JAK/Stat

Items 901-950 of 1031

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  1. CK2/PIM1 Inhibitor

    CK2/PIM1-IN-1 is a selective inhibitor targeting casein kinase 2 (CK2) and PIM1, demonstrating IC50 values of 3.787 μM and 4.327 μM, respectively. This compound is designed for research into proliferative disorders, particularly cancer, and has potential applications in studying kinase-related conditions such as inflammation, pain, vascular disorders, pathogenic infections, and certain immunological disorders.
  2. STAT6 Inhibitor

    STAT6-IN-7 is a potent inhibitor of STAT6, effectively disrupting the binding of human STAT6 to phosphorylated IL-4 receptor alpha (pIL-4Rα) with an IC50 value of 0.28 μM. Its mechanism of action makes it a valuable tool in the study of inflammatory and allergic diseases, aiding researchers in elucidating the role of STAT6 in these pathological conditions.
  3. STAT6 Inhibitor

    STAT6-IN-9 is a selective inhibitor of Signal Transducer and Activator of Transcription 6 (STAT6), demonstrating an EC50 value of 4 nM. This compound effectively interferes with STAT6 activation driven by the IL-13-IL-13 receptor/IL-4 receptor signaling pathway. Additionally, STAT6-IN-9 inhibits CCL17 secretion with an IC50 of 4.6 nM. It is a valuable tool for investigating chronic inflammatory diseases associated with STAT6 dysregulation, including allergies, asthma, and chronic obstructive pulmonary disease.
  4. STAT6 PROTAC Degrader

    PROTAC STAT6 degrader-1 is a targeted protein degradative compound designed to modulate STAT6 activity through the recruitment of E3 ligase CRBN. With a DC50 of less than 1 nM, this PROTAC showcases potent efficacy in STAT6 degradation. It is particularly relevant for research on inflammation and various cancer types, providing a valuable tool for exploring STAT6's role in pathophysiology and therapeutic responses.
  5. STAT6 Inhibitor

    STAT6-IN-10 is a potent inhibitor of signal transducer and activator of transcription 6 (STAT6), exhibiting an EC50 of 0.002 μM. This compound effectively inhibits the secretion of CCL17 in peripheral human whole blood with an IC50 of 0.095 μM, making it a valuable tool for studying inflammatory responses. STAT6-IN-10 is applicable in research focused on dermatological and respiratory conditions, providing insights into therapeutic interventions targeting these pathways.
  6. STAT3 Degrader

    KT-333 is a selective STAT3 degrader that induces the degradation of the STAT3 protein via the ubiquitin-proteasome pathway. This compound binds to STAT3 and the E3 ubiquitin ligase von Hippel-Lindau (VHL), facilitating targeted protein degradation. KT-333 has demonstrated significant antitumor activity and is particularly relevant for research in hematologic malignancies, including large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL).
  7. STAT6 Inhibitor

    STAT6-IN-3 is a potent STAT6 inhibitor designed to selectively target the SH2 domain of STAT6, exhibiting a high binding affinity with an IC50 value of 0.04 μM. This compound is valuable in studying inflammatory processes, particularly in disorders such as asthma, by providing insights into the modulation of STAT6 signaling pathways. Researchers can utilize STAT6-IN-3 to explore its effects on cytokine signaling and immune response regulation.
  8. STAT3 Inhibitor

    SI-109 is a potent inhibitor of the STAT3 SH2 domain, demonstrating an inhibitory constant (Ki) of 9 nM. This compound effectively reduces the transcriptional activity of STAT3 with an IC50 value of 3 μM. SI-109 is utilized in research applications involving antitumor activity and has been instrumental in the development of PROTAC STAT3 degrader SD-36, an important tool in targeted protein degradation studies.
  9. STAT3 Agonist

    ML115 is a selective agonist of the signal transducer and activator of transcription 3 (STAT3) with an EC50 of 2 nM. It enhances the expression of BCL3, a STAT3-dependent oncogene, while demonstrating inactivity towards related targets such as STAT1, STAT5, and NF-κB. ML115 has been shown to counterbalance the effects of Ginsenoside Rc on cell viability and inflammatory responses in LPS-stimulated H9c2 and RAW264.7 cells, impacting oxidative stress markers. This compound is valuable for investigating mechanisms in breast and prostate cancer research.
  10. STAT6 Inhibitor

