Inflammation/Immunology

Ascomycin (Immunomycin; FR-900520; FK520) is an ethyl analog of Tacrolimus (FK506) with strong immunosuppressant properties. Ascomycin is also a macrocyclic polyketide antibiotic with multiple biological activities such as anti-malarial, anti-fungal and anti-spasmodic. Ascomycin prevents graft rejection and has potential for varying skin ailments research.

APX-115 (Ewha-18278) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with K_i values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 effectively prevents kidney injury.

CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2^DHR-2 for Rac1 in a dose-dependent manner with an IC₅₀ of 22.8 µM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9.

MRS 1754 is a selective antagonist radioligand for A_2B adenosine receptor with very low affinity for A₁ and A₃ receptors of both humans and rats.

Fremanezumab (TEV-48125) is a humanized lgG2 monoclonal antibody that selectively and potently binds to calcitonin gene related peptide (CGRp) (IC₅₀ values = 7.943 nM). Fremanezumab binds to mouse CGRP with an IC₅₀ value of 19.6 nM. Fremanezumab counteracts anti-inflammatory effects of CGRP in vitro, including CGRP-mediated inhibition of LPS (HY-D1056)-induced microglial activation. Fremanezumab selectively inhibits the activation of Aδ meningeal nociceptors by cortical spreading depression (CSD) in rats. Fremanezumab can be used for the study of inflammation and chronic migraine.

RCM-1 is a forkhead box M1 (FOXM1) inhibitor with an EC₅₀ of 0.72 μM in U2OS cells. RCM-1 blocks the nuclear localization and increased the proteasomal degradation of FOXM1. RCM-1 can be used for asthma and other chronic airway diseases research.

Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.

JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice. JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC₅₀ of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM.

Tenatoprazole (TU-199) is an orally active imidazopyridine-based proton pump inhibitor with a prolonged plasma half-life. Tenatoprazole inhibits hog gastric H⁺/K⁺-ATPase activity with an IC₅₀ of 6.2 μM. Tenatoprazole blocks the interaction of ubiquitin with the ESCRT-1 factor Tsg101, inhibits production of several enveloped viruses, including EBV.

Enpatoran hydrochloride (M5049 hydrochloride) is an orally active and selective TLR7/8 antagonist. Enpatoran hydrochloride inhibits the activation of the downstream type I interferon pathway. Enpatoran hydrochloride is used in studies of cutaneous lupus erythematosus, systemic lupus erythematosus with cutaneous manifestations, and psoriasis.

Epratuzumab (Antibody hLL 2) is an anti-CD22 IgG1 monoclonal antibody. Epratuzumab is also a tumor-imaging agent and an immunomodulatory agent. Epratuzumab can induce CD22 phosphorylation. Epratuzumab has been used to research non-Hodgkin’s lymphomas (NHL) and certain autoimmune diseases.

Resibufogenin is an orally active anticancer agent. Resibufogenin can be extracted from toad venom. Resibufogenin blocks signaling pathways such as PI3K/Akt, NF-κB, AP-1, activates GSK-3β, and regulates cyclin D1. Resibufogenin can activate central neurons. Resibufogenin has anti-inflammatory activity. Resibufogenin has anti-tumor effects on a variety of tumors such as multiple myeloma, renal cancer, colorectal cancer, pancreatic cancer, and glioma.

Anti-Mouse IL-6 Antibody (MP5-20F3) is an anti-mouse IL-6 IgG1 monoclonal antibody. Anti-Mouse IL-6 Antibody (MP5-20F3) reshapes the tumor microenvironment by blocking IL-6. Anti-Mouse IL-6 Antibody (MP5-20F3) can inhibit the STAT3 pathway and enhance T cell infiltration. Anti-Mouse IL-6 Antibody (MP5-20F3) can be used for researches on inflammation and infection conditions such as malignant pleural effusion (MPE).

Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC₅₀s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory, antibacterial, antitumor therapies, as well as drug metabolism regulation.

Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A₂ (iPLA₂β) with an IC₅₀ value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca²⁺ influx.

KAT8-IN-1 is a lysine (K) acetyltransferase 8 (KAT8) inhibitor, with IC₅₀s of 141 μM (KAT8), 221 μM (KAT2B), 106 μM (KAT3B), respectively. KAT8 inhibits histone acetyltransferases (HATs), and could result in disease states, such as cancer or inflammatory diseases.

D-α-Hydroxyglutaric acid ((R)-2-Hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a K_i of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling.

Berberrubine chloride is an orally active metabolite of berberine. Berberrubine chloride alleviates mucosal lesions and inflammation in mouse colitis models. Berberrubine chloride has anti-inflammatory, anti-tumor, and antiviral activities.

ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC₅₀ of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs).

Citric acid-¹³C₆ is the ¹³C-labeled Citric acid (HY-N1428). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries.