Immunology & Inflammation

MCC950 sodium is a potent NLRP3 inflammasome inhibitor that inhibits IL-1beta production with IC50 value of 7.5 nm.

Paradol is the active flavor constituent of the seeds of Guinea pepper (Aframomum melegueta); Paradol has been found to have antioxidative and antitumor promoting effects

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.

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).

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.

AMD 070 is a CXCR4 chemokine receptor antagonist.

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

LNP023 is a highly potent factor B (FB) inhibitor with an IC50 value of 10 nM. LNP023 shows direct, reversible, and high-affinity binding to human FB (KD=7.9 nM).

Cyclosporin A (Cyclosporine A) is an immunosuppressant agent widely used in post-allogeneic organ transplant to reduce the activity of the immune system.

(S)-(+)-Flurbiprofen is a non-selective Cox-1 and Cox-2 inhibitor.

SCH 563705 is a potent dual CXCR2(IC50= 1.3 nM)/CXCR1(IC50= 7.3 nM) antagonist.

VTX-2337 is a small-molecule Toll-like receptor 8 (TLR8) agonist with potential immunostimulating and antineoplastic activities.

GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7.

Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic activity.

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

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.

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

Asaraldehyde is a selective 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.

Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects.

Deflazacort is a glucocorticoid used as an anti-inflammatory and immunosuppressant.

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.

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

Flurbiprofen is a nonsteroidal anti-inflammatory agent (NSAIA) with antipyretic and analgesic activity.

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

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.

Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively.

Mizoribine is an imidazole nucleoside immunosuppressant agent that was first isolated from the mold Eupenicillium brefeldimium with antibiotic and cytotoxic effects.

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.

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.

Phenylbutazone is a compound of research interest as an anti-inflammatory and anti-proliferative agent.

Pimecrolimus is a natural ascomycin macrolactam that binds to macrophilin-12 (FKBP-12) and inhibits calcineurin as well as prolyl isomerase (rotamase).

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

Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions

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.

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

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

CTCE-0214 is a chemokine CXC receptor 4 (CXCR4) agonist, SDF-1α (stromal cell-derived factor-1α) peptide analog. CTCE-0214 shows anti-inflammatory activity, and can be used in inflammation sepsis and systemic inflammatory syndromes research.

Antileukinate, a hexapeptide, is a potent inhibitor of CXC-chemokine receptor (CXCR). Antileukinate inhibits neutrophil chemotaxis and activation. Antileukinate can be used for the research of acute inflammation and injury.

Vudalimab is a fully human bispecific monoclonal antibody targeting both PD-1 and CTLA-4, two key immune checkpoint receptors. By simultaneously blocking these pathways, Vudalimab enhances T-cell activation in the tumor microenvironment and is widely used in research on immune checkpoint blockade, tumor immunology, and combination immunotherapy strategies.

Quavonlimab (MK-1308) represents a novel monoclonal antibody targeting CTLA-4 (Cytotoxic T-Lymphocyte-Associated Protein 4). This therapeutic agent is designed to modulate immune responses by inhibiting CTLA-4, a protein that plays a crucial role in regulating immune checkpoints. Quavonlimab is primarily utilized in research focusing on immune-oncology and the potential enhancement of anti-tumor immunity.

Tuvonralimab (PSB-205; QL1706) is a dual-action immunotherapy agent comprising a combination of Iparomlimab, an anti-PD-1 IgG4 antibody, and Tuvonralimab, an anti-CTLA-4 IgG1 antibody. This formulation is designed to synergistically inhibit both the PD-1 and CTLA-4 immune checkpoints, enhancing antitumor immune responses. Tuvonralimab is utilized primarily in research focused on cancer immunotherapy, aiming to study and potentially enhance the efficacy of checkpoint blockade strategies.

Ieramilimab (LAG525; IMP701) is a humanized IgG4 monoclonal antibody designed to target and bind to lymphocyte-activation gene 3 (LAG-3). This interaction effectively inhibits the binding of LAG-3 to major histocompatibility complex class II (MHC-II) molecules, which is critical in modulating immune response. Ieramilimab is utilized extensively in research focused on immune checkpoint regulation and potential therapeutic interventions for various immunological disorders.

Tebotelimab (MGD-013) is a humanized IgG4κ bispecific antibody designed for dual affinity re-targeting (DART) of PD-1 and LAG-3. This therapeutic agent demonstrates high affinity binding to cell-surface expressed PD-1 and LAG-3, with half-maximal effective concentrations (EC50s) of 1.65 nM and 0.41 nM in NS0 cells, respectively. By effectively blocking the interactions between PD-1/PD-L1, PD-1/PD-L2, and LAG-3/HLA (MHC-II), as well as inhibiting PD-1 signaling pathways, Tebotelimab plays a crucial role in restoring the function of exhausted T-cells. This restoration is pivotal in enhancing anti-tumor immunity, making Tebotelimab a significant tool in cancer immunotherapy research.

Gotistobart (ONC-392) is a humanized monoclonal antibody targeting CTLA-4, designed to enhance immunotherapeutic efficacy through the selective depletion of regulatory T cells (Tregs) within the tumor microenvironment. This antibody facilitates a targeted approach to modulate the immune system, potentially improving treatment outcomes in cancer immunotherapy.

OVA Peptide(257-264) TFA 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.

NIM811 ((Melle-4)cyclosporin; SDZ NIM811) is an orally bioavailable mitochondrial permeability transition and cyclophilin dual inhibitor, which exhibits potent in vitro activity against hepatitis C virus (HCV) .

PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.

Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates' complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.

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