Immunology & Inflammation

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  1. COX inhibitor

    Acetaminophen (paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic drug. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
  2. Acetylcysteine is a pharmaceutical drug and nutritional supplement used primarily as a mucolytic agent and in the management of paracetamol (acetaminophen) overdose. Oral acetylcysteine is also used for the prevention of radiocontrast-induced nephropathy (a form of acute renal failure).

  3. Allopurinol is a purine analog; it is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase.
  4. xanthine oxidase inhibitor

    Allopurinol is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase.
  5. COX-2 inhibitor

    Asaraldehyde is a selective COX-2 inhibitor.
  6. Berberine hydrochloride was novelly found that it has various beneficial effects on the cardiovascular system and significant anti-inflammatory activities. Berberine can effectively reduce intracellular superoxide levels in LPS-stimulated macrophages. Such a restoration of cellular redox by berberine is mediated by its selective inhibition of gp91phox expression and enhancement of SOD activity.

  7. COX-2 inhibitor

    Celecoxib is a sulfa non-steroidal anti-inflammatory drug (NSAID) and selective COX-2 inhibitor used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis.

  8. Dihydropyrimidinase Inhibitor

    Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects.
  9. Cyclosporin A (Cyclosporine A) is an immunosuppressant agent widely used in post-allogeneic organ transplant to reduce the activity of the immune system.
  10. Deflazacort is a glucocorticoid used as an anti-inflammatory and immunosuppressant.
  11. glucocorticoid receptor agonist

    Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs. It acts as an anti-inflammatory and immunosuppressant. Its potency is about 20-30 times that of the naturally occurring hormone hydrocortisone and 4-5 times of prednisone.
  12. COX inhibitor

    Diclofenac Sodium is a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation.
  13. Vascular Disrupting Agent (VDA)

    DMXAA (ASA404) is a tumor-vascular disrupting agent (tumor-VDA) that attacks the blood supply of a cancerous tumor to cause tumor regression.
  14. COX inhibitor

    Etodolac (AY-24236) is a non-steroidal anti-inflammatory compound that is a non-selective inhibitor of COX (IC50=53.5 nM).
  15. xanthine oxidase inhibitor

    Febuxostat is a non-purine inhibitor of xanthine oxidase (Ki = 1.2 nM).
  16. mTOR inhibitor

    FK-506 is an immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune system and so lower the risk of organ rejection. It reduces interleukin-2 (IL-2) production by T-cells.
  17. S1P Receptor antagonist

    FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine.
  18. Hydrocortisone is a steroid hormone or glucocorticoid produced by the adrenal gland.
  19. COX-1 inhibitor

    Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) targeting COX-1 with an IC50 of 13 μM.
  20. COX-1 inhibitor

    Ibuprofen Lysine(Motrin) is a non-steroidal anti-inflammatory drug.
  21. TLR7 agonist

    Imiquimod (Aldara) is a a heterocyclic imidazoquinoline amide that acts as an immune response modifier.
  22. COX inhibitor

    Indomethacin is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively. Indomethacin(Indocid, Indocin) is a non-steroidal anti-inflammatory compound commonly used to reduce fever, pain, stiffness, and swelling.
  23. NLRP3 inflammasome inhibitor

    Isoliquiritigenin is a licorice chalconoid, a type of natural phenols that is currently under experimentation phase testing for use as a cancer treatment as well as an aide for cocaine addiction.
  24. CCR antagonist

    Maraviroc is an antiretroviral drug in the CCR5 receptor antagonist class used in the treatment of HIV infection.
  25. Mizoribine is an imidazole nucleoside immunosuppressant agent that was first isolated from the mold Eupenicillium brefeldimium with antibiotic and cytotoxic effects.
  26. IMPDH inhibitor

