(S)-2-(1-Ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1-(2-hydroxy-2-phenylethyl)-1H-benzo[d]imidazole-5-carboxamide (compound 4) is a STING agonist containing a key amide benzimidazole (ABZI) component and shows reproducible inhibition of 3H-cGAMP binding to STING with an apparent inhibition constant IC50 of 14 μM. (S)-2-(1-Ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1-(2-hydroxy-2-phenylethyl)-1H-benzo[d]imidazole-5-carboxamide can be used for tumor research.

Refinicopan is a complement factor D inhibitor with an IC50 of 10 nM. Refinicopan inhibits rabbit erythrocyte hemolysis with an IC50 of 41 nM. Refinicopan exhibits excellent pharmacokinetic and pharmacodynamic activity.

SMU-L11-R is a selective TLR7 agonist with an EC50 of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits  MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8+T cells. SMU-L11-R shows potential in colorectal cancer studies.

Parent CDN is a cyclic dinucleotide and a STING agonist. Parent CDN exhibits anti-tumor activity.

3’,5’-DiOA-dC is a hydrophobic nucleotide lipid and a ligand for the STING agonist c-di-GMP (CDG). 3’,5’-DiOA-dC can assemble with CDG and form stable cyclic dinucleotide nanoparticles via various supramolecular forces driven by molecular recognition. 3’,5’-DiOA-dC can decrease tumor weight and volume, increase CD8 T cell, neutrophils as well as NK cell counts in tumor microenvironment in combination with CDG. 3’,5’-DiOA-dC also increases the levels of TNF-α and IFN-γ in murine melanoma model.

BMS-025 is a orthosteric STING agonist. BMS-025 can induces chemical shift of STING M271 residue, further activating STING IFN signaling. BMS-025 can be used for monogenic autoinflammatory disease like SAVI disease research.

ETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI60 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI60 modulates the expression of genes associated with inflammation. ETI60 effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI60 can be used for autoimmune and inflammatory diseases research.

Guanidino ethyl disulfide (GED) (Compound 23) is a NO Synthase (NOS) inhibitor with EC50s of 110, 630 and 180  μM for iNOS, eNOS and bNOS, respectivly. Guanidino ethyl disulfide effectively inhibits nitrite production in J774.2 macrophages. Guanidino ethyl disulfide can be used for circulatory shock, inflammation and neurological diseases research.

NPH16 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 24.4 nM. NPH16 can promote HepG2 cell apoptosis. NPH16 shows excellent in vivo antitumor efficacy and favorable pharmacokinetic properties. NPH16 can be used for the study of liver cancer.

Antitumor photosensitizer-9 is a near-infrared Photosensitizer (PS) with a high singlet oxygen production rate (relative rate = 1.79). Antitumor photosensitizer-9 exhibits strong phototoxicity against various cancer cells and induces ROS generation under light irradiation. Antitumor photosensitizer-9 inhibits tumor growth in vivo and exhibits excellent anticancer photodynamic therapy (PDT) efficacy at low drug and light doses. Antitumor photosensitizer-9 can be used in photodynamic therapy research.

endo-S-cGAFMP (Compound 3) is a STING agonist. endo-S-cGAFMP induces the production of interferon regulatory factors and proinflammatory cytokines by activating the cGAS-STING pathway, thereby enhancing innate and adaptive immune responses. endo-S-cGAFMP has potent immunostimulatory capacity in THP1 monocytes and RAW macrophages (EC50 values of 2.45 μM and 5.54 μM, respectively). endo-S-cGAFMP has significant antitumor activity. endo-S-cGAFMP can be used as a potential cancer immunotherapeutic agent, especially for studies of systemic administration.

ZSA-215 is a potent and orally active STING agonist with an EC50 of 3.3 μM. ZSA-215 enhances STING signaling through promoting the phosphorylation of STING and interferon regulatory factor 3 (IRF3) and secretion of IFN-β. ZSA-215 inhibits tumor regression and long-term survival of mice in MC38 colon cancer model. ZSA-215 can be used to the study of colon cancerr.

JNJ-79883960 is a NLRP3 inhibitor. JNJ-79883960 can be used for the study of inflammation.

AGU661 is a Microsomal prostaglandin E2 synthase 1 (mPGES-1) inhibitor with an IC50 of 0.22  nM. AGU661 lowers PGE2 formation in human pro-inflammatory M1 macrophages and activated monocytes without affecting other lipid mediator pathways. AGU661 has unfavorable physicochemical properties with poor metabolic stability and strong plasma protein binding tendencies. AGU661 into PLGA-based NPs significantly enhances its bioactivity. AGU661 can be used for inflammatory disorders research.

ONO-1714 is an orally active nitric oxide synthase inhibitor. ONO-1714 attenuates endotoxin-induced acute lung injury, reduces intestinal ischemia–reperfusion injury, represses biliary carcinogenesis.

