NF-κB/IκB

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  1. ACAT Inhibitor

    ACAT-IN-3 is an inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT), targeting the cholesterol esterification pathway. This compound effectively inhibits NF-κB-mediated transcription, making it a valuable tool in studying pathways associated with inflammation and lipid metabolism. Its application in research may help elucidate the role of ACAT in various disease models, particularly those related to atherosclerosis and other metabolic disorders.
  2. ACAT Inhibitor

    ACAT-IN-5 is a selective inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT), a key enzyme involved in cholesterol metabolism. By inhibiting ACAT activity, ACAT-IN-5 has been shown to modulate NF-κB mediated transcription, thereby influencing inflammatory pathways and lipid metabolism. This reagent is vital for research applications exploring cholesterol homeostasis, atherosclerosis, and related metabolic disorders.
  3. HDAC Inhibitor

    HDAC-IN-54 is a potent histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 25 nM for human HDAC1, 66 nM for HDAC2, 6.5 nM for HDAC3, and 281 nM for HDAC6. This compound effectively induces acetylation of α-tubulin and histone H3, promoting cancer cell apoptosis, particularly in synergy with cisplatin. HDAC-IN-54 is relevant for research applications in head and neck cancer, ovarian cancer, and tongue squamous cell carcinoma.
  4. Anti-neuroinflammatory Agent

    SB26019 is a potent anti-neuroinflammatory agent that primarily targets NF-κB activation. It functions by promoting the formation of monomeric α-tubulin, which in turn inhibits the translocation of the p65 subunit of NF-κB. This mechanism underscores its potential application in neuroscience research, particularly in studies related to neuroinflammation and associated disorders.
  5. MyD88 Inhibitor

    T6167923 is a selective inhibitor of MyD88-dependent signaling pathways, targeting the Toll/IL-1 receptor (TIR) domain of MyD88 to disrupt its homodimeric formation. This compound effectively inhibits NF-κB-mediated Staphylococcus enterotoxin AP (SEAP) activity, demonstrating notable anti-inflammatory effects with IC50 values of 2.7 μM for IFN-γ, 2.9 μM for IL-1β, 2.66 μM for IL-6, and 2.66 μM for TNF-α. T6167923 serves as a valuable tool in studying the role of MyD88 signaling in inflammatory responses and therapeutic interventions.
  6. Myd88 Inhibitor

    MyD88-IN-1 is a potent inhibitor of MyD88, targeting the interaction between TLR4 and MyD88. By suppressing the NF-κB signaling pathway, MyD88-IN-1 demonstrates significant biological activity relevant to cancer and inflammatory research. This compound serves as a valuable tool for elucidating the role of MyD88 in various disease processes and therapeutic interventions.
  7. Quinazoline alkaloid

    Dehydroevodiamine is a key bioactive quinazoline alkaloid derived from Evodiae Fructus, primarily known for its antiarrhythmic properties demonstrated in guinea pig ventricular myocytes. This compound effectively inhibits the expression of lipopolysaccharide (LPS)-induced inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), prostaglandin E2 (PGE2), and nuclear factor-kappa B (NF-κB) in murine macrophage cells. Its diverse biological activities make it a valuable reagent for research focused on cardiovascular function and inflammatory responses.
  8. Syk Inhibitor

    DBMB is a selective inhibitor of spleen tyrosine kinase (Syk) that effectively attenuates Syk kinase activity. Its mechanism of action involves the suppression of NF-κB signaling, leading to a decrease in the production of key inflammatory mediators, including nitric oxide (NO) and prostaglandin E2 (PGE2). DBMB is suitable for investigations focused on inflammatory diseases and elucidating the role of Syk in immune response pathways.
  9. iNOS Inhibitor

    Asperuloside is an iridoid compound derived from Hedyotis diffusa, primarily known for its role as an inducible nitric oxide synthase (iNOS) inhibitor. This compound exhibits notable anti-inflammatory properties by suppressing the NF-κB and MAPK signaling pathways. Asperuloside is valuable in studying inflammatory processes and developing therapeutic strategies for related diseases.
  10. NF-κB Inhibitor

    Neocryptotanshinone is a potent NF-κB inhibitor derived from Salvia miltiorrhiza. This compound effectively suppresses lipopolysaccharide-induced inflammation by targeting and inhibiting the NF-κB and iNOS signaling pathways. It shows promise in research applications focused on inflammatory diseases and provides valuable insights into the mechanisms of immune response modulation.
  11. iNOS/Nf-Κb Inhibitor

    Hymenoxin is a dual inhibitor of inducible nitric oxide synthase (iNOS) and nuclear factor kappa B (NF-κB), exhibiting IC50 values of 42.7 μM and 85.5 μM, respectively. This compound demonstrates the capacity to reduce oxidative stress by 16% at a concentration of 125 μg/mL. Hymenoxin is primarily utilized in research focused on inflammatory responses and related signaling pathways. Its inhibitory effects on key regulators make it valuable for studies investigating the roles of iNOS and NF-κB in various disease models.
  12. Anti-apoptotic Agent

    Bacoside A is an anti-apoptotic triterpenoid saponin derived from Bacopa monnieri, known for its ability to penetrate the blood-brain barrier. It exhibits significant antioxidant, anti-inflammatory, and neuroprotective properties by modulating the activities of ATPases, AChE, CaMK2A, and iNOS. Bacoside A helps maintain ion balance, scavenges reactive oxygen species, and regulates NF-κB and apoptosis-related proteins, thereby protecting nerve cells from stress-induced damage and exerting non-apoptotic cytotoxicity against glioblastoma cells. Its applications extend to research in neurological disorders, including Parkinson's disease and glioblastoma multiforme.
  13. Anti-Inflammatory Agent

    PPM-18 (NSC 73233) is a potent anti-inflammatory agent that inhibits nitric oxide synthase (iNOS) expression by preventing NF-κB from binding to its promoter. This compound has demonstrated the ability to induce autophagy and apoptosis in bladder cancer cells, mediated through reactive oxygen species (ROS) and AMP-activated protein kinase (AMPK) signaling pathways. PPM-18 is valuable for researchers studying inflammation and cancer therapeutics.
  14. NOS Inhibitor

    SDMA (p-hydroxyazobenzene-p′-sulfonate) is a potent endogenous inhibitor of nitric oxide synthase (NOS), making it a valuable tool for studying NOS-related pathways. This compound has been shown to activate NF-κB, leading to increased expression of pro-inflammatory cytokines such as IL-6 and TNF-α. Additionally, SDMA demonstrates stability in serum and plasma, allowing its use as a biomarker for assessing hepatic and renal dysfunction in various research applications.
  15. iNOS/ICAM-1 Inhibitor

    Aloenin aglycone is an inhibitor of iNOS and ICAM-1, derived from aloe exudate. It effectively suppresses TNFα-induced NF-κB transcriptional activity with an IC50 of 18.7 μM. Additionally, at a concentration of 10 μM, it significantly reduces the expression of both inducible nitric oxide synthase (iNOS) and intercellular adhesion molecule 1 (ICAM-1) in HepG2 cells following TNFα stimulation. This compound serves as a valuable tool for investigating inflammatory pathways and potential therapeutic interventions in related conditions.
  16. Anti-inflammatory Agent

    Anti-inflammatory Agent 65 is a Hederagonic acid derivative that exhibits significant anti-inflammatory activity. This compound effectively inhibits the release of nitric oxide (NO) and prevents the nuclear translocation of IRF3 and p65. By disrupting the STING/IRF3/NF-κB signaling pathway, Anti-inflammatory Agent 65 significantly reduces the inflammatory response, making it a valuable tool for studying inflammation-related conditions and potential therapeutic interventions.
  17. FOXP3 Inhibitor

    Peptide P60 is a potent FOXP3 inhibitor that disrupts the nuclear translocation of FOXP3, thereby decreasing its regulatory effects on NF-κB and NFAT signaling pathways. This action inhibits the immunosuppressive capabilities of regulatory T cells, facilitating the proliferation and activation of effector T cells. Experimental studies have shown that Peptide P60 can induce lymphoproliferative autoimmune syndrome in neonatal ICR mice and diminish the population of CD4+CD25+Foxp3+ T cells in the spleen. Additionally, it enhances the efficacy of peptide vaccines and recombinant adenovirus-based vaccines, making it valuable for research in tumor immunology, viral infections, and autoimmune conditions.
  18. RANKL Inhibitor

    RANKL-IN-1 is a selective and orally bioactive inhibitor of Receptor Activator of Nuclear Factor-κB Ligand (RANKL), displaying a KD value of 7.6 μM. This compound effectively inhibits osteoclastogenesis with an IC50 of 0.07 μM and a selectivity index of 82.57. RANKL-IN-1 directly interacts with RANKL, preventing downstream activation of the NF-κB and MAPK signaling pathways. It is a valuable tool for investigating metabolic disorders, particularly osteoporosis.
  19. 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.
  20. STING PROTAC Degrader

    PROTAC STING degrader-3 is a potent STING PROTAC degrader that operates through the ubiquitin-proteasome pathway, exhibiting a DC50 of 0.62 μM. This compound facilitates STING degradation, resulting in the inhibition of STING/TBK1/NF-κB signaling, thereby exerting notable anti-inflammatory effects. Additionally, PROTAC STING degrader-3 demonstrates renal protective properties and serves as a valuable tool for investigating acute kidney injury (AKI).
  21. Cyclic Guanosine Monophosphate

    3'2'-cGAMP is a cyclic guanosine monophosphate-adenosine monophosphate isomer that selectively targets Drosophila STING (dSTING). It activates the dSTING-NF-κB signaling pathway, leading to the upregulation of Sting-regulated genes and establishing a robust antiviral state in vivo. Additionally, 3'2'-cGAMP is resistant to degradation by viral poxins, making it a valuable tool for investigating viral infections and related biological processes.
  22. NF-κB Inhibitor

    Eupenicisirenin C is a potent inhibitor of the NF-κB signaling pathway. This compound effectively suppresses the cGAS-STING pathway, demonstrating significant potential in modulating inflammatory responses. Notably, Eupenicisirenin C inhibits RANKL-induced osteoclast differentiation in bone marrow macrophages, making it a valuable tool for research into bone metabolism and inflammatory diseases.
  23. TLR7 Agonist

    SMU-L11 is a selective TLR7 agonist with an EC50 of 0.024 μM, which engages the MyD88 adapter protein to activate downstream NF-κB and MAPK signaling pathways. This compound significantly enhances immune cell activation in murine models, promoting the proliferation of CD4+ T and CD8+ T cells, leading to direct tumor cell lysis and inhibition of tumor growth. SMU-L11 is a valuable reagent for cancer research and can also be utilized for investigations into immune system-related diseases.
  24. BACH1 Inhibitor

    ASP-8731 is a potent BACH1 inhibitor that enhances NRF2-mediated gene transcription, thereby activating antioxidant and anti-inflammatory pathways. This compound significantly upregulates the expression of key genes such as HMOX1 and FTH1, and increases fetal hemoglobin (HbF) levels, promoting F-cell production in hydroxyurea-unresponsive cells. Additionally, ASP-8731 mitigates inflammatory responses by downregulating VCAM1, ICAM-1, and NF-κB (p65) phosphorylation. Its ability to relieve glutathione depletion and microcirculatory stasis suggests potential applications in the treatment of sickle cell disease and other hematological disorders.
  25. Stable Isotope

    Oxaprozin-d5 is a deuterium-labeled derivative of Oxaprozin, a nonsteroidal anti-inflammatory drug (NSAID) that functions as a dual inhibitor of cyclooxygenase enzymes COX-1 and COX-2, exhibiting IC50 values of 2.2 μM and 36 μM, respectively, for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2. Additionally, Oxaprozin is known to inhibit the activation of NF-κB. This stable isotope can be utilized in pharmacokinetic studies and metabolic research, enhancing the understanding of Oxaprozin's biological pathways and mechanisms of action.
  26. Stable Isotope

    Guaiacol-d4-1 is a deuterated form of guaiacol that serves as a stable isotope. This phenolic compound is known to inhibit lipopolysaccharide (LPS)-induced cyclooxygenase-2 (COX-2) expression and activation of nuclear factor kappa B (NF-κB), demonstrating significant anti-inflammatory activity. It is widely used in research applications focused on inflammation and signaling pathways in various biological systems.
  27. COX-2 Inhibitor

    COX-2-IN-51 is a selective COX-2 inhibitor exhibiting an IC50 of 70.7 nM. It effectively reduces LPS-induced release of nitric oxide (NO) and prostaglandin E2 (PGE2), as well as the expression of COX-2 and inducible nitric oxide synthase (iNOS), and inhibits the NF-κB signaling pathway. This compound demonstrates anti-inflammatory and analgesic properties in various murine models by targeting the NF-κB cascade, while presenting a lower risk of gastrointestinal side effects compared to traditional nonsteroidal anti-inflammatory drugs.
  28. Active Compound

    threo-Guaiacylglycerol β-coniferyl ether is an active compound derived from the 95% ethanol extract of Lepisorus contortus, a member of the Polypodiaceae family. Although its inhibitory activity against key targets such as NF-κB, nitric oxide production, aromatase, quinone reductase 2, and cyclooxygenase (COX-1/-2) is not pronounced, it serves as a valuable research tool for exploring biochemical pathways. Investigators can utilize this compound in studies focusing on plant-derived metabolites and their potential applications in pharmacology and biochemistry.
  29. Stable Isotope

    Guaiacol-d7 is a deuterated form of Guaiacol, a phenolic compound known for its ability to inhibit LPS-stimulated COX-2 expression and NF-κB activation. This stable isotope serves as a useful tracer in various pharmacological studies, particularly in the investigation of anti-inflammatory mechanisms. Guaiacol-d7 can be employed in metabolic studies and drug metabolism research, enhancing the understanding of inflammatory pathways and therapeutic interventions.
  30. COX-2/15-LOX Inhibitor

    COX-2/15-LOX-IN-5 is a potent dual inhibitor of cyclooxygenase-2 (COX-2) and 15-lipoxygenase (15-LOX). This compound effectively attenuates lipopolysaccharide-induced NF-κB activation in RAW 264.7 macrophages, highlighting its role in modulating inflammatory responses. COX-2/15-LOX-IN-5 exhibits significant anti-inflammatory and antioxidant properties, making it a valuable tool for research into inflammatory diseases and other related biological processes.
  31. BPD

    COX-2/TAK1-NF-κB Inhibitor

    BPD is a selective inhibitor of COX-2 and TAK1-NF-κB, exhibiting an IC50 of 18.5 μM for COX-2. This compound effectively reduces the transcriptional expression of key pro-inflammatory cytokines, including iNOS, TNF-α, IL-6, and IL-1β, thereby demonstrating notable anti-inflammatory properties. BPD has been shown to inhibit carrageenan-induced paw edema and mitigate LPS-induced septic mortality, making it a valuable tool for research in inflammation and related pathways.
  32. Stable Isotope

    Guaiacol-13C6 is a stable isotope-labeled derivative of Guaiacol, a phenolic compound known for its anti-inflammatory properties. By inhibiting lipopolysaccharide (LPS)-stimulated cyclooxygenase-2 (COX-2) expression and nuclear factor kappa B (NF-κB) activation, Guaiacol-13C6 serves as a valuable tool in the study of inflammatory pathways. Its unique isotopic labeling facilitates advanced metabolic tracing and tracking in various biological research applications.
  33. Stable Isotope

    Guaiacol-d4 is a deuterium-labeled derivative of guaiacol, a phenolic compound recognized for its role in modulating inflammatory pathways. It inhibits lipopolysaccharide (LPS)-stimulated cyclooxygenase-2 (COX-2) expression and the activation of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB). This compound is valuable for research in inflammation, offering insights into anti-inflammatory mechanisms and potential therapeutic applications.
  34. Anti-inflammatory Agent

    MBL-1 is an orally active anti-inflammatory agent that targets the hCOX-2 protein, demonstrating an IC50 of 5.77 μM. This compound effectively reduces the production of key pro-inflammatory mediators, including nitrogen oxide (NO), reactive oxygen species (ROS), IL-1β, and IL-18, by inhibiting the MAPK/NF-κB and NLRP3 signaling pathways. MBL-1 has shown protective effects against dextran sulfate sodium (DSS)-induced colitis, making it a valuable tool for research into ulcerative colitis and related inflammatory conditions.
  35. NF-κB/COX Inhibitor

    Methoxycoronarin D is a potent inhibitor of NF-κB, demonstrating an IC50 value of 7.3 μM. Additionally, it selectively inhibits cyclooxygenase-1 (COX-1), with an IC50 value of 0.9 μM. This compound is relevant for research applications focused on inflammation and cancer due to its ability to modulate critical signaling pathways.
  36. COX-2 Inhibitor

    Cavidine is a selective COX-2 inhibitor that exhibits potent anti-inflammatory properties. It is particularly useful in research concerning skin injuries, hepatitis, cholecystitis, and scabies. Additionally, Cavidine has been shown to alleviate LPS-induced acute lung injury through modulation of the NF-κB signaling pathway, making it a valuable compound for studying inflammation-related conditions.
  37. Dissociative Steroid

    Vamorolone is a novel dissociative steroid that functions as an anti-inflammatory agent and membrane stabilizer. This compound demonstrates potent inhibition of NF-κB signaling, effectively mitigating inflammation while minimizing hormonal side effects. Vamorolone is particularly relevant for research into muscular dystrophy, showcasing its potential to improve muscle function and health without the adverse effects commonly associated with traditional steroid therapies.
  38. Cyclic dinucleotides

    cAIMP (Cyclic Adenosine-Inosine Monophosphate) functions as a synthetic cyclic dinucleotide that activates immune response pathways by engaging IRF and NF-κB in the THP1 human monocyte reporter cell line (THP1-Dual). This compound is capable of inducing the secretion of interferons and pro-inflammatory cytokines in vitro in human blood, demonstrating an EC50 of 6.4 μmol/L. cAIMP serves as a valuable tool for research focused on innate immune signaling and inflammation responses.
  39. HDAC6 Degrader

    HDAC6 degrader-5 functions as an HDAC6 degrader, demonstrating potent inhibitory and degradation capabilities with an IC50 of 4.95 nM and a DC50 of 0.96 nM. This compound effectively inhibits the release of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6, while also preventing hepatocyte apoptosis. Additionally, HDAC6 degrader-5 shows anti-inflammatory effects in mouse models of acetaminophen-induced liver injury, making it a valuable tool for research on inflammatory diseases and liver pathologies.
  40. HDAC3 Degrader

    HDAC3 Degrader-2 is a selective degrader of histone deacetylase 3 (HDAC3), functioning through targeted degradation to inhibit the activation of the NLRP3 inflammasome. By facilitating the reduction of IL-1β maturation and caspase-1 activity, HDAC3 Degrader-2 demonstrates significant anti-inflammatory effects. This reagent is applicable in researching conditions such as endotoxin shock, colitis, and gouty arthritis, providing valuable insights into mechanisms of inflammation and therapeutic interventions.
  41. Sphingomyelinase Inhibitor, K-Ras Inhibitor, H-Ras Inhibitor, NF-κB Inhibitor

    Avicin G is a potent inhibitor of sphingomyelinases, specifically targeting neutral sphingomyelinases (SMPD2/3) and acid sphingomyelinase (SMPD1). This compound elevates intracellular sphingomyelin levels and modulates the distribution of sphingomyelin, disrupting signal transduction pathways in oncogenic K-Ras and H-Ras. Avicin G exhibits significant biological activity, including the reduction of ERK and Akt phosphorylation and alterations in lysosomal pH. Its applications extend to research on pancreatic ductal adenocarcinoma and non-small cell lung cancer.
  42. AP-1/NF-κB Activation Inhibitor

    SPC 839 is an orally active inhibitor that targets AP-1 and NF-κB mediated transcriptional activation, demonstrating an IC50 of 0.008 μM. This compound is essential for studying pathways associated with inflammation, cancer progression, and cellular stress responses. Its potent inhibition of key transcription factors makes it a valuable tool for researchers investigating the role of AP-1 and NF-κB in various biological processes.
  43. NF-κB Inhibitor

    Ganoderic acid H is a lanostane-type triterpene that functions as an NF-κB inhibitor. It effectively suppresses the growth and invasive behavior of breast cancer cells by inhibiting the activity of transcription factors AP-1 and NF-κB. This compound holds potential for research applications in cancer biology, particularly for studies focusing on the modulation of signaling pathways involved in tumor progression and metastasis.
  44. NF-κB/AP-1 Inhibitor

    Glucocorticoid receptor modulator 1 is a selective non-steroidal modulator that targets the glucocorticoid receptor, exhibiting potent inhibition of NF-κB and AP-1 with IC50 values of 9 nM and 130 nM, respectively. This compound effectively reduces the expression of key inflammatory cytokines, including IL-6, IL-1β, and TNF-α. Additionally, it demonstrates potential in alleviating dermatitis in preclinical models, making it a valuable tool for research in inflammation and immune response.
  45. Glucocorticoid Receptor Modulator

    BMS-791826 is a selective glucocorticoid receptor modulator that targets glucocorticoid receptors to exert its biological effects. This compound effectively inhibits AP-1 and NF-κB-dependent signaling pathways, making it a valuable tool for studying the mechanisms underlying inflammatory diseases. Research applications include the exploration of potential therapeutic strategies for conditions associated with dysregulated glucocorticoid receptor activity.
  46. VDR Agonist

    20-Hydroxyvitamin D3 serves as a VDR agonist, modulating immune responses without inducing calcemia. By binding to the vitamin D receptor (VDR), it activates VDR and aryl hydrocarbon receptor (AhR) signaling pathways, enhances CYP24A1 expression, and promotes VDR nuclear translocation. This compound inhibits NF-κB activity through IκBα upregulation, demonstrating anti-proliferative effects in cancer cells by reducing cell proliferation, colony formation, migration, and tumor growth while inducing differentiation. 20-Hydroxyvitamin D3 is a valuable tool for investigating inflammatory and autoimmune diseases, as well as various cancers, including melanoma and hepatocarcinoma.
  47. COX Inhibitor

    Inulicin (1-O-Acetylbritannilactone) is a potent inhibitor of cyclooxygenase (COX) enzymes, specifically targeting COX-2 activity. This compound demonstrates significant biological activity by inhibiting lipopolysaccharide (LPS)-induced production of prostaglandin E2 (PGE2) as well as the expression of COX-2. Additionally, Inulicin suppresses NF-κB activation and its translocation, making it valuable for research applications related to inflammation and cancer.
  48. Stable Isotope

    Guaiacol-d3 is a deuterated form of guaiacol, a phenolic compound known for its ability to inhibit lipopolysaccharide (LPS)-induced cyclooxygenase-2 (COX-2) expression and nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) activation. This reagent exhibits significant anti-inflammatory properties and is employed in research applications studying inflammatory pathways and the modulation of COX-2 expression. Its stable isotope labeling facilitates tracing studies and enhances the understanding of metabolic processes in biological systems.
  49. Anti-Inflammatory Agent

    Phenyl β-D-glucopyranoside is an anti-inflammatory agent derived from Phellodendron amurense. It exerts its biological activity by inhibiting nitric oxide (NO) production, along with the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Additionally, Phenyl β-D-glucopyranoside prevents the nuclear translocation of nuclear factor kappa B (NF-κB), leading to the reduced expression of pro-inflammatory cytokines and associated genes. This compound is valuable for researchers studying inflammation and related signaling pathways.
  50. P2Y12 Receptor Activator

    ADP-β-S trilithium is the trilithium salt form of ADP-β-S, serving as a potent activator of the P2Y12 receptor. It facilitates the upregulation of IL-1β and IL-6 production in microglial cells, promotes NF-κB phosphorylation and nuclear translocation, and enhances NLRP3 inflammasome activation. This reagent is valuable for research into inflammatory responses and signaling pathways involving P2Y12 receptor activation.

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