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Catalog No.
Product Name
Application
Product Information
Citations
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FAP Inhibitor
FAPI-mFS is an irreversible inhibitor of fibroblast activation protein (FAP), which targets FAP's enzymatic activity to enhance cancer cell uptake and retention through covalent binding. This compound is particularly useful for cancer imaging and therapy when labeled with radioisotopes such as 68Ga or 177Lu. Additionally, FAPI-mFS serves as a valuable tool in the synthesis and research of radionuclide-drug conjugates (RDCs), facilitating advancements in targeted cancer treatments. -
FAP Inhibitor
NOTA-FAPI is a fibroblast activation protein (FAP) inhibitor designed for targeted tumor imaging. This compound effectively binds to FAP, facilitating the visualization of tumors with high detection efficacy. NOTA-FAPI demonstrates superior imaging quality, making it a valuable tool for cancer research and diagnostic applications. -
Autotaxin Inhibitor
MHC02181 is a potent inhibitor of Autotaxin (ATX), demonstrating an IC50 value of 9.41 μM. By inhibiting ATX, it plays a critical role in modulating lysophosphatidic acid (LPA) production, which is involved in various physiological and pathological processes. This reagent is valuable for research applications focused on cancer progression, fibrosis, and other ATX-mediated diseases. -
Autotaxin Inhibitor
MHC00188 is an allosteric inhibitor of Autotaxin (ATX) with an IC50 of 2.53 μM. This compound modulates ATX activity, which plays a critical role in the production of lysophosphatidic acid (LPA), a signaling lipid involved in various physiological processes. MHC00188 is useful for research into cancer biology, inflammation, and other conditions related to aberrant LPA signaling. -
COX Inhibitor
Aspirin DL-lysine is a lysine-conjugated derivative of aspirin that functions primarily as a cyclooxygenase (COX) inhibitor. This compound effectively inhibits the synthesis of thromboxane A2 (TXA2) in platelets, leading to a reduction in platelet activation and aggregation. Aspirin DL-lysine is valuable for research applications focused on thrombin generation, particularly in clinical studies involving unstable angina pectoris. -
PI3K/Akt Inhibitor, MAPK Inhibitor, NF-κB Inhibitor, Nrf2/ARE Activator
JRN73958 is a potent inhibitor of the PI3K/Akt, MAPK, and NF-κB signaling pathways. This compound effectively reduces LPS/IFNγ-induced activation of these pathways, making it a valuable tool for investigating their roles in cancer biology, particularly in leukemia research. Additionally, JRN73958 acts as an Nrf2/ARE activator, further expanding its utility in studies related to oxidative stress and cell survival mechanisms. -
FKBP12 Inhibitor
WAY-380153 is an FKBP12 inhibitor that demonstrates moderate binding affinity for FKBP12, with a KD of 19 μM measured via isothermal titration calorimetry and 15 μM via nuclear magnetic resonance. This compound is relevant for research applications involving neurotrophy and neuroprotection, serving as a valuable tool for investigating conditions related to neuronal health and function. -
FKBP12 Inhibitor
ElteN378 is a selective inhibitor of FKBP12. This compound has demonstrated significant biological activity in the modulation of protein folding and signaling pathways. Research applications include investigations into neurodegenerative diseases such as Alzheimer's and Parkinson's, as well as studies on amyotrophic lateral sclerosis, proliferation disorders, and various cancer types. -
FKBP35 Inhibitor
D44 is a selective inhibitor of FKBP35, targeting the PPIase activity essential for Plasmodium survival. With IC50 values of 132 nM for Plasmodium falciparum and 125 nM for Plasmodium vivax, D44 demonstrates significant antiplasmodium activity. This compound is valuable for research applications focused on malaria and other infectious diseases, providing insights into potential therapeutic approaches. -