    YM-341619 is a potent STAT6 inhibitor with an IC50 of 0.70 nM, demonstrating effective modulation of Th2 cell differentiation in mouse spleen T cells induced by IL-4, with an IC50 of 0.28 nM. This compound selectively inhibits Th2 differentiation without impacting Th1 cells, making it a valuable tool for research into allergic diseases, including allergic asthma. Its oral bioavailability enhances its utility in in vivo studies aimed at understanding the role of STAT6 signaling in immune responses.
  11. STAT6 Inhibitor

    STAT6-IN-1 is a potent STAT6 inhibitor that specifically targets the SH2 domain of STAT6 with an IC50 value of 0.028 µM. This compound demonstrates significant biological activity in the modulation of signaling pathways associated with allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease, and various cancer types. STAT6-IN-1 is a valuable tool in research applications focused on elucidating the role of STAT6 in inflammatory and oncogenic processes.
  12. STAT6 Inhibitor

    AS1810722 is a potent inhibitor of STAT6, exhibiting an IC50 of 1.9 nM. This compound possesses a favorable profile regarding CYP3A4 inhibition. As a derivative of fused bicyclic pyrimidine, AS1810722 is poised for research applications in allergic diseases, including asthma and atopic disorders.
  13. STAT6 Inhibitor

    STAT6-IN-4 is a selective inhibitor of Signal Transducer and Activator of Transcription 6 (STAT6), exhibiting an IC50 value of 0.34 μM. This compound has significant potential in the study of inflammatory and allergic conditions, providing researchers the ability to investigate the roles of STAT6 in disease pathogenesis and therapeutic responses. Its application can aid in elucidating the molecular mechanisms underlying STAT6-mediated pathways.
  14. STAT6 Inhibitor

    STAT6-IN-5 is a selective inhibitor of STAT6, demonstrating an IC50 value of 0.24 μM. This compound is primarily utilized in the investigation of inflammatory and allergic diseases, such as atopic dermatitis. Its efficacy in modulating STAT6 activity makes it a valuable tool for exploring therapeutic strategies in related biological pathways.
  15. STAT6 Inhibitor

    STAT6-IN-2 is a selective inhibitor of STAT6, effectively blocking the tyrosine phosphorylation of this transcription factor. By inhibiting STAT6, it reduces the secretion of eotaxin-3, which is pivotal in the inflammatory response. This reagent is particularly valuable for research into immune diseases and allergic inflammatory conditions, including asthma, providing insights into the underlying mechanisms and potential therapeutic targets.
  16. STAT6 Inhibitor

    PM-43I is a potent inhibitor of Signal Transducer and Activator of Transcription 6 (STAT6), effectively reducing its phosphorylation levels. This compound demonstrates significant biological activity in the modulation of immune responses and inflammatory pathways. PM-43I is applicable in research related to allergic lung diseases, allergic rhinitis, chronic obstructive pulmonary disease (COPD), and cancer, making it a valuable tool for investigating STAT6-mediated mechanisms.
  17. STAT3 Inhibitor

    LLL12 is a potent inhibitor of STAT3, specifically targeting its phosphorylation. By interfering with the STAT3 signaling pathway, LLL12 demonstrates significant anti-tumor activity, particularly enhancing the effects of Cisplatin and Paclitaxel on ovarian cancer cell proliferation, migration, and growth. This compound is valuable for research in cancer biology and therapeutic development, especially in exploring combinatorial treatment strategies.
  18. STAT5a Inhibitor

    Stafia-1 is a selective inhibitor of STAT5a, exhibiting a Ki of 10.9 μM and an IC50 of 22.2 μM. It demonstrates significant selectivity for STAT5a over STAT5b and other members of the STAT family. This compound is valuable for research investigating the role of STAT5a in cellular signaling pathways and its implications in various diseases, including cancer and inflammation.
  19. STAT3 Dimerization Inhibitor

    STX-0119 is a selective inhibitor of STAT3 dimerization, targeting the STAT3 signaling pathway. By inhibiting STAT3 transcription with an IC50 of 74 μM, STX-0119 effectively disrupts the aberrant activation of STAT3, which is implicated in various cancers and inflammatory diseases. This compound is valuable for research applications focused on understanding the role of STAT3 in tumorigenesis and potential therapeutic interventions.
  20. STAT6 Ligand

    AK-068 is a high-affinity ligand for STAT6, exhibiting a binding affinity with a Ki of 6 nM. It shows remarkable selectivity, with over 150-fold preference for STAT6 compared to STAT5A and over 85-fold against STAT5B. This compound serves as a beneficial building block for the synthesis of PROTACs, allowing for targeted protein degradation research applications and potential therapeutic development.
  21. STAT3 Inhibitor

    STAT3-IN-25 is a selective inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). It exhibits significant inhibition of STAT3 luciferase activity in HEK293T cells, displaying an IC50 of 22.3 nM, and inhibits ATP production in BxPC-3 pancreatic cancer cells with an IC50 of 32.5 nM. This compound shows potential for use in research focused on pancreatic cancer and other conditions linked to aberrant STAT3 signaling.
  22. STAT5b SH2 Inhibitor

    Stafib-1 is a selective inhibitor of the STAT5b SH2 domain, exhibiting a Ki value of 44 nM and an IC50 of 154 nM. It effectively disrupts STAT5b signaling, which plays a crucial role in various cellular processes, including proliferation and apoptosis. Stafib-1 is valuable for research applications aimed at understanding oncogenic signaling pathways and exploring potential therapeutic strategies for STAT5b-driven malignancies.
  23. STAT3 Antagonist

    5,15-Diphenylporphyrin acts as a STAT3 antagonist by binding specifically to the SH2 domain of the STAT3 protein. This interaction disrupts the pTyr-SH2 binding, consequently inhibiting STAT3 dimerization, nuclear translocation, and DNA binding activity. As a result, 5,15-Diphenylporphyrin reduces the expression of genes associated with cancer cell proliferation and survival. This compound is valuable for research in the development of novel anticancer therapies.
  24. STAT5b Inhibitor

    Stafib-2 is a selective inhibitor of the transcription factor STAT5b, demonstrating an IC50 of 82 nM specifically for STAT5b and 1.7 μM for STAT5a. This compound is critical for studies exploring the role of STAT5b in various biological processes, including cell proliferation and survival. Although Stafib-2 exhibits limited cell permeability, it remains a valuable tool for researchers investigating signaling pathways associated with STAT5b in cancer and other diseases.
  25. STAT3 Inhibitor

    5-FAM-GpYLPQTV-NH2 is a fluorescently labeled peptide that inhibits the signal transducer and activator of transcription 3 (STAT3). This compound exhibits significant biological activity as a STAT3 inhibitor, making it a valuable tool for cancer research. Its fluorescent properties enable easy tracking in various biological assays, facilitating the study of STAT3-mediated pathways in tumor biology.
  26. STAT5 Inhibitor

    HODHBt is a STAT5 inhibitor that disrupts the interaction between STAT5 and SUMO, thereby preventing the SUMOylation of phosphorylated STAT5. This action enhances IL-15 signaling, which significantly improves the cytotoxicity and functionality of natural killer (NK) cells, as well as promotes the generation of cytokine-induced memory-like (CIML) NK cells. HODHBt is valuable for research into HIV infection and cancer therapies.
  27. STAT6 Inhibitor

    PM-81I is a potent inhibitor of STAT6, targeting its SH2 structural domain to effectively reduce STAT6 phosphorylation levels. This compound serves as a valuable tool in research related to allergic lung diseases, allergic rhinitis, chronic obstructive pulmonary disease, and various cancer studies. Its ability to modulate STAT6 activity makes it relevant for elucidating the molecular mechanisms underlying these conditions.
  28. STAT3 PROTAC Degrader

