Immunology & Inflammation

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

TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.

BMS-1001 is a potent inhibitor of PD-1/PD-L1 interaction with EC50 of 253 nM.

MCC950 (CP-456773, CRID3) is a potent and selective inhibitor of NLRP3 (NOD-like receptor (NLR) family, pyrin domain-containing protein 3) with IC50 of 7.5 nM and 8.1 nM in BMDMs and HMDMs, respectively.

AEM1 is an inhibitor of deregulated NRF2 transcriptional activity in cancer.

R243 is an inhibitor of CCR8 signaling and chemotaxis.

MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity.

Avacopan (CCX168) is an orally administered and selective C5a receptor (C5aR) antagonist.

SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2.

Taletrectinib (DS-6051b) is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor.

LY-3475070 is a potent and selective CD73 Inhibitor with IC50 of 28 nM.

AUNP-12 (NP-12) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions.

Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ??1 nM.

Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities.

BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.

2-Phospho-L-ascorbic acid trisodium acts as an antioxidant and a stimulator of hepatocyte growth factor (HGF) production.

IRAK4-IN-4 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM.

7-Nitroindazole, a heterocyclic compound, acts as a selective inhibitor for neuronal nitric oxide synthase showing a 10-fold selectivity for neuronal NOS.

Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.

Beta-Elemonic acid (3-Oxotirucallenoic Acid), a known triterpene isolated from Boswellia (Burseraceae), exhibits anti?inflammatory effects.

Emamectin Benzoate (MK-244) is an orally active nervoussystem toxicant by binding g-aminobutyric (GABA) receptor in insects.

Coniferaldehyde (Ferulaldehyde), isolated from the ethanol extract of Vitex rotundifolia fruits, is an effective inducer of heme oxygenase-1 (HO-1).

Sinensetin is a methylated flavone found in certain citrus fruits. pocess potent antiangiogenesis and anti-inflammatory, sinensetin enhances adipogenesis and lipolysis.

Norbergenin, also known as Demethylbergenin, is the O-demethyl derivative of bergenin, the main component of Mallotus japonicus.It shows moderate antioxidant activity with IC(50)= 13 μM in DPPH radical scavenging and 32 μM in superoxide anion scavenging.

Nifeviroc is a CCR5 antagonist potentially for treatment of inflammatory responses to HIV type-1 infection

E6446 is an inhibitor os Toll-like receptor (TLR)7 and 9 signaling.

CAY10404 is one of the most selective inhibitors of COX-2 over COX-1.

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.

POT-4 (AL-78898A), a Compstatin derivative, is a potent inhibitor of complement factor C3 activation. POT-4 can be used for age-related macular degeneration research

CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells.

OVA 55-62 is a fragmented peptide of OVA (ovalbumin) antigen and can bind to the mouse MHC class I molecule, H2-Kb.

CKLF1-C19 is the C-terminal peptide of human chemokine-like factor 1 (CKLF1). CKLF1-C19 interacts with CCR4, and inhibits chemotaxis induced by both CKLF1 and CCL17. CKLF1-C19 can suppress allergic lung inflammation via inhibiting chemotaxis mediated by CCR3 and CCR4.

Suc-Ala-Leu-Pro-Phe-pNA (Suc-ALPF-pNA) is a substrate of FK-506 binding protein (FKBP).

Leteprinim, also known as AIT-082 and SPI-205, is a neurotrophic agent potentially for the treatment of Alzheimer's disease, and spinal cord injury.

SU5201 is an inhibitor of interleukin-2 (IL-2) production.

Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM.

Pamicogrel (KBT3022) is a cyclooxygenase (COX) inhibitor.

TMN355 is a potent chemical cyclophilin A inhibitor and reduces foam cell formation and cytokine secretion. TMN355 is used for atherosclerosis.