WNT7A Inhibitor/Photosensitizer
WNT7A-IN-1 is a WNT7A inhibitor that disrupts the interaction between WNT7A and its receptor FZD5, leading to the upregulation of MHC-I expression. This compound enhances the expression of MHC-I and phosphorylated p65 while decreasing the levels of active β-catenin. Additionally, WNT7A-IN-1 serves as a photosensitizer in the green spectral region, making it valuable for research in cancer immunotherapy and photodynamic therapy applications. -
COX-2 Inhibitor
APHS is a selective and covalent inhibitor of cyclooxygenase-2 (COX-2) that exerts neuroprotective effects. By acetylating serine 516 in the active site of COX-2, APHS effectively inhibits prostaglandin production, which is often upregulated in colorectal cancer. In addition to its role as a COX-2 inhibitor, APHS also co-inhibits the WNT signaling pathway, contributing to its anti-tumor mechanisms. This compound is valuable for research into cancer biology and neuroprotection. -
5-LO/COX-2/DPP-4 Inhibitor
Timosaponin A1 is a natural steroidal saponin that acts as an inhibitor of 5-lipoxygenase (5-LO), cyclooxygenase-2 (COX-2), and dipeptidyl peptidase 4 (DPP-4), with IC50 values of 3.29 µM, 36.43 µM, and 33.25 µM, respectively. This compound exhibits anti-inflammatory properties and is relevant for research on conditions such as asthma and diabetes. Its inhibitory effects on key enzymes involved in inflammatory pathways make it a valuable tool for exploring therapeutic strategies in related biological studies. -
Arginase Inhibitor
nor-NOHA monoacetate is a selective and reversible inhibitor of arginase. It induces apoptosis in cells expressing arginase 2 under hypoxic conditions and demonstrates anti-leukemic activity. This compound is valuable for investigating endothelial dysfunction, immunosuppression, and metabolic processes in various biological contexts. -
Arginase Inhibitor
ABH hydrochloride is a potent arginase inhibitor with a Ki value of 8.5 nM. This compound enhances nitric oxide production and downregulates inflammatory mediators, including ICAM-1, VCAM-1, and MCP-1. ABH hydrochloride is utilized in research focused on erectile dysfunction, lung protection, wound healing, blood pressure regulation, and vascular fibrosis. Its dual role in promoting vasodilation and reducing inflammation makes it a valuable reagent for studying cardiovascular and inflammatory diseases. -
Arginase Inhibitor
OATD-02 is a competitive, reversible, noncovalent inhibitor that targets arginase 1 and 2. It exhibits slow offset kinetics with IC50 values of 20 nM for human arginase 1, 39 nM for human arginase 2, 39 nM for mouse arginase 1, and 28 nM for rat arginase 1. OATD-02 effectively disrupts tumor immunosuppression mediated by arginases, making it a valuable tool for research in melanoma and other cancer immunotherapy studies. -
Arginase Inhibitor
ARG1-IN-1 is a potent arginase inhibitor with an IC50 value of 29 nM. This compound effectively inhibits serum arginase activity, leading to increased levels of arginine in various mouse tumor models. ARG1-IN-1 is particularly useful for research applications focused on tumor biology and arginine metabolism in cancer. -
Arginase Inhibitor
NED-3238 is a potent inhibitor of arginase I and II, exhibiting IC50 values of 1.3 nM and 8.1 nM, respectively. This compound is valuable in research focused on metabolic regulation and immune modulation, facilitating studies related to cancer, cardiovascular diseases, and inflammation. Its high specificity and potency make it a suitable tool for investigating arginine metabolism and its implications in various biological processes. -
Arginase Inhibitor
