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Catalog No.
Product Name
Application
Product Information
Citations
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PSMA Inhibitor
PSMA-IN-3 is a high-affinity inhibitor of Prostate-Specific Membrane Antigen (PSMA), demonstrating an IC50 value of 13 nM. This compound is particularly relevant for the development of 18F-labeled radioligands for positron emission tomography (PET) imaging to detect PSMA expression in prostate cancer. Researchers can utilize PSMA-IN-3 for studies aimed at advancing diagnostic imaging and therapeutic strategies in oncology. -
PSMA Inhibitor
DCFBC is a potent prostate-specific membrane antigen (PSMA) inhibitor, primarily utilized for small animal positron emission tomography (PET) imaging applications. Labeled with fluorine-18, [18F]DCFBC demonstrates preferential uptake in PSMA-expressing tumors, particularly in PIP tumors, while showing minimal uptake in FLU tumors. Additionally, while high accumulation in the kidneys and bladder is observed, the washout of radioactivity is faster compared to PIP tumors. This specificity positions [18F]DCFBC as a valuable tool for studying prostate cancer and assessing PSMA-targeted therapies. -
PSMA Inhibitor
(R)-Zadavotide guraxetan is a potent inhibitor of prostate-specific membrane antigen (PSMA), exhibiting significant antitumor activity. It is primarily utilized in research focused on prostate cancer, contributing to the understanding of targeted therapeutic approaches. This compound serves as a valuable tool for investigating the role of PSMA in cancer biology and evaluating efficacy in preclinical studies. -
SIK2/SIK3 Inhibitor
GLPG3970 is a selective inhibitor of SIK2 and SIK3, targeting these kinases to modulate their activity. This compound demonstrates significant potential in studying inflammatory responses and autoimmune diseases, contributing to the understanding of their underlying mechanisms and potential therapeutic approaches. Its role as a first-in-class inhibitor positions GLPG3970 as a valuable tool in biomedical research focused on these critical areas. -
SIK2/SIK3 Inhibitor
SK-124 is an orally active inhibitor of salt-inducible kinases 2 and 3 (SIK2/SIK3). It selectively inhibits SIK2 and SIK3, leading to enhanced levels of pro-peptide of type I collagen (P1NP) and C-terminal telopeptide of type I collagen (CTX). This modulation results in increased bone formation and bone mass, making SK-124 a valuable tool for research on bone metabolism and associated disorders. -
SIK Inhibitor
YKL-06-062 is a selectively potent inhibitor of salt-inducible kinases (SIKs), demonstrating IC50 values of 2.12 nM, 1.40 nM, and 2.86 nM for SIK1, SIK2, and SIK3, respectively. This compound is pivotal for research involving cellular stress responses, inflammatory processes, and metabolic regulation. Its specificity and efficacy make it a valuable tool for exploring SIK-related signaling pathways in various biological contexts. -
Sik3 Inhibitor
Pterosin B is an orally active indanone and a selective inhibitor of the SIK3 signaling pathway. It has demonstrated key biological activities, including the inhibition of Klf5 expression and a reduction in β-amyloid deposition, making it relevant in Alzheimer's disease research. Additionally, Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mouse models, while also inhibiting cardiomyocyte hypertrophy and improving cognitive impairment and glycemic control. This compound is valuable for studies related to arthritis, neurodegenerative disorders, pathological cardiac hypertrophy, and diabetes. -
SIK Inhibitor
WH-4-025 is an inhibitor of salt-inducible kinases (SIKs), which play a critical role in regulating various cellular processes, including metabolism, inflammation, and transcription. This compound has demonstrated significant biological activity by modulating SIK signaling pathways, making it a valuable tool for investigating the roles of SIKs in cellular response to environmental stressors. WH-4-025 is suitable for research applications aimed at understanding diseases linked to SIK dysregulation, such as metabolic disorders and cancer. -
SIK2 Inhibitor
SIC-19 is a selective inhibitor of SIK2, promoting its degradation through the ubiquitination pathway. This compound exhibits significant antiproliferative activity against cancer cells and enhances the sensitivity of these cells to PARP inhibitors, including Olaparib. Additionally, SIC-19 demonstrates efficacy in ovarian cancer organoids and xenograft models, making it a valuable tool for cancer research and therapeutic development. -
SIK Inhibitor
MR22 is a potent inhibitor of salt-inducible kinases (SIKs), demonstrating excellent selectivity in a representative kinase panel, while lacking activity against STE group kinases. This compound effectively induces centrosome dissociation and contributes to cell-cycle arrest in ovarian cancer cells. MR22 holds potential for research in cancer biology and the therapeutic targeting of SIK-related pathways. -
SIK Inhibitor
SIKs-IN-1 is a pyrimidine-5-carboxamide derivative that functions as an inhibitor of Salt-inducible kinases (SIKs). It modulates the balance between M1 and M2 macrophages, playing a crucial role in the inflammatory response. SIKs-IN-1 effectively inhibits SIK activity, leading to the upregulation of the anti-inflammatory cytokine IL-10 and the downregulation of the pro-inflammatory cytokine IL-12. This compound demonstrates significant anti-inflammatory effects in models of DSS-induced colitis, making it valuable for research into inflammatory diseases. -
SIK1/2 Inhibitor
SIK2-IN-3 is a selective inhibitor of SIK1 and SIK2, with IC50 values of 0.128 μM and 0.084 μM, respectively. This compound effectively inhibits the phosphorylation of CRTC3 and reduces pro-inflammatory cytokine production in myeloid cells. SIK2-IN-3 demonstrates potential in mitigating systemic and tissue inflammatory responses, as evidenced by its efficacy in a mouse anti-CD40 colitis model, making it a valuable tool for research in inflammation and immune response mechanisms. -
SIK2/3 Inhibitor
SIK2/3-IN-1 is a selective inhibitor of Salt-Inducible Kinases 2 and 3 (SIK2/3). It has demonstrated significant efficacy in inhibiting tumor growth in the MV4-11 acute myeloid leukemia (AML) mouse xenograft model, while maintaining animal body weight. This compound is valuable for investigating MEF2C-dependent pathways in acute myeloid leukemia research. -
CD36 Inhibitor
1-Palmitoyl-2-13(S)-HODE-sn-glycero-3-PC is a unique oxidized phospholipid that functions as a potent CD36 inhibitor. It features palmitic acid at the sn-1 position and 13(S)-HODE at the sn-2 position, allowing it to interfere with the binding of 125I-NO2-LDL to CD36-transfected 293 cells, exhibiting an IC50 value greater than 200 μM. This compound is useful for research applications exploring lipid interactions and receptor signaling pathways associated with CD36. -
STING Inhibitor
SN-011 is a selective inhibitor of the STING pathway, displaying an IC50 of 76 nM. By competing with cyclic dinucleotides (CDNs) for the binding site on the STING dimer, SN-011 effectively prevents CDN binding and subsequent STING activation. This compound is valuable for investigating STING-mediated autoimmune and inflammatory diseases, offering insights into therapeutic strategies targeting this critical signaling pathway. -
STING Inhibitor
STING-IN-2 is a potent covalent inhibitor of Stimulator of Interferon Genes (STING), effectively targeting both mouse and human STING isoforms. This compound is instrumental in studying the role of STING in autoinflammatory diseases, facilitating the exploration of therapeutic interventions. Its ability to modulate STING activity makes it a valuable tool for researchers investigating immune response and signaling pathways. -
STING Inhibitor
LB244 is a STING inhibitor that functions by modulating the STING signaling pathway to reduce inflammation. It exhibits a potent inhibitory effect (EC50 = 0.8 μM) on STING-dependent inflammatory responses. While LB244 shows promising potential in preclinical studies, its pharmacokinetic profile suggests limited oral bioavailability in murine models. This compound is suitable for research applications focused on understanding STING-related inflammatory disorders. -
STING Inhibitor
STING-IN-3 is a potent inhibitor of the stimulator of interferon genes (STING), specifically targeting both human and murine STING. It covalently modifies the conserved transmembrane cysteine residue at position 91, effectively preventing activation-induced palmitoylation. This activity provides valuable utility in research applications exploring STING-related pathways in immune response and therapeutic interventions in autoimmune diseases and cancer. -
STING Inhibitor
SN-001 is a selective inhibitor of the STING (Stimulator of Interferon Genes) pathway, exhibiting an IC50 of 3.82 μM. This compound is valuable for investigating the role of STING in immune responses and inflammatory diseases. Its inhibitory activity allows for the evaluation of STING's effects on cytokine production and other immune-related pathways, making it a useful tool for research in immunology and drug development. -
STING Inhibitor
STING-IN-4 is a potent STING inhibitor that effectively reduces the expression and activation of STING and nuclear factor-κB (NF-κB) signaling pathways. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for investigating sepsis and related inflammatory conditions. Researchers can utilize STING-IN-4 to explore the therapeutic potential of modulating STING activity in various biological contexts. -
STING Inhibitor
STING-IN-7 is a potent inhibitor of the Stimulator of Interferon Genes (STING) pathway, demonstrating an IC50 of 11.5 nM. This compound effectively inhibits the phosphorylation of STING, interferon regulatory factor 3 (IRF3), and TANK-binding kinase 1 (TBK1). STING-IN-7 is valuable for investigating the role of STING modulation in autoimmune and inflammatory disease research. -
STING Inhibitor
STING-IN-15 is a potent STING inhibitor that exhibits an IC50 of 116 nM against human STING and 96.3 nM against mouse STING. It effectively disrupts the STING signaling pathway in cellular models, leading to a decrease in the secretion of IFN-β and IP-10, and downregulating the expression of key inflammatory markers such as ISG15, ISG56, and TNF-α. Additionally, STING-IN-15 shows promise in reducing systemic and renal inflammation triggered by STING agonists in murine models, thereby mitigating tissue damage and the overexpression of interferon-related genes. This compound is valuable for research into acute kidney injury and various autoimmune/inflammatory diseases. -
STING Inhibitor
H-151 Alkyne is a selective inhibitor of STING (Stimulator of Interferon Genes). This compound demonstrates potential for modulating immune responses, making it valuable in the study of autoimmune diseases such as systemic lupus erythematosus and scleroderma, as well as autoinflammatory conditions. Its ability to interfere with STING pathways allows researchers to explore therapeutic strategies targeting these diseases. -
STING Inhibitor
STING-IN-5 is a potent inhibitor of the STING pathway, specifically targeting the STING protein to attenuate LPS-induced nitric oxide synthesis in macrophages, with an IC50 value of 1.15 μM. This compound effectively reduces inflammatory responses, making it valuable for research focused on anti-inflammatory diseases and sepsis. Its ability to modulate immune responses highlights its potential in elucidating the role of STING in various pathological contexts. -
STING Inhibitor
STING-IN-14 is a potent STING inhibitor with an IC50 value of 0.6 nM. This compound effectively suppresses the activation of the IRF pathway in THP1-DualTM cells, making it a valuable tool for studying the role of STING in immune responses. STING-IN-14 is particularly relevant for research focused on autoimmune diseases, contributing to a better understanding of disease mechanisms and potential therapeutic interventions. -
STING Inhibitor
STING modulator-3 is a selective STING inhibitor that targets the R232 variant of STING, exhibiting an inhibition constant (Ki) of 43.1 nM in scintillation proximity assays. This compound does not influence IRF-3 activation or TNF-β induction in THP-1 cells, making it a valuable tool for studying STING-mediated signaling pathways and their implications in immune responses and inflammatory diseases. Its specificity and potency provide researchers with a resource for exploring STING-related mechanisms in various biological contexts. -
TLR4/HCN Inhibitor
HCN-IN-1 is a TLR4 inhibitor and modulator of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels, specifically targeting HCN2 and HCN4. It effectively inhibits TLR4-mediated signaling, evidenced by reduced alkaline phosphatase activity. HCN-IN-1 modulates HCN2 currents by shifting the voltage-dependent activation to hyperpolarized potentials and slowing activation kinetics, while also blocking currents through HCN4 channels. This compound demonstrates significant analgesic, anti-inflammatory, and anti-anginal properties, making it valuable for research into inflammatory pain, neuropathic pain, heart failure, and related inflammatory conditions. -
COX Inhibitor
SC57666 is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 26 nM. This compound exhibits anti-inflammatory activity by specifically blocking COX-2, thereby reducing prostaglandin synthesis. SC57666 is valuable for research applications focused on understanding inflammation and pain mechanisms, as well as for screening in drug discovery efforts targeting COX-2 related conditions. -
COX Inhibitor
FR-188582 is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 17 nM. This compound exhibits potent anti-inflammatory activity, making it a valuable tool for studies related to pain and inflammation pathways. Its specificity for COX-2 allows for the exploration of therapeutic applications in conditions such as arthritis and other inflammatory diseases. -
COX Inhibitor
Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor known for its nitric oxide (NO)-donating properties. It effectively modulates increased intrahepatic vascular tone, making it a valuable tool in studying portal hypertension and liver diseases. This compound is utilized in research contexts focused on the therapeutic mechanisms of COX inhibition and its impact on hepatic vascular dynamics. -
COX Inhibitor
RWJ 63556 is an orally active inhibitor of cyclooxygenase-2 (COX-2) and a 5-lipoxygenase inhibitor, exhibiting significant anti-inflammatory properties. This compound is utilized in research to explore its potential therapeutic effects in conditions characterized by inflammation, such as arthritis and other inflammatory diseases. Its selective inhibition may provide insights into the role of COX-2 and lipoxygenase pathways in various biological processes. -
COX Inhibitor
COX-2-IN-6 is a selective cyclooxygenase-2 (COX-2) inhibitor, specifically designed for oral administration and exhibiting gut-restricted properties. With an IC50 value of 0.84 μM and a Ki of 69 nM, COX-2-IN-6 effectively targets COX-2, inhibiting COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM. This compound is utilized in research focused on colorectal cancer chemoprevention, offering valuable insights into inflammatory processes and therapeutic strategies. -
COX-2 Inhibitor
COX-2-IN-28 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 0.054 µM for COX-2, while demonstrating significantly lower inhibitory activity against 15-lipoxygenase (2.14 µM) and cyclooxygenase-1 (13.21 µM). This selective inhibition positions COX-2-IN-28 as a valuable tool for investigating the role of COX-2 in inflammation and pain pathways. It is suitable for research applications focused on inflammatory diseases and therapeutic development targeting COX-2 pathways. -
COX Inhibitor
Tolmetin sodium is a potent inhibitor of cyclooxygenase (COX), demonstrating IC50 values of 0.35 μM for human COX-1 and 0.82 μM for COX-2. As a non-steroidal anti-inflammatory drug (NSAID), it is primarily used for its analgesic and anti-inflammatory properties. Tolmetin sodium is valuable in research applications focused on pain management, inflammation, and associated disorders. -
COX-2 Inhibitor
SD 8381 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2). It demonstrates an IC50 value of 0.0098 μM against human COX-2 and 0.69 μM against human COX-1, indicating a high degree of selectivity. This compound is valuable for research applications focused on inflammation and pain management, as well as studies examining the role of COX-2 in various disease states. -
COX2 Inhibitor
COX-2-IN-56 is a selective inhibitor of cyclooxygenase-2 (COX-2), demonstrating minimal inhibition of cyclooxygenase-1 (COX-1). This compound is valuable for investigating COX-2-dependent disorders, particularly in the context of inflammatory processes. Its specificity makes it suitable for research applications focused on understanding the role of COX-2 in various pathological conditions. -
COX Inhibitor
Benzoylgomisin O is a selective inhibitor of cyclooxygenase enzymes COX-1 and COX-2, as well as 15-lipoxygenase (15-LOX). This compound, isolated from Schisandra rubriflora, exhibits significant anti-inflammatory activity, making it a valuable reagent for research into inflammatory diseases and related pathways. Its ability to modulate lipid mediators positions it as a potential tool in the study of pathophysiological conditions where COX and LOX pathways are implicated. -
COX-1 inhibitor
COX-1-IN-1 is a selective inhibitor of cyclooxygenase-1 (COX-1) with an IC50 value of 0.23 μM, demonstrating a high degree of selectivity over COX-2 (IC50 > 50 μM), resulting in a selectivity index of 217. This compound effectively inhibits platelet aggregation, making it a useful tool in the study of inflammatory processes and cardiovascular research applications. COX-1-IN-1 can aid in understanding the role of COX-1 in various physiological and pathological conditions. -
COX-2 Inhibitor
Desmethyl etoricoxib is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 1 μM in whole blood, demonstrating significant potential in modulating inflammatory responses. It exhibits a lower affinity for COX-1, with an IC50 of 16 μM in U937 cells, highlighting its selectivity. This compound is valuable for research applications targeting inflammatory pathways and exploring therapeutic effects in various inflammatory conditions. -
COX1/2 Inhibitor
COX-1/2-IN-2 is a selective inhibitor of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), demonstrating potent activity with IC50 values of 9.7 ± 0.09 µM for COX-1 and 4.6 ± 1.45 µM for COX-2. This compound is useful in research applications involving inflammation and pain modulation, as it effectively reduces the synthesis of pro-inflammatory prostaglandins. Its utility in pharmacological studies makes it a valuable reagent for exploring COX-related pathways. -
COX-2 Inhibitor
Cassiatannin A is a proanthocyanidin tetramer that acts as a selective COX-2 inhibitor. It has demonstrated significant inhibition rates of 38%, 52%, and 97% at concentrations of 10, 100, and 1000 μg/mL, respectively. This compound is valuable for research into inflammatory processes and the molecular pathways associated with COX-2-mediated responses. -
COX-2 Inhibitor
COX-2-IN-21 is a selective, orally active inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 0.039 μM. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research into inflammatory diseases and pain management. Its selectivity for COX-2 over COX-1 enhances its therapeutic potential while minimizing side effects associated with non-selective NSAIDs. -
iNOS/COX-2 Inhibitor
Longiferone B is a daucane sesquiterpene derived from the rhizomes of Boesenbergia longiflora, acting as an inhibitor of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). It exhibits significant anti-inflammatory properties, effectively reducing nitric oxide production with an IC50 value of 21.0 μM. Longiferone B also suppresses the mRNA expression of iNOS and COX-2, making it a valuable compound for research in inflammation-related studies. -
COX-2 Inhibitor
COX-2-IN-27 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 0.045 µM against COX-2, while demonstrating significantly higher IC50 values of 13.22 µM for COX-1 and 1.67 µM for 15-lipoxygenase (15-LOX). This compound exhibits notable anti-inflammatory activity, making it a valuable tool for research in inflammation-related pathways and the study of COX-2 mediated processes. Its selectivity enables detailed investigations into the role of COX-2 in disease and therapeutic applications. -
COX-1 Inhibitor
VU0487836 is a selective inhibitor of cyclooxygenase-1 (COX-1), exhibiting an IC50 value of 0.36 μM against ovine-derived COX-1. This compound is being investigated as a prototype for developing radiological imaging agents aimed at COX-1 in ovarian cancer. VU0487836 is relevant for research focused on ovarian cancer and may provide insights into therapeutic strategies targeting COX-1 pathways. -
COX-2 Inhibitor
LM-4108 (N-(2-Phenylethyl)-indomethacin amide) is a selective and orally active inhibitor of COX-2, demonstrating an IC50 of 0.06 μM against purified human COX-2. This compound exhibits significant anti-inflammatory properties and has potential applications in cancer prevention. The metabolic stability of LM-4108 varies across species, with half-lives of 11 minutes in rat, 21 minutes in human, and 51 minutes in mouse liver microsomes. -
COX-2 Inhibitor
COX-2-IN-5 is a selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 value of 0.65 µM. This compound is primarily utilized in research focused on inflammation and related pathways. Its potent inhibitory activity makes it an invaluable tool for studying COX-2 mediated processes in various biological contexts. -
COX-2/5-LOX Inhibitor
COX-2/5-LOX-IN-2 is a potent dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). This benzothiophen-2-yl pyrazole carboxylic acid derivative demonstrates significant analgesic and anti-inflammatory properties, exhibiting COX-2 inhibitory activity with an IC50 of 0.01 μM and 5-LOX inhibitory activity with an IC50 of 1.78 μM. COX-2/5-LOX-IN-2 is a valuable tool for research applications aimed at understanding and modulating inflammatory pathways. -
COX Inhibitor
Plantanone A is a selective cyclooxygenase (COX) inhibitor, demonstrating an IC50 of 33.37 μM for ovine COX-1 and 46.16 μM for ovine COX-2. This compound exhibits limited DPPH radical scavenging activity with an IC50 of 467.7 μM. Plantanone A serves as a valuable tool for investigating inflammation-related diseases and their underlying mechanisms. -
COX-2 Inhibitor
COX-2-IN-17 is a potent inhibitor of cyclooxygenase-2 (COX-2) with a remarkable ability to penetrate the blood-brain barrier (BBB), exhibiting an IC50 of 0.02 μM. This compound demonstrates significant anti-inflammatory and analgesic properties, effectively reducing hyperalgesia during both the neurogenic and inflammatory phases. COX-2-IN-17 is suitable for research applications aimed at understanding pain mechanisms and exploring potential therapeutic interventions for inflammatory conditions.
