Inflammation/Immunology

FABPs ligand 6 (MF6) is an FABP5 and FABP7 inhibitor with K_D values of 874 nM and 20 nM, respectively. FABPs ligand 6 can be used for multiple sclerosis research.

Tyrosol is a derivative of phenethyl alcohol. Tyrosol attenuates pro-inflammatory cytokines from cultured astrocytes and NF-κB activation. Anti-oxidative and anti-inflammatory effects.

GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC₅₀ of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.

(2-Chloropyridin-4-yl)methanamine hydrochloride is a selective LOXL2 inhibitor with an IC₅₀ of 126 nM.

AMY-101 acetate (Cp40 acetate), a peptidic inhibitor of the central complement component C3 (K_D = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 acetate (Cp40 acetate) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.

CSK-IN-1 (compound 13) is a potent, orally active c-terminal Src kinase (CSK) with IC₅₀ values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. CSK-IN-1 shows the ability to increase T cell proliferation induced by T cell receptor signaling.

Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC₅₀ value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC₅₀ value of 1.4-1.6 nM. Palazestrant can inhibit ER⁺/HER2⁺ cancer.

Fezakinumab (ILV 094) is an anti-IL-22 monoclonal antibody. Fezakinumab inhibits IL-22 signal transduction, and regulates the JAK1/STAT3 pathway as well as apoptotic proteins. Fezakinumab alleviates airway remodeling, alveolar enlargement and inflammatory cell infiltration in lung tissues. Fezakinumab reduces the levels of neutrophils, lymphocytes, eosinophils and macrophages in lung tissues. Fezakinumab can be used in the research of chronic obstructive pulmonary disease and skin diseases.

Mirikizumab (LY3074828) is a humanized IgG4 monoclonal antibody that targets the p19 subunit of interleukin 23 (IL-23). Mirikizumab binds to human and monkey IL-23 with high affinity, with K_d values of 21 pM and 55 pM, respectively. By inhibiting the binding of IL-23 to IL-23R, Mirikizumab modulates the immune response and holds potential for research in ulcerative colitis and Crohn's disease.

Zasocitinib (NDI-034858) is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant K_d of <200 pM.

Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC₅₀ = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection.

Piroxicam (CP-16171) is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC₅₀s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively.

Hemocyanin is an extracellular giant copper-containing glycoprotein. Hemocyanin can be found in the hemolymph of both mollusk and arthropod. Hemocyanin is responsible for oxygen transport. Hemocyanin is also involved in several physiological processes, such as energy storage, osmoregulation, molt cycle and exoskeleton formation. Hemocyanin in shrimp can enhance its immune response by modulating the p38 MAPK pathway. Hemocyanin from Penaeus monodon could act as an antiviral agent against a variety of viruses including DNA and RNA viruses. Hemocyanin from horseshoe crab Carcinoscorpius rotundicauda could possess a strong antimicrobial defense by the production of ROS activated with microbial proteases. Hemocyanin from L. vannamei would be effective against cervical cancer cell growth.

NVP-DFV890 is an orally administered, selective NLRP3 inhibitor. NVP-DFV890 directly binds to NLRP3, blocks maturation of pro-inflammatory cytokines IL-1β and IL-18, and inhibits pyroptotic cell death. NVP-DFV890 acts as an inducer of viral clearance, promoting earlier clearance of SARS-CoV-2. NVP-DFV890 can be used for the research of COVID-19 pneumonia and coronavirus-associated acute respiratory distress syndrome (CARDS).

CL097, a potent TLR7 and TLR8 agonist, induces pro-inflammatory cytokines in macrophages. CL097 induces NADPH oxidase priming, resulting in an increase of the fMLF-stimulated ROS production.

Crocetin (Transcrocetin) is an aglycone of crocin. Crocetin is an orally active and brain-penetrant. Crocetin shows strong NMDA receptor affinity and channel opening activity. Crocetin can downregulate the proinflammatory cytokines and COX-2 exoression. Crocetin can inhibit apoptosis and activation of MAPK. Crocetin can delay delays brain and body aging. Crocetin can be used for the researches of cancer, neurological disease and inflammation, such as cervical cancer and ischemia.

Escin, a natural compound of triterpenoid saponins that can be isolated from horse chestnut (Aesculus hippocastanum) seeds, can be used as a vasoprotective anti-inflammatory, anti-edematous and anti-nociceptive agent.

TLR9-IN-1 is a potent and selective TLR9 inhibitor with an IC₅₀ value of 7 nM for human TLR9. TLR9-IN-1 can be used for researching diseases associated with undesirable immune response.

Riliprubart (SAR 445088) is a selective anti-C1s humanized IgG4 monoclonal antibody with mutations that enhance its binding to the neonatal Fc receptor. Riliprubart blocks activation of the classical complement pathway, prevents the formation of the C3 convertase C4b2a, and inhibits complement-mediated hemolytic activity. Riliprubart can be used in research related to classical complement-mediated diseases, cold agglutinin disease, and chronic inflammatory demyelinating polyneuropathy. For the isotype control of Riliprubart, refer to Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).

Fexofenadine (MDL-16455) hydrochloride is an orally active and nonsedative H₁ receptor antagonist. Fexofenadine hydrochloride can be used in allergic rhinitis and chronic idiopathic urticarial research.