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Monoterpenoids
Neral is a monoterpene compound that exhibits anti-inflammatory and anti-cancer properties. It functions by inhibiting pro-inflammatory cytokines such as TNF-α and IL-6, and it downregulates key inflammatory mediators including pro-IL-1β, iNOS, COX-2, and NLRP-3. Neral's biological activities make it valuable for research in inflammation and cancer treatment strategies. -
TLR9 Antagonist
TLR9 antagonist 1 is a selective toll-like receptor 9 (TLR9) antagonist that exhibits an IC50 of 0.1 nM for human TLR9, demonstrating a significant preference over TLR2, TLR4, TLR5, TLR7, and TLR8. This compound is known to exacerbate symptoms in systemic lupus erythematosus (SLE) mouse models by increasing levels of anti-dsDNA and anti-Sm antibodies. TLR9 antagonist 1 is valuable for research in inflammatory and autoimmune diseases, particularly in the study of disorders such as lupus and arthritis. -
STING Agonist
STING Agonist-45 is a selective agonist of the stimulator of interferon genes (STING), exhibiting an EC50 value of 0.28 μM. It activates the innate immune response via the cGAS-STING pathway, leading to the upregulation of critical markers such as p-TBK1 and IRF3. STING Agonist-45 effectively stimulates the production of type I interferons, including IFN-β, as well as cytokines like TNF-α and IL-6 in human peripheral blood mononuclear cells (PBMCs). This compound shows potential in enhancing anti-tumor immunity, inhibiting tumor growth, and promoting CD8+ T cell infiltration in animal models, making it a valuable tool for research into STING-related diseases. -
Anti-inflammatory Agent
Desoxo-narchinol A is a potent anti-inflammatory agent that is derived from the roots and rhizomes of Nardostachys jatamansi. This compound exhibits significant biological activity, making it a valuable tool for research into septic shock and various inflammatory diseases. Its oral activity further enhances its applicability in preclinical studies, providing insight into therapeutic strategies for managing inflammation-related conditions. -
CSE1L/PD-L1 Inhibitor
Naamidine J is an imidazole-type alkaloid that functions as a CSE1L/PD-L1 inhibitor. It demonstrates significant anti-inflammatory activity by reducing pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6, while enhancing the expression of anti-inflammatory markers like CD206 and Arg-1. Additionally, Naamidine J exhibits antitumor properties and alleviates pulmonary tissue edema and inflammatory infiltrates in murine models. This compound is valuable for research focused on the immune microenvironment in the contexts of acute lung injury and cancer. -
Anti-inflammatory Analgesic/Anti-tumor/Diuretic Agent
Hecogenin acetate is an orally active steroid saponin aglycone that functions primarily as an anti-inflammatory and analgesic agent. It exerts its biological effects by inhibiting the phosphorylation of NF-κB and p38 MAPK signaling pathways, antagonizing TRPA1/TRPM8 channels, and reducing the production of pro-inflammatory cytokines. Additionally, Hecogenin acetate demonstrates neuroprotective and anti-tumor properties, inhibits reactive oxygen species (ROS) production, and downregulates MMP-2 expression. This compound also enhances gastric mucosal defense and promotes ulcer healing while potentially restoring antibiotic sensitivity when used in combination with specific antibiotics. -
CD206 Targeting Peptide
RP-832c is a synthetic analogue of host defense peptides that selectively targets the mannose receptor CD206 on M2 polarized macrophages (Kd = 3.5 μM). Binding of RP-832c to CD206 induces significant conformational changes, activating signaling pathways that promote apoptosis and repolarization of M2 macrophages to an M1 phenotype. The treatment with RP-832c effectively reduces CD206 gene expression while transiently increasing TNF-α levels, a hallmark of M1 macrophages. This reagent is valuable for research on T-cell lymphoma (CTCL) and idiopathic pulmonary fibrosis (IPF). -
Anti-inflammatory Agent
