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iNOS/ PKC-θ Dual Inhibitor
(Rac)-Anemonin is a dual inhibitor targeting inducible nitric oxide synthase (iNOS) and protein kinase C theta (PKC-θ). It selectively inhibits iNOS while also reducing the stability of the PKC-θ protein, showcasing significant biological activity. Research indicates that (Rac)-Anemonin can alleviate symptoms in dextran sodium sulfate-induced acute ulcerative colitis in murine models, making it valuable for studying inflammation-related diseases. -
iNOS/ PKC-θ Dual Inhibitor
Anemonin is a dual inhibitor targeting inducible nitric oxide synthase (iNOS) and protein kinase C theta (PKC-θ). This compound significantly reduces the translation and enhances the protein stability of PKC-θ, demonstrating potent anti-inflammatory effects. Anemonin has been shown to alleviate symptoms of dextran sodium sulfate-induced acute ulcerative colitis in murine models, making it a valuable tool for researching inflammation-related diseases. -
PAD4 Inhibitor
GSK484 is a selective inhibitor of peptidylarginine deiminase 4 (PAD4), effectively blocking the enzyme's catalytic activity to inhibit protein citrullination and neutrophil extracellular trap (NET) formation. This compound demonstrates anti-inflammatory properties by reducing histone H3 production, modulating MHC-I expression, and inhibiting CD8+ T cell activation and proliferation. Research applications include studies on rheumatoid arthritis, sickle cell disease, myocardial ischemia-reperfusion injury, and colitis, as well as investigations into intestinal microbial homeostasis and ferroptosis-related dysbiosis. -
PAD4 Inhibitor
JBI-589 is a non-covalent inhibitor selectively targeting the PAD4 isoform. This compound effectively reduces CXCR2 expression and inhibits neutrophil chemotaxis, making it instrumental in the study of inflammatory processes. JBI-589 demonstrates potential in diminishing primary tumors and metastases while enhancing the efficacy of checkpoint inhibitors. It is suitable for various applications in cancer research. -
HLA-A*0201 Stabilizer
ELTLGEFLKL is a survivin-derived peptide that functions as a stabilizer of HLA-A*0201. This peptide demonstrates significant enhancement of HLA-A*0201 stability, making it a valuable tool in the study of tumor immunotherapy. ELTLGEFLKL can be employed in research focused on optimizing immune responses against cancer through modulation of peptide-MHC interactions. -
CCR3 Antagonist
SB-328437 is a selective non-peptide antagonist of the CCR3 receptor, demonstrating an IC50 of 4.5 nM. This compound effectively inhibits eosinophil migration induced by eotaxin, eotaxin-2, and monocyte chemotactic protein-4, making it valuable in studies of allergic inflammation. Additionally, SB-328437 has shown the ability to sensitize 5-FU-resistant gastric cancer cells and reduce neutrophil recruitment to the lungs, thus mitigating pulmonary inflammation during acute inflammatory responses. Its applications extend to the investigation of various inflammation-related diseases. -
Anti-inflammatory and Analgesic Agent
Deoxyartemisinin (2-Deoxyartemisinin) is an orally active anti-inflammatory and analgesic agent that selectively reduces the pro-inflammatory cytokine TNF-α. This compound demonstrates efficacy in alleviating various forms of pain, including neuropathic and inflammatory pain, as well as reducing croton oil-induced ear edema. Additionally, Deoxyartemisinin exhibits anti-ulcer properties, making it a valuable tool for research focused on inflammatory diseases, pain management, and gastric ulcers. -
TNFSF13B/BAFF/CD257 Inhibitor
Aritinercept is a recombinant fusion protein that functions as an inhibitor of TNFSF13B (BAFF/CD257). This compound effectively neutralizes BAFF and APRIL, leading to reduced B cell proliferation and suppression of peripheral B cells, along with a decrease in serum immunoglobulins. Aritinercept has demonstrated beneficial effects in a mouse model of systemic lupus erythematosus (SLE) by lowering markers of renal damage, as well as reducing levels of IFNγ, IL-17A, and anti-dsDNA autoantibodies. This reagent is suitable for research focused on systemic lupus erythematosus and related autoimmune disorders. -
CXCR6 Antagonist
ML339 is a selective antagonist of the CXCR6 receptor, displaying an IC50 of 140 nM. It inhibits β-arrestin recruitment and the cAMP signaling pathway induced by CXCL16 in human CXCR6, with IC50 values of 0.3 μM and 1.4 μM, respectively. While exhibiting reduced efficacy against mouse CXCR6 with an IC50 of 18 μM, ML339 demonstrates no significant inhibition of CXCR5, CXCR4, or the apelin receptor (APJ), with IC50 values exceeding 79 μM. This compound shows promise for advancing research focused on prostate cancer. -
CXCR Inhibitor
ALX 40-4C is a small peptide inhibitor targeting the chemokine receptor CXCR4. It effectively prevents the binding of SDF-1 to CXCR4 with a Ki of 1 μM, thereby inhibiting the replication of X4 strains of HIV-1. Additionally, ALX 40-4C Trifluoroacetate serves as an antagonist of the APJ receptor, exhibiting an IC50 value of 2.9 μM. This dual activity makes ALX 40-4C a valuable tool for research in HIV-1 studies and chemokine receptor signaling pathways. -
CCR6 Antagonist
IDOR-1117-2520 is a potent and selective reversible antagonist targeting CCR6. It effectively inhibits CCL20-mediated calcium influx with an IC50 of 63 nM and blocks β-arrestin recruitment to human CCR6, showing an IC50 of 30 nM in recombinant cell models. As a substrate of P-glycoprotein/MDR1, IDOR-1117-2520 is a valuable tool for investigating autoimmune diseases and skin inflammation in research settings. -
CXCR Receptor Inhibitor
SCH-900875 is a selective inhibitor of the CXCR3 receptor, known for its oral bioavailability and ability to penetrate the blood-brain barrier. By binding to CXCR3, it effectively prevents the interaction of ligands CXCL9, CXCL10, and CXCL11, thereby inhibiting downstream G protein and β-arrestin signaling pathways, which reduces inflammatory cell migration. This compound holds potential for investigating various autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis, as well as inflammatory conditions like psoriasis and inflammatory bowel disease. -
Anti-inflammatory agent
Emorfazone is a non-steroidal anti-inflammatory drug that functions primarily through the inhibition of bradykinin-like substances and kininogen release. This compound exhibits notable anti-inflammatory and analgesic properties, making it a valuable tool for research on pain management and inflammatory conditions. Its oral activity further expands its application in pharmacological studies aimed at understanding inflammatory pathways. -
Non-steroidal Anti-inflammatory Agent
Zoliprofen is a non-steroidal anti-inflammatory agent that primarily acts by antagonizing bradykinin, leading to significant suppression of bradykinin-induced edema and pain responses. It also exhibits a moderate inhibitory effect on arachidonic acid-induced edema and pain, while additionally inhibiting PGE2 synthesis in bovine vesicular gland microsomes. This dual action makes Zoliprofen a valuable tool for research applications focused on pain management and inflammatory processes. -
CETP Inhibitor/CB1 Agonist
BI-5756 is a selective CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. It promotes a significant increase in HDL-C levels while reducing LDL-C levels, thereby improving lipid profiles. Additionally, BI-5756 enhances the function of regulatory T cells and preserves T cell-mediated anti-tumor activity, exhibiting direct anti-proliferative effects on tumor cells. This compound also upregulates the expression of MHC I, MHC II, and CD80 on tumor cells and demonstrates protective effects in graft-versus-host disease. BI-5756 is applicable in research related to oncology, graft-versus-host disease, and metabolic disorders. -
CB1R/iNOS Antagonist
(Rac)-Zevaquenabant is a potent cannabinoid receptor type 1 (CB1R) and iNOS antagonist, exhibiting a Ki value of 5.7 nM for CB1R. This compound is primarily utilized in studies related to liver fibrosis, providing valuable insights into its pathophysiology and potential therapeutic interventions. Its selective inhibition of CB1R and iNOS pathways makes it a significant tool for investigating cannabinoid signaling and its implications in fibrotic diseases. -
CXCR7 Antagonist
CXCR7 antagonist-1 functions as a CXCR7 antagonist by inhibiting the binding of the SDF-1 (CXCL12) and I-TAC (CXCL11) chemokines to the CXCR7 receptor. This inhibition plays a critical role in suppressing tumor cell proliferation and tumor growth, thereby providing potential therapeutic applications in cancer treatment. Additionally, CXCR7 antagonist-1 may be beneficial in the study and management of various inflammatory diseases and other pathologies associated with the CXCR7 pathway. -
CXCR7 Antagonist
CXCR7 antagonist-1 hydrochloride functions as an antagonist to the CXCR7 receptor, effectively inhibiting the binding of the SDF-1 chemokine (CXCL12) and I-TAC (CXCL11). This compound demonstrates significant potential in research related to tumor cell proliferation and formation, as well as in inflammatory diseases and other pathologies associated with CXCR7 signaling. Its ability to modulate chemokine receptor activity makes it a valuable tool for exploring therapeutic strategies in cancer and inflammation. -
mPGES-1 Inhibitor
Zaloglanstat is a selective microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor, demonstrating an IC50 of 5 nM for human mPGES-1 while sparing COX-1 and COX-2 with IC50 values greater than 10 μM. It effectively inhibits the conversion of prostaglandin PGH2 to prostaglandin PGE2, thereby mitigating inflammation-related overproduction of PGE2 and alleviating pain. In vitro studies show that Zaloglanstat reduces IL-1β-induced PGE2 release in A549 cells and human synovial fibroblasts. It is applicable in research exploring asthma, osteoarthritis, and neurodegenerative diseases, and exhibits effective inhibition of PGE2 release in whole blood from pig and dog models with IC50 values of 161 nM and 154 nM, respectively. -
Anti-inflammatory Agent
3-Hydroxyxanthone is a xanthone compound recognized for its anti-inflammatory properties. It effectively inhibits NADPH-catalyzed lipid peroxidation in human umbilical vein endothelial cells (HUVECs) and suppresses TNF-alpha-induced ICAM-1 expression. This compound is utilized in research focused on understanding inflammatory processes and vascular endothelial function. -
AMPK/Nrf2 Activator
Fortunellin is a flavonoid that acts as an AMPK/Nrf2 activator, derived from the fruits of Fortunella margarita (kumquat). It demonstrates minimal toxicity in murine models and effectively reduces inflammation and reactive oxygen species (ROS) generation in H9C2 cells induced by lipopolysaccharide (LPS). By enhancing the AMPK/Nrf2 pathway, Fortunellin protects against fructose-induced inflammation and oxidative stress, making it a valuable tool for research in diabetic cardiomyopathy. -
SIK Inhibitor
SIK-IN-1 is a potent inhibitor of salt-inducible kinases (SIK1, SIK2, and SIK3), exhibiting IC50 values of 0.1 nM, 0.4 nM, and 1.5 nM, respectively. This compound effectively inhibits the release of TNF-alpha with an IC50 of 0.5 nM and promotes LPS-induced IL-10 release, demonstrating an EC50 of 4 nM in human macrophages. SIK-IN-1 is a valuable tool for research investigating inflammatory responses and macrophage polarization. -
SIK Inhibitor
SIK-IN-2 is a potent inhibitor of salt-inducible kinases (SIK), selectively targeting SIK1, SIK2, and SIK3 with IC50 values of 0.1, 0.2, and 0.4 nM, respectively. This compound has demonstrated significant biological activity by inhibiting the release of TNF-alpha with an IC50 of 0.5 nM and enhancing LPS-induced IL-10 release in human macrophages with an EC50 of 2 nM. SIK-IN-2 is valuable for research applications focused on inflammatory responses and immune modulation. -
AMPK/Nrf2 Activator
Ethyl (E)-ferulate is an activator of the AMPK/Nrf2 signaling pathway, demonstrating significant potential in reducing acute lung injury induced by lipopolysaccharide. This compound exhibits antioxidant and free radical scavenging properties, contributing to its anti-inflammatory and neuroprotective effects. Ethyl (E)-ferulate is a valuable tool for research focused on inflammation and neurodegenerative diseases. -
Anti-inflammatory Agent
1-Terpineol is a lipid-soluble monoterpenoid alcohol recognized for its anti-inflammatory properties. This compound exhibits significant antibacterial and antioxidant activities, making it valuable for various research applications. It is commonly explored in studies related to inflammation and oxidative stress management. -
Antimicrobial and Anti-inflammatory Agent
1-Hydroxy-2-methylanthraquinone targets various biological pathways as an antimicrobial and anti-inflammatory agent. This compound demonstrates significant antimicrobial and antioxidant properties, making it useful for studies related to infection control and inflammation modulation. Its pesticidal activity further broadens its applicability in agricultural research and product development. -
Anti-inflammatory Agent
Anti-inflammatory agent 14, also known as compound 28, is a potent anti-inflammatory compound that inhibits inflammation-related pathways. It exhibits a minimum inhibitory concentration (MIC50) of 2 μM against Mycobacterium tuberculosis strain H37Rv, demonstrating significant antibacterial properties. This reagent is valuable for research applications focused on anti-inflammatory therapies and tuberculosis studies. -
Anti-inflammatory Agent
2-Methyldecalin is a chemical compound known for its anti-inflammatory properties. It exhibits significant antioxidant and antibacterial activities, making it a valuable reagent for studies related to inflammatory conditions. This compound is suitable for various research applications aimed at understanding and mitigating inflammation-related disorders. -
CcrM Inhibitor
NSC177365 is a potent CcrM inhibitor that acts by competitively disrupting DNA binding. It demonstrates significant antibacterial activity, displaying IC50 values of 2.3 μM and 14.6 μM against C. crescentus and M. lincolnii, respectively. Furthermore, NSC177365 has potential applications in reversing neurodegenerative disorders and shows promise as an anticancer agent, making it a valuable tool for chemical research. -
Anti-inflammatory Agent
Vasicinolone is a natural alkaloid that functions primarily as an anti-inflammatory agent. It demonstrates significant anti-inflammatory and antimicrobial activity, making it valuable for research applications related to inflammation and infection. Its potential use in therapeutic development highlights its importance in the study of chronic inflammatory conditions. -
Anti-inflammatory Agent
Anti-inflammatory agent 94 (compound 4b) is a potent cannabinoid ligand targeting the CB1 and CB2 receptors, exhibiting Kis of 29 nM and 8 nM, respectively. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for studying inflammation-related processes. Its application in research may enhance understanding of cannabinoid signaling and its therapeutic potential in inflammatory conditions. -
CCR6 Antagonist
CCR6 antagonist 1 is a selective antagonist of the CCR6 receptor, effectively inhibiting the CCL20/CCR6 signaling pathway. This compound is instrumental in research focusing on autoimmune-mediated inflammatory diseases, particularly inflammatory bowel diseases (IBDs). Its role in modulating the CCR6 axis provides insights into potential therapeutic strategies for managing such conditions. -
CCR Antagonist
Abaucin is a potent CCR2 antagonist, demonstrating an IC50 of 360 nM. It selectively inhibits CCR2 without affecting CCR1, making it a valuable tool for studying immunological responses and inflammatory processes. Abaucin is applicable in research focusing on the role of CCR2 in disease models and therapeutic interventions targeting chemokine receptors. -
CCR Inhibitor
CCR6 Inhibitor 1 is a highly selective inhibitor of the CCR6 receptor, demonstrating IC50 values of 0.45 nM for monkey CCR6 and 6 nM for human CCR6, while exhibiting minimal activity against human CCR1 and CCR7. This inhibitor effectively prevents ERK phosphorylation, making it a valuable tool in the study of signaling pathways. CCR6 Inhibitor 1 is employed in research focused on autoimmune diseases and cancer, facilitating insights into therapeutic strategies targeting CCR6-related pathways. -
CCR7 Antagonist
CCR7 Ligand 1 is a potent allosteric antagonist targeting the human CC chemokine receptor 7 (CCR7), with a dissociation constant (Kd) of 3 nM. This thiadiazole-dioxide compound effectively inhibits arrestin binding upon CCL19 activation, exhibiting an IC50 of 7.3 μM. CCR7 Ligand 1 is valuable for research applications focused on immune response modulation, chemokine signaling pathways, and therapeutic development for related conditions. -
CCR4 Inhibitor
Zelnecirnon is an orally active CCR4 inhibitor that effectively blocks the recruitment of Th2 inflammatory immune cells to inflamed tissues. This compound exhibits potent anti-inflammatory activity, making it valuable in researching allergic inflammation associated with conditions such as atopic dermatitis and asthma. Zelnecirnon serves as a critical tool for understanding and developing therapeutic strategies in inflammatory diseases. -
CCR1 Antagonist
J-113863 is a potent and selective antagonist of the CCR1 receptor, demonstrating IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1, respectively. Additionally, it acts as a strong antagonist of the human CCR3 receptor (IC50 of 0.58 nM), while exhibiting weak antagonistic activity against mouse CCR3 (IC50 of 460 nM). J-113863 shows inactivity toward CCR2, CCR4, and CCR5, as well as LTB4 and TNF-α receptors. This compound is primarily utilized in anti-inflammatory research applications. -
CCR4 Antagonist
C-021 dihydrochloride is a highly effective antagonist of the CC chemokine receptor-4 (CCR4). It significantly inhibits chemotaxis in both human and mouse models, exhibiting IC50 values of 140 nM and 39 nM, respectively. Additionally, C-021 dihydrochloride demonstrates capability in preventing the binding of human CCL22-derived [35S]GTPγS to CCR4, with an IC50 of 18 nM. This compound is valuable for research applications focused on immune response modulation and related therapeutic strategies. -
CCR6 Antagonist
PF-07054894 is a potent and orally active antagonist of the C-C Chemokine Receptor 6 (CCR6), effectively blocking CCR6-mediated chemotaxis with an IC50 of 5.7 nM in vitro. As a target of G protein-coupled receptors (GPCRs), PF-07054894 demonstrates significant potential in the study of inflammatory bowel disease and related immunological disorders, providing a valuable tool for understanding CCR6’s role in inflammation. -
CCR4 Antagonist
C-021 is a potent antagonist of the CC chemokine receptor-4 (CCR4). It effectively inhibits functional chemotaxis in both human and mouse models, exhibiting IC50 values of 140 nM and 39 nM, respectively. Additionally, C-021 demonstrates strong efficacy in blocking the binding of human CCL22-derived [35S]GTPγS to CCR4, with an IC50 of 18 nM. This compound is valuable for research applications focused on immune response modulation and cancer biology. -
CCR10 Antagonist
BI-6901 is a potent and selective antagonist of the CCR10 receptor, exhibiting a pIC50 of 9.0. It demonstrates high selectivity among various GPCRs, including multiple chemokine receptors. BI-6901 has shown efficacy in the murine DNFB model of contact hypersensitivity, making it a valuable tool in inflammation research. -
CCR Antagonist
INCB 3284 is a selective and potent antagonist of the human CCR2 receptor, functioning by inhibiting the binding of monocyte chemoattractant protein-1 to hCCR2, with an IC50 value of 3.7 nM. This compound is of particular interest in studies related to acute liver failure, providing insights into the role of CCR2 signaling in inflammatory processes. Its oral bioavailability makes it a valuable tool for in vivo research applications. -
CCR4 Antagonist
Tivumecirnon is a selective CCR4 antagonist that functions by blocking the interaction of CCR4 with its ligands, CCL17 and CCL22. This mechanism reduces the infiltration of regulatory T cells (Tregs) into the tumor microenvironment, thereby enhancing antitumor activity. It is useful for research applications aimed at understanding immune modulation in cancer therapy. -
CCR2b Antagonist
CCR2 antagonist 4 hydrochloride is a selective antagonist targeting the CCR2b receptor, exhibiting a potent inhibitory effect with an IC50 value of 180 nM. This compound effectively reduces MCP-1-induced chemotaxis, with an IC50 of 24 nM, making it a valuable tool for studying inflammatory pathways. Its application in research includes investigations into immune responses and the role of CCR2 in various disease models, particularly those related to monocyte migration and chronic inflammation. -
CCR Inhibitor
Ilacirnon is a potent CCR2 antagonist that specifically targets the C-C chemokine receptor type 2 (CCR2). This compound exhibits significant inhibitory activity, making it valuable in research focused on inflammatory diseases and immune response modulation. Ilacirnon can be utilized in studies exploring the role of CCR2 in various pathophysiological conditions, including atherosclerosis and chronic kidney disease. -
CCR1 Antagonist
AZD-4818 is a potent, orally active antagonist of the chemokine receptor CCR1. This compound selectively inhibits CCR1 signaling, making it a valuable tool for studying the role of this receptor in various inflammatory conditions. Applications include research into chronic obstructive pulmonary disease (COPD) and other related respiratory disorders. -
CCR2 Antagonist
BMS CCR2 22 is a potent antagonist of CC-type chemokine receptor 2 (CCR2), exhibiting a high binding affinity with an IC50 value of 5.1 nM. This compound demonstrates strong functional antagonism, as evidenced by its calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM. BMS CCR2 22 is valuable for research applications targeting inflammatory responses and immune cell trafficking, providing insights into CCR2-related pathways. -
CCR Antagonist
MK-0812 Succinate is a potent and selective antagonist of the CCR2 receptor. It demonstrates high affinity for CCR2 and effectively inhibits its signaling pathway, making it a valuable tool for research into inflammatory and immune response processes. This compound is particularly relevant for studies focused on chronic pain, cardiovascular diseases, and various inflammatory disorders. -
CCR9 Antagonist
Vercirnon sodium is a potent and selective antagonist of CCR9, acting primarily by inhibiting CCR9-mediated Ca2+ mobilization and chemotaxis. This compound demonstrates significant biological activity, exhibiting IC50 values of 5.4 nM for Ca2+ mobilization and 3.4 nM for chemotaxis in Molt-4 cells. Vercirnon sodium shows high selectivity for CCR9, with IC50 values greater than 10 μM for other CCR and CX3CR subtypes. It effectively inhibits CCL25-directed chemotaxis in both CCR9 splice forms, CCR9A and CCR9B, with IC50 values of 2.8 nM and 2.6 nM, respectively, making it a valuable tool for research in inflammatory responses and related pathways. -
CCR4 Antagonist
CCR4 Antagonist 4 is a selective and potent inhibitor of the CC chemokine receptor-4 (CCR4), exhibiting an IC50 of 0.02 μM. This compound effectively blocks MDC-mediated chemotaxis and Ca2+ mobilization, with IC50 values of 0.007 μM and 0.003 μM, respectively. CCR4 Antagonist 4 is valuable for investigations into allergic inflammation mechanisms and related therapeutic applications.