(-)-3-O-Acetylcatechin is an arginase inhibitor that demonstrates significant activity against Leishmania amazonensis, with an IC50 value of 3.7 μM. This compound serves as a valuable tool for investigating leishmaniasis and studying arginase-related metabolic pathways in parasitic infections. Its application in biochemical research may contribute to the development of therapeutic strategies for managing leishmaniasis. -
Arginase Inhibitor
BEC is a competitive inhibitor of the binuclear manganese metalloenzyme arginase, functioning as an arginine analogue with slow-binding characteristics. This compound promotes the increased availability of arginine for nitric oxide synthase, thereby facilitating nitric oxide-dependent smooth muscle relaxation in the corpus cavernosum. As a result, BEC is significant in studies related to penile erection and vascular health. -
Arginase Inhibitor
NG-Hydroxy-L-arginine acetate is a selective arginase inhibitor that participates in modulating the nitric oxide pathway. By interfering with the conversion of arginine to citrulline, it facilitates increased nitric oxide production via nitric oxide synthase. This compound is valuable in research related to cardiovascular health, neurobiology, and inflammation, where nitric oxide signaling plays a critical role. -
COX-2 Inhibitor
Thymohydroquinone is a selective inhibitor of cyclooxygenase-2 (COX-2) with noted anti-SARS-CoV-2 activity. It exhibits cytotoxic properties, antiproliferative effects, and the ability to suppress tumor growth in various cancer models. This compound is applicable in research focused on squamous cell carcinoma, fibrosarcoma, and the pathogenesis and treatment of COVID-19 caused by SARS-CoV-2. -
iNOS Inhibitor
S-Methylisothiourea sulfate serves as a potent, selective, and competitive inhibitor of inducible nitric oxide synthase (iNOS). This compound has demonstrated significant biological activity in reducing nitric oxide production and exhibits protective effects in rodent models of septic shock. Its role in modulating iNOS activity makes it a valuable reagent for research focused on inflammation and immune response mechanisms. -
Nonimmunosuppressive Cyclophilin Inhibitor
NIM258 is a potent nonimmunosuppressive cyclophilin inhibitor, specifically targeting cyclophilin A with a Kd of 1.2 nM. It exhibits significant anti-HCV activity, with an EC50 of 40 nM. This compound serves as a valuable tool for research into HCV infection and its associated pathways. -
CCR5 Inhibitor
DAPTA is a synthetic peptide that acts as a selective inhibitor of the CCR5 receptor. By blocking CCR5, DAPTA interferes with viral entry into host cells, exhibiting significant anti-HIV activity. This compound is valuable for research in virology and the development of therapeutic strategies against HIV. -
HIV-1 Entry Inhibitor
RPR103611 is a derivative of betulinic acid that functions as a potent HIV-1 entry inhibitor. It displays IC50 values of 80 nM for CCR5-tropic virus YU2, 0.27 nM for CXCR4-tropic virus NL4-3, and 0.17 nM for dual tropic virus 89.6. This compound is valuable for research focused on the mechanisms of HIV-1 entry and the development of antiviral therapies. -
CXCR Inhibitor
AMD 3329 octahydrobromide is a potent CXCR4 inhibitor that effectively reduces HIV-1 and HIV-2 viral replication. It demonstrates exceptional antiviral activity with EC50 values of 0.8 nM and 1.6 nM, surpassing the efficacy of related compounds. Additionally, AMD 3329 significantly obstructs the binding of specific CXCR4 monoclonal antibodies and inhibits SDF-1 alpha-induced Ca(2+) influx. This compound also disrupts virus-induced syncytium formation, with an EC50 of 12 nM, making it a valuable tool for HIV research and therapeutic development. -
COX1/2 Inhibitor
Indomethacin sodium is a potent inhibitor of cyclooxygenase enzymes COX-1 and COX-2, exhibiting IC50 values of 18 nM and 26 nM, respectively. This compound demonstrates significant anticancer and anti-infective properties, making it valuable in various biological research applications. Indomethacin sodium is essential for investigating mechanisms related to cancer treatment, inflammation, and viral infections. -