Shizukaol B is an anti-inflammatory agent derived from the lindenane-type dimeric sesquiterpene found in Chloranthus henryi. This compound demonstrates significant inhibitory effects against lipopolysaccharide (LPS)-induced activation of BV2 microglial cells, effectively reducing nitric oxide production and downregulating the expression of pro-inflammatory markers such as iNOS, COX-2, TNF-α, and IL-1β. Shizukaol B is suitable for research applications focused on neuroinflammation and related therapeutic strategies. -
TLR3/9 Inhibitor
M199 is a selective inhibitor of TLR3 and TLR9 signaling pathways. This compound effectively induces the secretion of pro-inflammatory cytokines, including IL-6, IL-8, and TNFα, in human peripheral blood mononuclear cells (PBMCs). M199 is utilized in research to investigate immune response modulation and the role of TLR signaling in various biological processes. -
Anti-inflammatory Agent
Chloranthalactone B is a lindenane-type sesquiterpenoid that functions as an anti-inflammatory agent. Isolated from the Chinese medicinal herb Sarcandra glabra, this compound effectively inhibits the production of inflammatory mediators by targeting the AP-1 and p38 MAPK signaling pathways. Its role in modulating inflammation makes it a valuable tool for research in inflammation-related studies and therapeutic applications. -
CD27 Agonist
MG-C-30 is a potent oral agonist of CD27, demonstrating an EC50 of 0.84 μM. This compound activates natural killer (NK) cells and enhances T cell co-stimulatory signals, thereby augmenting the immune response. MG-C-30 has also shown significant antitumor efficacy in the EG7-OVA mouse model, making it a valuable tool for research in immunotherapy and cancer treatment. -
Anti-neuroinflammatory Agent
Grossamide is a natural compound extracted from the dried fruit of Cannabis sativa L. Its primary mechanism involves anti-neuroinflammatory activity, making it a valuable agent for research into neuroinflammatory conditions. Grossamide has potential applications in studies focused on neuroprotection and inflammation-related pathways in the nervous system. -
Anti-inflammatory Agent
EM-163 is an anti-inflammatory agent that selectively targets the TIR domain of MyD88. By intervening in the inflammatory signaling pathways, EM-163 has demonstrated efficacy in alleviating inflammation and protecting against toxic shock. This compound is particularly relevant for research related to Staphylococcal enterotoxin B (SEB) poisoning, providing a valuable tool for investigators studying inflammatory responses and potential therapeutic interventions. -
Geraniol Derivative
Geranial, a derivative of geraniol, primarily targets inflammatory pathways. It exhibits anti-inflammatory activity by inhibiting the secretion of pro-inflammatory cytokines such as TNF-α and IL-6 from macrophages. Additionally, Geranial inhibits IL-1β secretion via the NLRP-3 inflammasome, making it a valuable tool for research focused on inflammation and immune response modulation. -
Anti-Inflammatory Agent
Skimmin, a glucoside of umbelliferone, is primarily recognized for its anti-inflammatory properties. Extracted from Hydrangea paniculata, this compound exhibits renal protective effects by enhancing creatinine clearance and mitigating kidney injury. Additionally, Skimmin demonstrates significant anti-amoebic activity against Entamoeba histolytica, as well as anti-cancer and neuroprotective effects. Its influence on cardiac health is evident through the reduction of fibrosis and the modulation of inflammatory cytokines, including TNF-α and IL-6. Skimmin serves as a valuable research tool in the study of diabetes and associated metabolic disorders. -
Anti-inflammatory Agent
1,4-Dicaffeoylquinic acid is a phenylpropanoid compound that functions as an anti-inflammatory agent through the inhibition of xanthine oxidase, with an IC50 of 7.36 μM. This compound effectively reduces inflammation by inhibiting the production of TNF-α induced by lipopolysaccharides (LPS). Its role in modulating inflammatory responses makes 1,4-Dicaffeoylquinic acid a valuable tool for research in inflammation-related studies. -
Selective Intranasal TLR7 Agonist
