Cadonilimab (AK104) is a targeting PD1/CTLA4 IgG1 scaffold Fc-engineered humanized antibody. Cadonilimab can be used for researching metastatic cervical cancer[1][2].
MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate[1].
Fc 11a-2, a benzimidazole compound, is an orally active and potent NLRP3 inflammasome inhibitor. Fc 11a-2 restrains the formation of NLRP3 inflammasome by inhibiting activation of caspase-1 and thus the activation of IL-1b/IL-18. Fc 11a-2 prevents the development of Dextran sulfate sodium (DSS; HY-116282C)-induced murine experimental colitis[1][2][3].
C29 is a Toll-like receptor 2 (TLR2) inhibitor.
Dehydroperilloxin is a natural compound isolated from the dichloromethane extract of the stems of Perilla frutescens var. acuta. Dehydroperilloxin possesses inhibitory activity against cyclooxygenase-1, with the IC50 value of 30.4 μM[1].
Flurbiprofen axetil is a non-selective cyclooxygenase (COX) inhibitor. Flurbiprofen axetil has anti-inflammatory effect[1].
hPGDS-IN-1 is a hPGDS inhibitor ,with IC50 of 12 nM in the Fluorescence Polarization Assay or the EIA assay.IC50 value: 12 nMTarget: hPGDSThe detailed information please refer to WO2011044307A1 and WO2010080563A2
(R)-(-)-α-Methylhistamine dihydrobromide is a potent and selective H3 histamine receptor agonist with a Kd of 50.3 nM[1][2]. (R)-(-)-α-Methylhistamine dihydrobromide can cross the blood-brain barrier, and can enhance memory retention, attenuates memory impairment in rats[3][4][5].
Soyasaponin II is a saponin with antiviral activity. Soyasaponin II inhibits the replication of HSV-1, HCMV, influenza virus, and HIV-1. Soyasaponin II shows potent inhibition on HSV-1 replication. Soyasaponin II serves as a inhibitor for YB-1 phosphorylation and NLRP3 inflammasome priming and could protect mice against LPS/GalN induced acute liver failure[1][2].
(+)-14-Deoxy-ε-caesalpin (14-Deoxy-ε-caesalpin), a cassane diterpenoid, inhibits nitric oxide (NO) production release of RAW 264.7 cells stimulated by Lipopolysaccharide (LPS)[1].
Acrivastine D7 (BW825C D7) is a deuterium labeled Acrivastine. Acrivastine is a short acting histamine 1 receptor antagonist.
ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca2+ concentrations[1][2].
Inflexuside A, an abietane diterpenoid, can be isolated from the aerial parts of Isodon inflexus. Inflexuside B strongly inhibits lipopolysaccharide (LPS)-activated NO production (NO Synthase) in RAW264.7 macrophages[1].
IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.
CTX-471 is a fully human monoclonal antibody of CD137. CTX-471 has bind affinity for recombinant human, cynomolgus macaque CD137 and mouse CD137 with Kd values of 50 nM, 61 nM and 748 nM, respectively. CTX-471 can be used for the research of immunomodulation and cancer[1].
DL-Norvaline, a derivative of L-norvaline, L-norvaline is a non-competitive inhibitor of arginase.
Anti-inflammatory agent 21 (compound 9o) is an orally active and low cytotoxic anti-inflammatory agent, with an IC50 value of 0.76 μM for NO. Anti-inflammatory agent 21 acts via accumulation ROS and blocks the NF-κB/MAPK signaling pathway. Anti-inflammatory agent 21 can ameliorate cartilage destruction and inflammatory cell infiltration in arthritis rats model[1].
AXC-715 hydrochloride is a TLR7/TLR8 dual agonist, extracted from patent WO2020168017 A1[1]. AXC-715, compound D from WO2020190734A1, can be used for synthesis of antibody-adjuvant immunoconjugates, comprising an antibody construct that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants[2].
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.
SC-58125 is a potent and selective inhibitor of cyclooxygenase 2 (COX-2), with an IC50 of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo, and it also can inhibit edema at the inflammatory site and is analgesic[1][2][3].
TLR1 (compound 4a) is a low molecular weight, cell-penetrating Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop mimic. TLR1 inhibits IL-1 receptor-mediated responses[1].
NLRP3 agonist 1 (compound 23) is a potent and orally active NLRP3 agonist. NLRP3 agonist 1 can activate the enzyme Caspase-1 to cleave pro-IL-1β and pro-IL-18 proinflammatory cytokines into their mature forms[1].
MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2 on human monocytes.
TLR7 agonist 6 (compound IIb-19) is an TLR7 agonist with an EC50 value of ~4 nM[1].
LFS-1107 is a reversible CRM1 inhibitor (Kd: 12.5 pM). LFS-1107 can selectively eliminate extranodal natural killer/T cell lymphoma (ENKTL) cells and can be used for cancer research[1].
YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively[1]. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo[3].
SRI-42127 is a HuR translocation inhibitor. HuR is an RNA regulator that binds to AREs, and HuR translocations promote the production of inflammatory cytokines in glial cells. However, SRI-42127 can destroy mRNA stability and inhibit gene promoter activation. SRI-42127 also inhibits microglial cell activation and attenuates recruitment/chemotaxis of neutrophils and monocytes[1].
Tislelizumab, a monoclonal antibody with high binding affinity to the PD-1 receptor, minimizes Fcγ receptor binding on macrophages, thereby abrogating antibody-dependent phagocytosis, a mechanism of T cell clearance and potential resistance to anti-PD-1 therapy. Tislelizumab can be used for the research of advanced squamous non-small-cell lung cancer[1].
Eltrombopag is a thrombopoietin (TPO) receptor agonist developed for certain conditions that lead to thrombocytopenia.
PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA)[1].