BAL-1516 is a brain-penetrant and highly selective NLRP3 inhibitor (IC50=14.2 nM). BAL-1516 significantly suppresses IL-1β and IL-18 release in microglial neuroinflammation models (IC50=11-59 nM). BAL-1516 is promising for research of neurodegenerative diseases (e.g., Alzheimer’s, Parkinson’s) and systemic inflammatory disorders.

diABZI-i is a orthosteric STING inhibitor. diABZI-i significantly inhibits cGAMP-induced IFNβ in PBMCs with an IC50 of 49 nM. diABZI-i also activates V155M SAVI constitutive signaling in STING V155M THP-1 cells model with potent agonism (EC50: 17  nM). diABZI-i can be used for monogenic autoinflammatory disease like SAVI disease research.

diABZI-a1 is a orthosteric STING agonist with EC50 of 117 nM for IFNβ in human PBMCs. diABZI-a1 can be used for monogenic autoinflammatory disease like SAVI disease research.

CCL-34 is a Toll-like receptor 4 (TLR4) activator. CCL-34 significantly induced dendritic cell (DC) CD83 expression and IL-12p70 production in a dose-dependent manner, thereby inducing DC maturation. CCL-34 enhanced the allostimulatory activity of DC on naive CD4+CD45+RA+ T cell proliferation and IFN-γ secretion. CCL-34 further induced antigen presentation ability in mice inoculated with doxorubicin-treated colorectal cancer cells. CCL-34 can be used in studies of immune stimulation.

RC-552 is a novel synthetic glycolipid related in chemical structure to MLA. RC-552 induces delayed cardioprotective effects via an iNOS-dependent pathway. RC-552 attenuates myocardial stunning.

E-5531 is an endotoxin antagonist. E-5531 quickly becomes inactive after binding with HDL. E-5531 can block the Toll like receptor 4 (TLR4) signaling pathway. E-5531 can be used for the study of endotoxemia and septic shock.

SCL-1 is an orally active anti-PD-1/PD-L1 inhibitor. SCL-1 can inhibit PD-1/PD-L1 binding. SCL-1 increases T cells, B cells and natural killer cells. SCL-1 exerts strong tumor growth inhibitory effects that were mediated by effector T-cell induction inside tumors and the up-regulated expression of long non-coding RNAs as neoantigens leading to cytotoxic T lymphocyte activation. SCL-1 can be used for the research of cancer, such as triple-negative breast cancer.

NP3-742 is an orally active NLRP3 inhibitor that binds to the NLRP3 NACHT domain. NP3-742 inhibits IL-1β release with IC50s of 6 nM and 47 nM in both the cellular and whole blood assays, respectively. NP3-742 is highly selective against a panel of more than 50 enzymes, receptors and sodium and calcium channels. NP3-742 can be used for the study of gout, cardiovascular disease or osteoarthritis.

1-Palmitoyl-2-pyropheophorbide a-sn-glycero-3-pc is a phospholipid-porphyrin conjugate. 1-Palmitoyl-2-pyropheophorbide a-sn-glycero-3-pc can be utilized in photodynamic therapy research.

SB-T-101141 is a novel taxane. SB-T-101141 effectively induces a noncanonical ferroptosis to overcome Paclitaxel resistance of breast cancer. SB-T-101141 facilitates the production of iron and ferrous ions and ROS. SB-T-101141 stably binds to KHSRP to inhibit the iron-dependent expression of CISD1 related to iron homeostasis. SB-T-101141 synergistically enhances the iron-dependent activation of JNK and PERK pathways via KHSRP. SB-T-101141 suppresses breast tumor growth in MCF-7(PR)/MDA-MB-231(PR) or KHSRP knock-down MCF-7 xenograft mice model.

SMU-C68 is a highly selective small-molecule TLR1/2 heterodimer agonist (EC50=0.009 μM). SMU-C68 activates NF-κB and MAPK pathways to promote pro-inflammatory cytokine release (e.g., TNF-α, IL-1β). SMU-C68 is promising for research of cancers.

ETI41 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.63 μM) and TLR9 (IC50 = 0.16 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI41 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI41 suppresses the expression of inflammation-associated genes and effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI41 can be used for autoimmune and inflammatory diseases research.

AL-1 is a potent O2- generation inhibitor (IC50 = 7.6 μM) through the inhibition of leukocytic NADPH oxidase. AL-1 inhibits 12-O-Tetradecanoylphorbol-13-acetate (TPA)-induced H2O2 production. AL-1 reduces tumor incidence in ICR mouse skin. AL-1 can be used for research on oxidative stress-related diseases including cancer.

GJ19 is a PD-L1 inhibitor with an IC50 of 32.06 nM. GJ19 can effectively bind to human/murine PD-L1 protein with KD values of 171 and 290 nM, respectively. GJ19 concentration-dependently promotes HepG2 cell mortality in a co-culture model of HepG2/hPD-L1 and Jurkat T/hPD-1 cells. GJ19 effectively suppresses tumor growth in a B16-F10 melanoma mouse model. GJ19 can be used for the study of tumor immunotherapy.

L-ENIPO (hydrochloride) is an inhibitor of iNOS, nNOS, and eNOS with Ki values of 17, 10.3, and 58.2 μM. L-ENIPO (hydrochloride) exerts reversible tight binding inhibition selective for iNOS with longer incubation time.