AGU654 (Compound 44) is a selective mPGES-1 inhibitor with an IC50 of 2.9 nM against mPGES-1. AGU654 inhibits mPGES-1 to block the pathway converting arachidonic acid into prostaglandin E2 (PGE2) by COX-1/2, thereby alleviating inflammatory responses, pain, and fever. In activated human monocyte-derived macrophages and human whole blood models, AGU654 selectively suppresses bacterial exotoxin-induced PGE2 production while preserving the production of other prostaglandins. In guinea pig models, AGU654 significantly alleviates fever, inflammation, and inflammatory pain, exhibiting excellent anti-inflammatory, analgesic, and antipyretic effects. AGU654 holds promise as a strategy for studying inflammatory diseases and pain.

ADP-β-S (trisodium) is an ADP analog and partial agonist. ADP-β-S (trisodium) induces human platelet aggregation and inhibits PGE1-stimulated adenylate cyclase.

LTB is a prodrug formed by coupling glycolysis inhibitor (Lonidamine) with PD1/PDL1 blocker (BMS-1) by thioketal linkage. LTB can further encapsulate photosensitizer chlorine e6 (Ce6)) to construct a co-delivery photodynamic nanoplatform (LTB-6 NPs) by self-assembly.

Lon-TK is a glycolysis inhibitor + linker conjugate of LTB. LTB is an intelligent responsive prodrug that connects Lonidamine (Lon) and a PD-L1 inhibitor (BMS-1) through a thioketal linker. It significantly inhibits the glycolytic metabolism of tumor cells and blocks the PD-1/PD-L1 immune escape pathway. Lon-TK shows potential for application in photodynamic-enhanced immunotherapy research.

D5B is a potent and selective PD-L1 inhibitor. D5B has been modified by DBCO. The EC50 of D5B degrading PD-L1 in 4T1 and B16-F10 tumor cells are 5.4 μM and 6.2 μM, respectively. D5B can block PD-L1/PD-1 interaction and has anti-tumor activity.

AB-3PRGD2 is a radiotherapeutic agent targeting integrin αvβ3. AB-3PRGD2 shows improved tumor uptake and prolonged tumor retention, leading to significantly enhanced tumor growth suppression. AB-3PRGD2 can remodel the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.

VEN-02XX is an orally active and brain-permeable NLRP3 inhibitor. VEN-02XX inhibits the release of IL-1β and IL-18 (IC50 0.3 and 0.28 μM, respectively). VEN-02XX restores memory and cognition, inhibits microgliosis, and reduces neuroinflammation and tau pathology in the 5XFAD/Rubicon KO mouse model. VEN-02XX may be used in the study of Alzheimer's disease (AD).

NP3-253 is an NLRP3 inhibitor with oral activity and blood-brain barrier permeability, and NP3-253 can serve as a tool to further investigate the biological characteristics of NLRP3 in peripheral and neuroinflammatory model.

HNW005 is a dual inhibitor of NLRP3 inflammasome and urate transporter 1 (URAT1). It has a KD value of 204.6 nM and an IC50 of 1.7 μM for inhibiting NLRP3 inflammasome activation, and an IC50 of 6.4 μM for inhibiting uric acid transmembrane transport. When administered at a dose of 2 mg/kg in vivo, HNW005 can achieve a uric acid reduction rate of 64.8%. It can exert anti - inflammatory, analgesic, and uric acid - lowering activities by inhibiting the activation of NLRP3 inflammasome and uric acid transmembrane transport. HNW005 can be used in the research of gouty arthritis.

Emavusertib tosylate (CA-4948 tosylate) is the tosylate salt form of Emavusertib. 12-((4-Bromobutyl)amino)dodecanoic acid can be utilized in PROTAC synthesis.

Emavusertib phosphate (CA-4948 phosphate) is the phosphate salt form of Emavusertib-induced mechanical hyperalgesia in rats. BI-113823 can be used for the research of chronic inflammatory pain.

Emavusertib mesylate (CA-4948 mesylate) is the mesylate salt form of Emavusertib-stimulated cAMP production with an IC50 value of 18 nM. L-796778 acetate has anticonvulsant effect.

Emavusertib maleate (CA-4948 maleate) is the maleate salt form of Emavusertib that can be extracted from C. forskohlii. Deacetylforskolin activates rat adipocyte adenylyl cyclase (IC50 = 20 µM), inhibits glucose transport in rat adipocyte plasma membranes and exhibits antihypertensive activity.

Tarvicopan is an inhibitor for complement factor D.

SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic.

H-151(H151) is a novel STING (stimulator of interferon genes) antagonist.

CU-CPT-8m is a nolve TLR8 inhibitor.

Leukadherin-1 is a specific agonist of CR3 and the leukocyte surface integrin CD11b/CD18.

CA-170, also known as AUPM170 and PD-1-IN-17, is a programmed cell death-1 (PD-1) inhibitor. PD-1-IN-17 was first reported in patent WO2015033301A1, (Compound 4), inhibits 92% splenocyte proliferation at 100 nM.

RS 09 is a TLR4 agonist. RS 09 promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 acts as an adjuvant in vivo; RS 09 enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.

CU-CPD107 is a TLR8-specific small molecule with unique synergistic agonist activities in the presence of ssRNA, but inactive without the aid of ssRNA.CU-CPD107 significantly inhibited of R848-induced signaling in HEK-Blue hTLR8 cells with an IC50 of 13.7 uM.CU-CPD107 only inhibited synthesized small-molecule agonist-induced TLR8 signaling without affecting other TLRs.CU-CPD107 synergistically increased IFN-β, TNF-α, IL-1β, IL-6, and IL-8 mRNA expression levels in the presence of 5 μg/ml ssRNA40 in HEK-Blue hTLR8 cells, whereas CU-CPD107 alone did not. CU-CPD107 only activated TLR8-mediated signaling in the presence of ssRNA.CU-CPD107 showed no pure agonistic activity, addressing a major challenge that has existed for previous TLR7 and TLR8 agonists as vaccine adjuvants or antiviral drugs.

C29 is a potential TLR2 inhibitor.

GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma.

Monophosphoryl lipid A (Glucopyranosyl lipid A) is a toll-like receptor 4 agonist. Monophosphoryl lipid A is derived from the cell wall of nonpathogenic Salmonella. Monophosphoryl lipid A can be used for the research of immunization and vaccine.

Polyinosinic-polycytidylic acid (Poly(I:C)) sodium is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis.

Benralizumab (MEDI-563) is an interleukin-5 receptor α (IL-5Rα)-directed cytolytic monoclonal antibody that induces direct, rapid and nearly complete depletion of eosinophils via enhanced antibody-dependent cell-mediated cytotoxicity. Benralizumab can be used for severe eosinophilic asthma.

Dupilumab (REGN-668) is a fully human mAb to IL-4 receptor α (IL-4Rα) that inhibits both IL-4 and IL-13 signaling, markedly improved moderate-to-severe atopic dermatitis.

TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC50 value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon).

STING agonist-7 is a non-nucleotide STING agonist. STING agonist-7 binds selectively to mouse STING but not human STING. STING agonist-7 penetrates cell membrane poorly.

JC124 is a specific NLRP3 inflammasome inhibitor. JC124 has anti-inflammatory and neuroprotective effects.