(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.

PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects.

IL-4-inhibitor-1 (compound 52) is an IL-4 inhibitor, with an EC50 of 1.81 µM.

Sulfo-ara-F-NMN (CZ-48) is a mimetic of nicotinamide mononucleotide (NMN). Sulfo-ara-F-NMN acts selectively, activating SARM1 but inhibiting CD38 (IC50 around 10 μM). Sulfo-ara-F-NMN induces intracellular cyclic ADP-ribose (cADPR) production.

Pam3CSK4 TFA is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2.

AMT hydrochloride is a selective inhibitor of inducible NOS (iNOS) with Ki of 4.2 nM.

ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity.

DFV890 (IFM-2427) is apotent, selective and orally active inhibitor of NLRP3 inflammasome, directly binds to NLRP3 and locks the protein in an inactive conformation,prevents NLRP3 inflammasome assembly in response to sterile danger signals.

diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

TAK-242 (Resatorvid), a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4.

AXC-715 trihydrochloride is a TLR7/TLR8 dual agonist, extracted from patent WO2020168017 A1. AXC-715 trihydrochloride, 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.

IL-17A inhibitor 1 (example 24) is a IL-17A inhibitor, with IC50 values of <9.45 nM and 9.3 nM in alphalisa assay and HT-29 cells.

IL-17 modulator 4 is a prodrug of IL-17 modulator 1. IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator.

cGAMP (Cyclic GMP-AMPP) diammonium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.

3’3’-cGAMP Fluorinated (c-[2'FdGMP]-[2'FdAMP]) is a synthetic analog of cyclic guanosine monophosphate- adenosine monophosphate (cyclic GMP-AMP, cGAMP) with a fluorine atom at 2’ position of the nucleosides. 3’3’-cGAMP is a cyclic di-nucleotide produced by bacteria. It is also referred to as "canonical" cGAMP due the presence of the classical 3’-5’ phosphodiester linkages between the guanosine and the adenosine. It has been reported that cGAMP binds STING (stimulator of IFN genes) and subsequently induces TBK1-IRF3-dependent production of IFN-β [1]. The incorporation of fluorine into biologically active molecules is commonly used in medicinal chemistry to improve their metabolic stability or to modulate physicochemical properties such as lipophilicity [2, 3]. Moreover, the introduction of a fluorine atom can change the biological activities of a molecule. Interestingly, when used at low concentrations in various cellular assays, 3’3’-cGAMP Fluorinated induces higher levels of type I IFNs than does cGAMP. STING ligands such as cGAMP induce type I IFNs and activate interferon stimulated genes (ISG) through IRFs. To facilitate their study, InvivoGen has developed stable reporter cells in two well established immune cell models: THP-1 human monocytes and RAW 264.7 murine macrophages. These cells express a reporter gene (SEAP or Lucia luciferase), under control of an IRF-inducible promoter.

MCC7840 sodium, a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM. MCC7840 sodium can be used for the research of inflammatory diseases.

Selnoflast (example 6) is a NLRP3 inhibitor (extracted from patent WO2019008025).

SZU-106 is a small molecule TLR7 agonist, selectively activates TLR7 and increases the expression of SEAP by activating the NF-κB pathway.

SZU101 is a small molecule TLR7 agonist that directly activates, induces reporter activity (23-fold) in a TLR7-NF-kB reporter system expressed in HEK-293 cells TLR7 signalling.

MHV370 (MHV-370) is a potent, selective, orally bioavailable inhibitor of Toll-like receptors 7 and 8 (TLR7/8) with IC50 of 1.1 and 4.5 nM in cell-based assays.

E567 is a small moleculeTLR2 signaling inhibitor with anti-viral activity, efficiently inhibits both LCMV and HSV-1 induced cytokine responses in both human and mouse cell cultures.

Diprovocim-X is a potent human and murine TLR1/TLR2 agonist with EC50 of 0.14 nM (hTLR1/TLR2) and 0.75 nM (m TLR1/TLR2), respectively.

AZD8848 (AZD 8848) is a potent, selective TLR7 agonist with EC50 of 4 nM for induction of IFNα from human PBMCs and an IC50 of 0.2-1.0 nM for inhibition of IL-5.

SHR1032 is a novel small molecule non-cyclic di-nucleotide STING agonist, exhibits significantly high affinity binding to STING and cellular reporter assay (EC50=30 nM).

SB24011 (SB 24011) is a selective small molecule inhibitor of the STING-TRIM29 interaction with IC50 of 3.85 uM in luciferase complementation assays, enhances cGAMP-mediated STING immunity.

MK-1454 (Ulevostinag) is a novel cyclic dinucleotide STING agonist with robust tumor cytokine upregulation and effective antitumor activity.

LB244 (LB-244) is a highly potent, selective and irreversible STING antagonist, blocks STING oligomerization and inhibits STING signaling THP1 dual cells with IC50 of 0.8 uM.

HB3089 (HB-3089) is a novel potent, highly specific STING agonist, dose-dependently activates interferon-stimulated gene (ISG) signaling in THP1-Dual reporter cells with EC50 of 1-10 uM.

DWL-4-140 is a small molecule inhibitor of cyclized nucleotide-binding domain (CBD) of STING, selectively inhibits DNA-mediated IFNβ responses with IC50 of 617 nM.

ChX710 (ChX0306710) is a small molecule that primes the type I interferon response to cytosolic DNA, which is dependent on the adaptor MAVS and IRF1, but not the IRF3.