GSK2245035 is a selective intranasal agonist for Toll-Like Receptor 7 (TLR7), exhibiting potent Type-1 interferon (IFN) stimulation, with pEC50 values of 9.3 for IFNα and 6.5 for TFNα. This compound demonstrates efficacy in suppressing allergen-induced Th2 cytokine production in human peripheral blood cell cultures, making it a valuable tool for asthma research. Its unique mechanism of action highlights its potential in studying immune responses and therapeutic applications in allergic conditions. -
Anti-inflammatory Agent
9-Methoxycanthin-6-one, an alkaloid derived from canthin-6-one, acts as an anti-inflammatory agent. This compound demonstrates notable anti-tumor activity and effectively inhibits LPS-induced production of pro-inflammatory cytokines such as TNF-α and IL-1β. It is utilized in research applications focused on inflammation and tumor biology. -
Anti-inflammatory Agents
(±)-Perillaldehyde is an anti-inflammatory agent that demonstrates significant biological activity by inducing JNK activation in RAW264.7 cells. This compound inhibits the expression of TNF-α, with an IC50 value of 171.7 μM, highlighting its potential in modulating inflammatory responses. Additionally, (±)-Perillaldehyde exhibits antidepressant effects through its action on the olfactory nervous system, making it relevant for research into stress-related disorders. -
GPRC5D/CD3ε/TNFRSF17 Antibody
Ramantamig is a humanized monoclonal antibody that targets CD3ε on T cells, as well as GPRC5D and TNFRSF17 (BCMA) on multiple myeloma cells. It facilitates T-cell-mediated cytotoxicity by forming immunological synapses, leading to selective killing of myeloma cells without non-specific T-cell activation when target cells are absent. Additionally, Ramantamig has been engineered to minimize interactions with Fc receptors, enhancing its specificity. This reagent is ideal for research in multiple myeloma therapies. -
Anti-inflammatory Agent
7,3',4'-Tri-O-methylluteolin is a flavonoid that acts as an anti-inflammatory agent by inhibiting soybean lipoxygenase (LOX), with an IC50 value of 23.97 µg/mL. This compound demonstrates significant anti-inflammatory effects in LPS-induced RAW 264.7 macrophages and has been shown to inhibit the MDM2-p53 binding, thereby inducing apoptosis in MCF-7 breast cancer cells. Furthermore, 7,3',4'-Tri-O-methylluteolin exhibits antioxidant, antifungal, and antitrypanosomal properties, making it valuable for various biological research applications. -
TLR4 Activator
Kdo2-Lipid A ammonium is a selective TLR4 activator known for its potent endotoxin activity comparable to that of lipopolysaccharide (LPS). It effectively stimulates the release of pro-inflammatory mediators, including tumor necrosis factor (TNF) and prostaglandin E2 (PGE2). This compound is widely utilized in immunological research to investigate TLR4 signaling pathways and the associated inflammatory responses. -
Anti-inflammatory Agent
Episappanol is a natural compound derived from the heartwood of Caesalpinia sappan, functioning primarily as an anti-inflammatory agent. It effectively inhibits the secretion of pro-inflammatory cytokines, including IL-6 and TNF-α. This compound is valuable for research applications aimed at exploring inflammation-related pathways and potential therapeutic interventions for inflammatory diseases. -
Anti-Inflammatory Agent
Kaempferol 3-O-sophoroside is an anti-inflammatory agent that functions primarily by inhibiting the toll-like receptors TLR2 and TLR4 associated with High mobility group box 1 (HMGB1). This compound displays notable anti-inflammatory and analgesic properties, primarily through the inhibition of NF-κB activation and the subsequent reduction of TNF-α production. Additionally, it promotes the synthesis of brain-derived neurotrophic factor (BDNF) and enhances autophagy via AMP-activated protein kinase (AMPK) activation, contributing to its antidepressant effects. Kaempferol 3-O-sophoroside is a valuable tool for research focused on inflammation and neurodegenerative diseases. -
Anti-inflammatory Agent
