ROS inducer 8 (Compound 11g) is the inhibitor for glutathione (GSH), that induces the ROS accumulation in Enterococcus faecalis, thereby exhibiting antibacterial activity. ROS inducer 8 disrupts the biofilm, inhibits S. aureus and E. faecalis with MIC of 8 μg/mL and 2 μg/mL, exhibits post-antibiotic effect. ROS inducer 8 exhibits low hemolytic toxicity to sheep erythrocytes (HC50 > 1280 μg/mL).

ROS inducer 6 (compound 9) is a reactive oxygen species (ROS) inducer. ROS inducer 6 (compound 9) acts as an anticancer agent by inducing ROS generation through the depletion of intracellular glutathione.

NPC26 is a small molecule mitochondrial disruptor with anti-tumor activity. NPC-26 shows significant anti-proliferative and cytotoxic effects on CRC cell lines (HCT-116, DLD-1, and HT-29). NPC26 can damage mitochondrial function, leading to the opening of the mitochondrial permeability transition pore (mPTP) and the production of reactive oxygen species, ultimately inducing cell death. NPC-26 can kill CRC cells by activating the AMP-activated protein kinase (AMPK) signaling pathway.

Nitrosobenzene is a radical scavenger that can be used to study oxidative DNA damage and the respiratory burst reaction of neutrophils induced by nitro compounds.

meso-Zeaxanthin accumulates in the central retina and forms macular pigment together with lutein and zeaxanthin, which has the function of light filtering. meso-Zeaxanthin can quench ROS and exert antioxidant function.

L-Ascorbic acid (L-Ascorbate) magnesium, an electron donor, is an endogenous antioxidant. L-Ascorbic acid selectively inhibits Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition promoter and elastin production inhibitor. L-Ascorbic acid exhibits anticancer effects by generating reactive oxygen species (ROS) and selectively damaging cancer cells.

Hypoxystat increases the affinity of hemoglobin for oxygen and reduces the release of oxygen to tissues, thereby inducing the tissue hypoxia. Hypoxystat alleviates the mitochondrial disease Leigh syndrome in Ndufs4 knockout mouse models. Hypoxystat exhibits orally activity.

DIM-C-pPhtBu is an orally active endoplasmic reticulum stress activator. DIM-C-pPhtBu induces mitochondrial and lysosome dysfunction, excessive mitosis, ROS production, and unfolded protein response-mediated cell death in neck cancer cells. DIM-C-pPhtBu has antitumor activity.

Cyanidin arabinoside is an antioxidant agent, that exhibits a Trolox and can be used to prepare ADC compounds.

BJ-13 is a reactive oxygen species (ROS) inducer that can lead to mitochondrial membrane potential collapse and caspase-dependent apoptosis. BJ-13 inhibits the proliferation of SGC-7901, U-87MG, and HepG-2 cancer cells (IC50 values of 15.33, 27.18, and 20.44 nM, respectively). BJ-13 can be used in the study of gastric cancer.

(+)-Secolongifolene-diol is a sesquiterpene, that can be isolated from the marine fungal Drechslera sp. (+)-Secolongifolene-diol exhibits slightly weak effectiveness in antioxidation, antimicrobial and antifouling aspects.

SMU-14a is a TLR3 inhibitor (IC50: 0.18 µM). SMU-14a inhibits IL-6 secretion in mouse peritoneal macrophages and downregulates TNF-α in human peripheral blood monocytes. SMU-14a exerts anti-inflammatory effects by reducing the phosphorylation of p65, ERK, and TBK1 through NF-κB, MAPK, and IRF3 signaling pathways, and decreasing serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. SMU-14a can be used in the study of acute hepatitis.

Pixatimod free acid (PG545 free acid) is a mimetic of Heparan Sulfate. 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats.

FP20Rha is a potent TLR4 agonist. FP20Rha enhances vaccine efficacy against Pseudomonas aeruginosa.

FGT-4 is a folate receptor β (FR-β) targeting chimeric molecule. FGT-4 is a TLR7 agonist. FGT-4 facilitates the secretion of iNOS and proinflammatory cytokine IL-6 associated with M1 macrophages and enhances the proliferation of cytotoxic CD8+ T cells. FGT-4 has anti-tumor activity in the 4T1 breast cancer mouse model. FGT-4 can be used for the study of cancer immunity.

Creatine ethyl ester (CEE) is a readily available form of creatine used in supplements. Creatine ethyl ester (CEE) upregulates TLRs (TLR2, 3, 4 and TLR7) over the short-term.

AXC-879, a TLR agonist (EC50: 157.2 nM). AXC-879 is an ADC Cytotoxin and can be used for ADC synthesis.

ZSA-51 is a potent and orally active STING agonist. ZSA-51 shows anticancer activity. ZSA-51 remodeles immune microenvironment both in tumor and lymph node.

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.