysis in ADCC assays. Papain can induce pulmonary emphysema. Papain can be used for the researches of Rh haemolytic disease of the newborn and pulmonary emphysema.

Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist used clinically to treat type 2 diabetes mellitus.

EGTA is a cell-impermeant specific calcium ion chelator. EGTA has an apparent calcium dissociation constant (K_d) of 60.5 nM at physiological pH (7.4) and has very high specificity for Ca²⁺ over Mg²⁺ (Mg²⁺ K_d 1-10 mM). EGTA significantly inhibits the substrate adherence capacity of inflammatory macrophages.

GSK484 hydrochloride is a selective and reversible peptidylarginine deiminase 4 (PAD4) inhibitor. GSK484 hydrochloride demonstrates high affinity binding to PAD4 with IC₅₀s of 50 nM in the absence of Calcium. In the presence of 2 mM Calcium, notably lower potency (250 nM) is observed.

U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC₅₀of 1-2.1 µM for PLC.

Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.

Auranofin (SKF-39162) is a thioredoxin reductase (TrxR) inhibitor with an IC₅₀ of 0.2 μM. Auranofin exhibits antiviral activity against SARS-CoV21, with a CC₅₀ of 4.2 μM for monkey kidney Vero E6 cells.

Deucravacitinib (BMS-986165) is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC₅₀ of 0.2 nM and a K_i of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation. Deucravacitinib can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus.

Rituximab is an anti-CD20 chimeric monoclonal antibody used for research of certain autoimmune diseases and cancer.

Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC₅₀ of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation. Selumetinib can penetrate the blood brain barrier (BBB).

Calcimycin (A-23187) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin induces Ca²⁺-dependent cell death by increasing intracellular calcium concentration. Calcimycin inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin induces apoptosis and autophagy.