Edpetiline is an anti-inflammatory agent that targets the inhibition of IκB phosphorylation, thereby preventing the nuclear translocation of NF-κB p65. This compound also inhibits p38 MAPK and ERK MAPK phosphorylation, leading to reduced intracellular ROS levels. Furthermore, Edpetiline downregulates pro-inflammatory cytokines such as TNF-α, IL-6, iNOS, and COX-2 while promoting the expression of the anti-inflammatory cytokine IL-4. It is suitable for research into conditions related to inflammation and oxidative stress. -
ROS/iNOS/TNF-α/COX-2 Inhibitor
Callistephin chloride is an anthocyanin that functions as an inhibitor of reactive oxygen species (ROS) and nitric oxide synthase (iNOS), as well as tumor necrosis factor-alpha (TNF-α) and cyclooxygenase-2 (COX-2). This compound regulates the expression of inflammatory and apoptosis-related proteins by inhibiting p38 phosphorylation, thereby enhancing the protective effects against microglial cell damage. Callistephin chloride also significantly reduces ROS levels, mitigates glutamate excitotoxicity, and provides neuroprotection to cerebellar granule neurons. Additionally, it inhibits the proliferation and metastasis of breast cancer cells through the induction of apoptosis. -
Arginase Inhibitor
L-Norvaline is an arginase inhibitor that enhances nitric oxide production and reduces oxidative stress. It has been shown to improve insulin resistance and demonstrates antioxidant and anti-hyperglycemic properties. This compound is particularly relevant in research related to Alzheimer's disease and other metabolic disorders. -
TLR1/TLR2 Agonist
Diprovocim is a potent TLR1/TLR2 agonist that activates immune responses by inducing full agonist activity in human THP-1 cells, with an EC50 of 110 pM. This compound effectively stimulates TNF-α release from mouse macrophages at an EC50 of 1.3 nM. By activating downstream signaling pathways, including MAPK and NF-κB, Diprovocim demonstrates significant adjuvant activity in mice, enhancing cellular immune responses and making it a valuable tool for immunological research. -
Anti-inflammatory Agent
Taurohyodeoxycholic acid sodium is the taurine-conjugated derivative of hyodeoxycholic acid, serving as an anti-inflammatory agent. It effectively reduces the activity and expression of myeloperoxidase, TNF-α, and IL-6, demonstrating protective effects against colonic damage in TNBS-induced ulcerative colitis models. This compound is valuable for researchers investigating inflammatory pathways and therapeutic strategies in gastrointestinal disorders. -
Proinflammatory Cytokine Inhibitor
Semapimod tetrahydrochloride is a potent inhibitor of proinflammatory cytokine production, specifically targeting tumor necrosis factor-alpha (TNF-α), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6). This compound effectively disrupts Toll-like receptor 4 (TLR4) signaling with an IC50 of approximately 0.3 μM, thereby inhibiting p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride holds promise for the treatment of various inflammatory and autoimmune disorders through its modulatory effects on immune responses. -
PD-L1/HDAC6 Inhibitor
PD-L1/HDAC6-IN-1 is a dual inhibitor targeting PD-L1 and HDAC6, effectively disrupting the PD-L1/PD-1 interaction with IC50 values of 26.8 nM and 69 nM, respectively. This compound significantly enhances the cytotoxicity of Jurkat T cells against HepG2 cells with an IC50 of 3.4 μM. Additionally, PD-L1/HDAC6-IN-1 demonstrates favorable pharmacokinetics in rat models, achieving a drug exposure level of 871.62 ng·h/mL, and shows promising antitumor efficacy in B16-F10 xenograft models in mice. -
PD-L1/HDAC Inhibitor
PD-L1/HDAC-IN-1 is a dual inhibitor targeting PD-L1, HDAC2, and HDAC3, with IC50 values of 88.10 nM, 27.98 nM, and 14.47 nM, respectively. This compound effectively disrupts the PD-1/PD-L1 interaction and demonstrates minimal cytotoxicity in MCF-7 cells (IC50=19.34 μM). PD-L1/HDAC-IN-1 enhances the expression of PD-L1 and CXCL10, thereby facilitating an anti-tumor immune response through increased T-cell recruitment into the tumor microenvironment (TME). Its unique mechanism positions it as a valuable tool for research in cancer immunotherapy. -
COX-2/HDAC Inhibitor
