VB-85247 is a STING agonist. VB-85247 induces upregulation of inflammatory cytokines IFNα/β, TNFα, IL6, and CXCL10, as well as maturation and activation of dendritic cells by activating the STING pathway. VB-85247 can achieve regression of intrabladder tumors and can be used in bladder cancer research.

PDIC-NN is an intermediate in the synthesis of PDIC-NS. PDIC-NS is a STING activator with anticancer activity.

PDIC-NC is a STING agonist. PDIC-NC is cytotoxic to tumor cells and induces ROS explosion, apoptosis and autophagy. PDIC-NC has lung specific distribution and can be used in the study of lung cancer.

M04 is an agonist of STING. It induces the expression of the IFN reporter gene in HEK293T cells expressing wild-type human STING, but does not induce this expression in HEK293T cells expressing the R71H-G230A-R293Q (HAQ) STING variant or in mouse RAW 264.7 cells, indicating that its activity is dependent on allelic and species variations. M04 induces the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At a concentration of 50 µM, M04 stimulates dendritic cells isolated from PBMCs to express the MHC class II cell surface receptor HLA-DR and co-stimulatory molecules CD40, CD80, and CD86, and also enhances their ability to activate T cells in an ex vivo assay. M04 can be used in research on inflammatory immune diseases.

GHN105 is an orally active inhibitor for STING that inhibits STING-dependent IFN-β secretion in THP-1 human monocytes with an IC50 of 4.4 μM. GHN105 reduces the IFN-β, IL-6 and CXCL10 levels in serum, and alleviates colitis in DSS.

BDW-OH is an active metabolite of BDW568. 2-Methylbiphenyl-oxadiazole-NH-Ph-NH-PEG3-C2-NH-Boc can be utilized in AUTAC synthesis.

2'2'-cGAMP, a synthetic CDN, binds STING in the immune response, inducing IFN-β. 2'2'-cGAMP binds weaker binding to STING than 2'3'-cGAMP. Emavusertib tosylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib tosylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib tosylate exhibits antitumor activity in mouse model.

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.