Keap1/S349-p-p62 Interaction Inhibitor
K67 is a selective inhibitor targeting the interaction between Keap1 and S349 phosphorylated p62, with an IC50 of 1.5 μM. This compound demonstrates a weaker inhibitory effect on the Keap1-Nrf2 interaction (IC50 of 6.2 μM) and functions by competitively binding to Keap1's binding site, disrupting the aberrant activation of the p62-dependent Nrf2 pathway. K67 has been shown to inhibit tumor cell proliferation and increase the sensitivity of hepatocellular carcinoma (HCC) cells to chemotherapeutic agents by restoring Keap1-mediated ubiquitination and subsequent degradation of Nrf2. This makes K67 a valuable tool for investigating therapeutic strategies in cancer research. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
CCR3 Inhibitor
ALK4290 is a potent, orally active inhibitor of CCR3, exhibiting a Ki of 3.2 nM for human CCR3. Its biological activity positions ALK4290 as a valuable tool for research into neovascular age-related macular degeneration and Parkinsonism. This compound may help elucidate the role of CCR3 in these diseases, facilitating the development of targeted therapeutic strategies. -
hCCR2 Inhibitor
JNJ-41443532 is a selective antagonist of the human CCR2 receptor, exhibiting an IC50 of 37 nM for binding and demonstrating potent functional antagonism with an IC50 of 30 nM in chemotaxis assays. This compound shows a Ki value of 9.6 µM for murine CCR2 binding. JNJ-41443532 is suitable for research into inflammatory diseases and related inflammatory pathways. -
CCR3 Inhibitor
ALK4290 dihydrochloride is a potent inhibitor of the CCR3 receptor, exhibiting a Ki value of 3.2 nM for human CCR3. This compound demonstrates significant potential for modulating immune responses, making it a valuable tool in the study of neovascular age-related macular degeneration and Parkinson's disease. Researchers can utilize ALK4290 to investigate its effects on CCR3-related signaling pathways and its implications in various pathological conditions. -
CCR2 Inhibitor
ECL1i is an allosteric inhibitor targeting the CCR2 receptor. It selectively disrupts CCL2/CCR2-mediated chemotaxis, thereby impeding the recruitment of CCR2-positive cells. ECL1i has demonstrated efficacy in attenuating disease progression in models of experimental autoimmune encephalomyelitis, making it a valuable tool for studying autoimmune disease mechanisms and potential therapeutic interventions. -
CCR1 Inhibitor
BX-513 is a potent and selective antagonist of the CCR1 receptor. It effectively inhibits the binding of radiolabeled MIP-1α and RANTES to CCR1, with inhibition constants (Ki) of 40 nM and 60 nM, respectively. BX-513 demonstrates the ability to suppress MIP-1α-induced extracellular acidification, as well as MIP-1α- and RANTES-induced intracellular calcium mobilization and peripheral blood mononuclear cell migration. This compound is applicable in research focusing on autoimmune diseases such as rheumatoid arthritis and multiple sclerosis. -
CCR2 Inhibitor-DOTA Conjugate
DOTA-ECL1i is a CCR2 inhibitor conjugated with DOTA, designed for use in positron emission tomography (PET) imaging. When radiolabeled with 68Ga, DOTA-ECL1i provides a specific PET tracer that targets CCR2 expression in various pathological conditions. This compound is applicable in research focused on pulmonary fibrosis, cardiac injury, abdominal aortic aneurysm inflammation, atherosclerosis, and cancers of the head, neck, and pancreas. -
CCR5/CXCR3 Inhibitor
CCR5/CXCR3-IN-1 is a potent inhibitor of the chemokine receptors CXCR3 and CCR5. This compound effectively suppresses the chemotaxis of transformed cells expressing CCR5 and CXCR3, while exhibiting no inhibitory effect on CXCR4-expressing transfected cells. CCR5/CXCR3-IN-1 is valuable for research into chronic arthritic rheumatism and other conditions where modulation of these receptors is crucial.