Andrographidine E is an inhibitor of cyclooxygenase-2 (COX-2) and histone deacetylases (HDAC), with an IC50 of 19 μM for COX-2 and a strong affinity for HDAC1 and HDAC3. This compound selectively binds to macrophages, suggesting its potential as an immunotargeting agent. Andrographidine E is valuable for research applications focused on inflammation and immune modulation. -
Anti-Inflammatory Agent
Triamcinolone acetonide is a potent anti-inflammatory agent that primarily targets fibroblast growth factor (bFGF) signaling pathways. It effectively inhibits bFGF-induced proliferation of retinal endothelial cells, promotes macrophage activation with anti-inflammatory properties, and reduces chondrocyte viability, contributing to cartilage degradation. This compound is valuable for research applications related to various inflammatory conditions, including atopic dermatitis. -
Nrf2 Activator
Dimethyl fumarate is an orally bioavailable Nrf2 activator that enhances the expression of antioxidant genes. This compound has been shown to induce necroptosis in colon cancer cells via mechanisms involving glutathione depletion, reactive oxygen species elevation, and activation of MAPK pathways. Additionally, Dimethyl fumarate promotes autophagy and is applicable in studies focused on multiple sclerosis and related neurodegenerative conditions. -
Anti-inflammatory Agents
Balsalazide disodium is a prodrug that releases mesalamine in the colon, primarily targeting anti-inflammatory pathways. It exhibits significant anti-inflammatory activity in conditions such as colitis and demonstrates potential anticancer effects through modulation of the IL-6/STAT3 signaling pathway. This compound is useful in research focused on gastrointestinal disorders and cancer therapy. -
Anti-inflammatory Agent
Luteolin 5-O-glucoside is a potent anti-inflammatory agent derived from Cirsium maackii. This compound effectively inhibits lipopolysaccharide (LPS)-induced nitric oxide production and tert-butyl hydroperoxide (t-BHP)-induced reactive oxygen species generation. Additionally, Luteolin 5-O-glucoside downregulates the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in macrophages, making it valuable for research in inflammatory pathways and related conditions. -
Anti-inflammatory Agent
Ajugol is an orally active iridoid glycoside that functions as an anti-inflammatory agent. It activates TFEB-mediated autophagy and lysosomal biogenesis, contributing to its protective effects on cellular homeostasis. Ajugol demonstrates significant potential for research in conditions such as asthma, non-alcoholic fatty liver disease (NAFLD), and osteoarthritis due to its dual role in promoting autophagy and mitigating inflammation. -
PDE IV Inhibitor/A1AR Antagonist
Doxofylline is an orally active phosphodiesterase IV (PDE IV) inhibitor and adenosine A1 receptor (A1AR) antagonist. It exhibits anti-inflammatory properties by reducing mitochondrial reactive oxygen species (ROS) production and modulating various cellular pathways, including the NLRP3-TXNIP inflammasome activation. This compound is valuable for research related to respiratory diseases such as asthma, chronic obstructive pulmonary disease (COPD), and bronchospasm. -
Nonsteroidal Anti-inflammatory Agent
2-Ethoxybenzamide is a nonsteroidal anti-inflammatory agent that exhibits both analgesic and antipyretic activities. Its mechanism involves the induction of melanin synthesis through the phosphorylation of cAMP response element-binding protein (CREB). This compound is valuable for research focused on hypopigmentation and inflammation-related diseases, providing insights into therapeutic applications and biological pathways involved in these conditions. -
PD-1/PD-L1 Interaction Inhibitor
PD-1/PD-L1-IN 3 is a macrocyclic peptide that acts as a selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions. By binding to PD-L1, it effectively disrupts the binding of PD-L1 to PD-1 and CD80, exhibiting IC50 values of 5.60 nM and 7.04 nM, respectively. This compound is valuable for research in various fields, particularly in cancer immunotherapy and the study of infectious diseases. -
Anti-inflammatory Agent
Salsalate is an anti-inflammatory agent primarily targeting the modulation of cytokine expression without direct cyclooxygenase inhibition. This compound exhibits significant anti-inflammatory effects and has been shown to lower blood glucose levels, enhance insulin sensitivity, and mitigate the effects of metabolic disorders associated with high-fat diets. Salsalate is utilized in research pertaining to type 2 diabetes, atherosclerosis, and non-alcoholic steatohepatitis, demonstrating its potential in the management of metabolic disorders. -
COX-1/cAMP Phosphodiesterase Inhibitor
Triflusal is a dual inhibitor of Cyclooxygenase-1 (COX-1) and cAMP phosphodiesterase, which penetrates the blood-brain barrier. It effectively inhibits platelet aggregation, nuclear factor kappa B (NF-κB) activation, inducible nitric oxide synthase (iNOS) activity, and prostaglandin synthesis in ischemic tissues. Additionally, Triflusal enhances neutrophil nitric oxide production, endothelial nitric oxide synthase (eNOS) expression, and constitutive nitric oxide synthase (cNOS) activity. This compound is valuable for investigating thromboembolic and ischemic diseases of the cardiovascular and cerebrovascular systems, as well as Alzheimer's disease pathology. -
Nrf2 Activator
Raffinose serves as an Nrf2 activator and is known for its ability to modulate intestinal flora. It inhibits the TLR4-MyD88-NF-κB signaling pathway while promoting Nrf2 signaling, contributing to its anti-inflammatory, antioxidant, and immunomodulatory properties. This compound is orally active and is valuable in research applications focusing on inflammation and oxidative stress. -
β/α-1 Blocker
Carvedilol phosphate hemihydrate is a non-selective β/α-1 adrenergic receptor blocker. It demonstrates significant biological activity by inhibiting lipid peroxidation with an IC50 of 5 μM and acts as a multiple-action antihypertensive agent, with potential applications in treating angina and congestive heart failure. Additionally, carvedilol phosphate hemihydrate has been identified as an autophagy inducer that suppresses the NLRP3 inflammasome, making it valuable for research in inflammation and cardiovascular diseases. -
nNOS Inhibitor
NXN-188 is a selective nNOS inhibitor that also acts as an agonist for the 5HT-1B/1D receptors. This compound exhibits potential in modulating neurogenic inflammation and is particularly relevant in research focused on migraine pathophysiology and treatment strategies. Its dual action supports investigations into the intricate mechanisms underlying headache disorders. -
COX Inhibitor
Pentagamavunon-1 (PGV-1) is a COX-2 inhibitor that modulates multiple molecular pathways to induce apoptosis. This Curcumin analog exhibits notable oral bioactivity and suppresses key angiogenic factors, including vascular endothelial growth factor (VEGF). Additionally, PGV-1 inhibits NF-κB activation, highlighting its potential in cancer research and therapeutic applications targeting inflammation and tumor progression. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-piperazine-Boc is an E3 ligase ligand-linker conjugate that serves as an intermediate in the synthesis of PROTAC targeting B-cell lymphoma 6 protein (BCL6). This compound plays a significant role in targeted protein degradation, facilitating the selective destruction of BCL6 and aiding in research related to cancer therapeutics. Its application is essential for studies focusing on E3 ligase modulation and PROTAC development in oncology. -
CD47-SIRPα axis Inhibitor
DMUP is a potent inhibitor of the CD47-SIRPα axis. This compound promotes apoptosis and enhances macrophage phagocytosis in A549 lung cancer cells, while also reducing the expression of CD47 and SIRPα proteins. DMUP demonstrates significant antitumor activity, making it a valuable tool for research in cancer immunotherapy and macrophage biology. -
PD-1/PD-L1 Inhibitor
PD-1/PD-L1-IN-10 is a potent orally active inhibitor of the PD-1/PD-L1 interaction, with an IC50 value of 2.7 nM. This compound exhibits significant anticancer efficacy by blocking the immune checkpoint pathway, thereby enhancing T-cell activation and promoting anti-tumor responses. PD-1/PD-L1-IN-10 is valuable for research in immunotherapy and cancer treatment studies.