    Mycophenolate mofetil is a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH) in purine biosynthesis (specifically guanine synthesis) which is necessary for the growth of T cells and B cells.
  27. Mycophenolic Acid is an immunosuppressant small molecule isolated as a fermentation product from several Penicillium species.
  28. COX inhibitor

    Naproxen sodium is a non-selective cyclooxygenase (COX) inhibitor that displays anti-inflammatory, antipyretic and analgesic effects. Has a neuroprotective role against colchicine-induced cognitive impairment and oxidative stress.
  29. COX inhibitor

    Phenylbutazone is a compound of research interest as an anti-inflammatory and anti-proliferative agent.
  30. Pimecrolimus is a natural ascomycin macrolactam that binds to macrophilin-12 (FKBP-12) and inhibits calcineurin as well as prolyl isomerase (rotamase).
  31. COX inhibitor

    Piroxicam is an effective and potent inhibitor of prostaglandin synthesis and a Cox-1 and Cox-2 inhibitor.
  32. COX inhibitor

    Pravadoline (WIN 48,098) is antiinflammatory and prostaglandin synthesis inhibitor, acting through inhibition of the enzyme cyclooxygenase (COX).
  33. mTOR Inhibitors

    Rapamycin (Sirolimus) prevents activation of T cells and B-cells by inhibiting their response to interleukin-2 (IL-2).
  34. COX inhibitor

    Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions
  35. Suplatast Tosilate is a novel capsular anti-asthmatic agent that suppresses both IgE production, IL-4 and IL-5 synthesis with IC50 above 100 μM.
  36. CXCR4 antagonist

    Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation.
  37. 6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent,
  38. CCR5 antagonist

    Vicriviroc Malate is a second generation orally active CCR5 antagonist, which is also a potent inhibitor of HIV-1 entry into target cells, with a mean IC50 =0.46 nM and IC50 =1~10 nM to HIV isolates (n=52).
  39. CXCR2 ligand

    SRT3109 is a CXCR2 ligand for use in the treatment of chemokine mediated diseases and conditions.
  40. HCCR2 antagonist

    INCB 3284 dimesylate is a potent, selective hCCR2 antagonist that exhibits potenct antagonism against monocyte chemoattractant molecule binding to hCCR2 and chemotaxis activity.
  41. CCR2 antagonist

    MK-0812 is a potent and selective CCR2 antagonist with low nM affinity for CCR2 on human monocytes and low nM in the chemotaxis assay. It has good PK profiles in preclinical species and demonstrated efficacy in animal models.
  42. CCR2 Antagonist

    INCB8761(PF-4136309) is a potent, selective, and orally bioavailable CCR2 antagonist.
  43. HIV Entry Inhibitor

    BMS-806, also known as BMS-378806 , is a type of medicine called an entry inhibitor. Entry inhibitors work by blocking HIV from entering human cells. BMS-378806 (BMS-806) is a small molecule that blocks the binding of host-cell CD4 with viral gp120 protein and therefore inhibits the first steps of HIV-1 infection.
  44. CXCR4 antagonist

    AMD 070 is a CXCR4 chemokine receptor antagonist.
  45. IRAK modulator

    IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2.
  46. COX-2 inhibitor

    Iguratimod(T 614) is one of a series of 4H-1-benzopyran-4-ones which has potent anti-inflammatory, analgesic and antipyretic activity. Iguratimod(T 614) is a selective inhibitor of cyclo-oxygenase-2 (COX-2), and inhibits the production of interleukin-1 (IL-1), IL-6, IL-8 and tumour necrosis factor.
  47. CCR2 antagonist

    INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
  48. SIK/TBK-1/IKKe inhibitor

    MRT67307 is a potent and dual IKKε and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively.
  49. TLR4 inhibitor

    Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor and plays pivotal role in various inflammatory diseases.
  50. CXCR1/CXCR2 antagonist

    SCH527123 is a potent and selective antagonist of the human CXCR1 and CXCR2 receptors with IC50 of 42 nM and 3 nM, respectively.

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