    SD-436 is a selective and potent degrader of STAT3, functioning through the PROTAC mechanism with a DC50 of 0.5 μM and an IC50 of 19 nM for STAT3. It promotes the ubiquitination and subsequent degradation of STAT3, leading to significant tumor regression. This reagent is applicable in cancer research, including studies focused on leukemia and lymphoma.
  29. ERK2/STAT3 Activator

    Fulipiftide is a short peptide that acts as an activator of the ERK2 and STAT3 signaling pathways. This compound promotes the expansion of nuclear stem cell factor +TSPC, demonstrating significant anti-inflammatory activity. Fulipiftide is particularly useful in research related to acute tendon injury and in studies exploring regenerative medicine and tissue repair mechanisms.
  30. STAT3 Inhibitor

    STAT3-IN-17 is a selective inhibitor of the signal transducer and activator of transcription 3 (STAT3), exhibiting an IC50 of 0.7 μM in HEK-Blue IL-6 assays. This compound demonstrates antiproliferative effects in HeLa cancer cell lines, making it valuable for oncology research. Additionally, STAT3-IN-17 inhibits pyruvate-ferredoxin oxidoreductase (PFOR) and has shown efficacy against Helicobacter pylori, further expanding its potential applications in microbiological studies.
  31. STAT3 Inhibitor

    MM-206 is a potent inhibitor of the STAT3 SH2 domain-phosphopeptide interaction, with an IC50 of 1.2 μM. This compound induces apoptosis in a dose-dependent manner in acute myeloid leukemia (AML) cell lines. MM-206 is valuable for research applications focused on understanding the role of STAT3 in cancer biology and exploring potential therapeutic strategies targeting this pathway.
  32. STAT3 Inhibitor

    STAT3-IN-20 is a selective inhibitor of the STAT3 protein, exhibiting an IC50 value of 0.65 μM. By binding to the SH2 domain, this compound effectively inhibits STAT3 phosphorylation, translocation, and subsequent downstream gene transcription. Demonstrating significant antiproliferative activity, STAT3-IN-20 shows IC50 values of 2.97 μM against STAT3-overactivated DU145 cells and 3.26 μM against MDA-MB-231 cancer cells. Furthermore, STAT3-IN-20 induces cell cycle arrest and apoptosis, making it a valuable tool for research in cancer therapeutics targeting the STAT3 signaling pathway.
  33. STAT3 Inhibitor

    STAT3-IN-14 is a selective inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3), demonstrating potent inhibitory activity against STAT3 phosphorylation. By binding directly to the hinge region of STAT3, this compound effectively disrupts its activity, making it a valuable tool for research applications targeting STAT3-mediated signaling pathways. It is useful in studies of cancer, inflammation, and autoimmune diseases where STAT3 plays a critical role in disease progression.
  34. STAT6 degrader

    STAT6 degrader-3 is a highly potent and selective degrader of the signal transducer and activator of transcription 6 (STAT6), exhibiting a DC50 of <1 nM. This compound facilitates the targeted degradation of STAT6, making it instrumental in investigating Type 2 immune responses and associated allergic mechanisms in various biological contexts. Its precise action allows for in-depth studies into the modulation of immune pathways linked to inflammatory diseases.
  35. CXCR4/STAT3 Inhibitor

    Minecoside is a potent inhibitor of the CXCR4 receptor and STAT3 signaling pathway. It demonstrates significant anticancer and anti-inflammatory activities by downregulating CXCR4 expression and suppressing STAT3 activation, which leads to the inhibition of CXCL12-induced cellular invasion. Minecoside has been shown to effectively hinder cancer metastasis and enhance apoptosis, making it a valuable tool for research in cancer biology and therapeutic development.
  36. STAT3 inhibitor

    (+)-Ochromycinone is a natural antibiotic that serves as a potent inhibitor of STAT3. Its primary biological activity is the modulation of signaling pathways involved in cancer progression and inflammatory responses. This compound is widely utilized in research applications focusing on cancer biology and dermatological diseases such as psoriasis.
  37. STAT3 Inhibitor

