Immunology & Inflammation

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  1. Balsalazide sodium hydrate could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
  2. antioxidant

    α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells.
  3. COX-2 inhibitor

    Aceclofenac is a cyclooxygenase-2 inhibitor used to treat osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.
  4. COX inhibitor

    Indobufen is a platelet aggregation inhibitor.
  5. Acid pump antagonist

    Revaprazan hydrochloride is a novel acid pump antagonist (APA). Revaprazan hydrochloride reduces COX-2 expression and has significant anti-inflammatory actions activities in H. pylori infection.
  6. COX inhibitor

    Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
  7. Topoisomerase IV inhibitor

    Ciprofloxacin Hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, interfering with the bacterial DNA gyrase, inhibiting the DNA synthesis, and preventing bacterial cell growth.
  8. Nitric oxide donor

    Isosorbide dinitrate is an organic nitrate ester and nitric oxide (NO) donor in the same class as nitroglycerin. Isosorbide dinitrate increases oxygenation of tumor tissue in vivo in a mouse xenograft model. It also inhibits platelet aggregation in vitro and in vivo at concentrations in the micromolar range. Formulations containing isosorbide dinitrate have been used for the treatment of angina pectoris.
  9. Hydrocortisone Acetate is the synthetic acetate salt form of hydrocortisone, a corticosteroid with anti-inflammatory and immunosuppressive properties
  10. Tiaprofenic acid is a non-steroidal anti-inflammatory drug (NSAID) of the arylpropionic acid (profen) class, used to treat pain, especially arthritic pain Long-term use of tiaprofenic acid is associated with severe cystitis, roughly 100 times more commonly than other NSAIDs. It is contraindicated in patients with cystitis and urinary tract infections.
  11. Norgestrel is a synthetic analog of progesterone, a compound commonly found in oral contraceptive pill, and a powerful neuroprotective antioxidant, preventing light-induced ROS in photoreceptor cells, and cell death.
  12. S1P antagonist

    Fingolimod is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant.
  13. COX inhibitor

    Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 nM, 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1, 0.84 μM for ovine COX-1 and COX-2, respectively.
  14. Nrf2 activator

    AKBA (Acetyl-11-keto-β-boswellic acid) is an active triterpenoid compound from the extract of Boswellia serrate and a novel Nrf2 activator.
  15. antifolate agent

    Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
  16. COX inhibitor

    Loxoprofen is an anticancer drug.
  17. Methionine is a sulfur-containing essential L-amino acid that is important in many body functions.
  18. Hydrocortisone buteprate (Hydrocortisone probutate) is a medium potent, non-halogenated double-ester of hydrocortisone with a favorable benefit/risk ratio for the treatment of inflammatory skin disorders.
  19. Tetrahydrobiopterin is a cofactor of the aromatic amino acid hydroxylases enzymes and also acts as an essential cofactor for all nitric oxide synthase (NOS) isoforms.
  20. COX-2 inhibitor

    Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with an IC50 value of 18 nM, it also inhibits COX1- activity with an IC50 value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect.
  21. immunosuppressant

    Tacrolimus monohydrate (FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate) is a macrocyclic lactone with potent immunosuppressive properties, an immunosuppressant.
  22. Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.
  23. Temoporfin(KW 2345) used in photodynamic therapy for the treatment of squamous cell carcinoma of the head and neck. Target: Others Temoporfin used in photodynamic therapy for the treatment of squamous cell carcinoma of the head and neck. Patients can remain photosensitive for several weeks after treatment.
  24. NSAID and COX-2 inhibitor

    Deracoxib is an NSAID and COX-2 inhibitor used to treat osteoarthritis. It induces cell cycle arrest and apoptosis in mammary tumor cells, decreases platelet aggregation, and lowers inflammatory responses.
  25. thrombopoietin (TPO) receptor agonist

    Lusutrombopag, also known as S-888711, is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist being developed by Shionogi for chronic liver disease (CLD) patients with thrombocytopenia prior to elective invasive surgery.
  26. anti-inflammatory agent

    Balsalazide is an anti-inflammatory agent for treatment of Inflammatory Bowel Disease. Balsalazide could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
  27. platelet adhesion inhibitor

    Limaprost(OP1206) is a PGE1 analog and potent platelet adhesion inhibitor.
  28. thromboxane A2 (TXA2) receptor (TP receptor) antagonist

    Seratrodast is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist used primarily in the treatment of asthma.
  29. Anti-inflammatory

    Hydrocortisone butyrate is a topical corticosteroid use to treat a variety of dermatological conditions. It acts as an antiinflammatory, antiproliferative and immunosuppresive agent.
  30. COX-2 inhibitor

    Bromfenac Sodium Sesquihydrate is a nonsteroidal anti-inflammatory drug (NSAID), which inhibits cyclooxygenase II (COX-2).
  31. PD-1/PD-L1

    Avelumab is a fully human IgG1 anti-PD-L1 monoclonal antibody with potential antibody-dependent cell-mediated cytotoxicity.
  32. COX inhibitor

    Dipyrone, also known as Anador and NSC-73205, is a nonsteroidal anti-inflammatory drug used to treat pain (postoperative, colic, cancer, and migraine).
  33. TNF receptor inhibitor

    AX-024 is an orally available inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation (IC50 value 1 nM). Inhibiting an immediate TCR signal has promise for treating a broad spectrum of human T cell-mediated autoimmune and inflammatory diseases.
  34. Neuroinflammation inhibitor

    GIBH-130 is an effective inhibitor of neuroinflammation. GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50=3.4 nM).
  35. TYROSINE 3-MONOOXYGENASE inhibitor

    Metyrosine is an inhibitor of the enzyme TYROSINE 3-MONOOXYGENASE.
  36. H-PGDS inhibitor

    HPGDS inhibitor 2 is a highly potent and selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC50 of 9.9 nM.
  37. PD-1/PD-L1 interaction inhibitor

    PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor with an IC50 of 92.3 nM.
  38. MD2-TLR4 inhibitor

    MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
  39. glucocorticoid receptor agonist

    Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Anti-inflammatory agent.
  40. CCR4 antagonist

    CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues.
  41. CD73 inhibitor

    AB-680 is highly potent, reversible and selective small molecule inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity.
  42. TLR4 antagonist

    IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. It inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein.
  43. Gal-3 inhibitor

    GB1107 is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with a Kd of 37 nM for human Galectin-3. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model.
  44. STING ligand

    STING ligand-1 is a lead STING ligand with an IC50 of 68 nM for HAQ STING.
  45. Factor D inhibitor

    Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM.
  46. CCR8 agonist

    LMD-009 is a selective CCR8 nonpeptide agonist. LMD-009 mediates chemotaxis, inositol phosphate accumulation, and calcium release in high potencies with EC50s from 11 to 87 nM.
  47. CCR2 /CCR5 dual antagonist

    PF-04634817 is an orally administered CCR2 and CCR5 chemokine receptor antagonist, for the treatment of diabetic nephropathies and diabetic macular oedema.
  48. DMNQ is a redox cycling agent that generates both superoxide and hydrogen peroxide intracellularly in a concentration dependent manner. DMNQ increases ROS generation.
  49. NOS inhibitor

    Asymmetric dimethylarginine is an endogenous inhibitor of nitric oxide synthase (NOS), and functions as a marker of endothelial dysfunction in a number of pathological states.
  50. SIK2 inhibitor

    ARN-3236 is potent, orally active and selective SIK2 inhibitor. ARN-3236 inhibited the growth of 10 ovarian cancer cell lines at an IC50 of 0.8 to 2.6 μmol/L.

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