    Galiellalactone is a selective inhibitor of STAT3 signaling, exhibiting an IC50 value of 250-500 nM. This small, non-toxic, and non-mutagenic fungal metabolite is relevant for research involving castration-resistant prostate cancer, providing insights into the mechanisms of cancer biology and therapeutic resistance. Its specificity towards STAT3 makes it a valuable tool for studying the role of this pathway in various cellular processes.
  38. STAT3 Inhibitor

    MC0704 is a selective STAT3 inhibitor with an IC50 of 2.13 μM. This compound effectively induces apoptosis and triggers cell cycle arrest, demonstrating significant antitumor activity in murine models of breast cancer. MC0704 is a valuable tool for investigating therapeutic strategies in metastatic triple-negative breast cancer (mTNBC) research.
  39. STAT3 Inhibitor

    STAT3-IN-24 is a cell-permeable inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3). This peptide inhibitor effectively disrupts the recruitment of STAT3 to Janus Kinase 2 (Jak2) and inhibits the phosphorylation of tyrosine 705, thereby preventing STAT3 dimerization and its subsequent nuclear translocation. STAT3-IN-24 is applicable in studies investigating the oncogenic role of STAT3 and its potential as a therapeutic target in various malignancies.
  40. STAT Inhibitor

    JI069 is a selective JAK-STAT inhibitor that effectively targets the STAT signaling pathway. It demonstrates potent inhibition of STAT3, as well as other STAT proteins including STAT1, STAT5, and STAT6, thereby suppressing Th1, Th2, and Th17 differentiation while promoting iTreg differentiation. Due to its ability to inhibit cytokine production from T cells and decrease STAT3 phosphorylation in synovial cells, JI069 exhibits significant therapeutic potential in models of collagen-induced arthritis.
  41. STAT3 Inhibitor

    Eucannabinolide is a STAT3 inhibitor that targets the activation of STAT3 at tyrosine 705, inhibiting its translocation to the nucleus and reducing its DNA binding capacity. This compound demonstrates potential in studies related to triple-negative breast cancer (TNBC) and other diseases characterized by aberrant STAT3 signaling. Eucannabinolide serves as a valuable tool for researchers investigating therapeutic strategies aimed at modulating STAT3 pathways in oncogenesis.
  42. STAT3 Inhibitor

    STAT3-IN-37 is a selective inhibitor of the transcription factor STAT3, exhibiting potent inhibitory activity with an IC50 of 15 nM in a DNA-HTRF assay and 2 nM in a human whole blood assay utilizing SOCS3 qPCR. This compound is valuable for research applications targeting STAT3-mediated signaling pathways, often implicated in oncogenesis and immune regulation. Its efficacy makes it a suitable tool for studies investigating the therapeutic potential of STAT3 modulation in cancer and inflammatory diseases.
  43. Hsp110-STAT3 Interaction Inhibitor

    Hsp110-STAT3 PPI-IN-1 is a potent inhibitor of the Hsp110-STAT3 protein-protein interaction. This compound exhibits antiproliferative activity against the HPAEC cell line, demonstrating an IC50 value of 22.67 μM. It serves as a valuable tool for investigating the role of Hsp110-STAT3 interactions in various biological processes and therapeutic applications.
  44. STAT3 Inhibitor

    S3I-1757 is a selective STAT3 inhibitor that effectively hinders the phosphorylation and dimerization of STAT3 proteins. By targeting this pathway, S3I-1757 demonstrates significant potential in the study of STAT3-driven malignancies, including melanoma. Its application is particularly relevant for investigating therapeutic strategies in cancers characterized by aberrant STAT3 activation.
  45. STAT3 Inhibitor

    Ac-GpYLPQTV-NH2 is a selective inhibitor of the STAT3 signaling pathway, exhibiting an IC50 value of 0.33 μM. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology and therapeutic applications targeting STAT3-mediated oncogenic functions. Its efficacy in modulating STAT3 activity provides insights into the role of this transcription factor in tumor progression and treatment resistance.
  46. STAT5a Inhibitor

    Stafia-1-dipivaloyloxymethyl ester functions as a selective inhibitor of STAT5a. This compound effectively reduces the expression of phosphorylated STAT5a (pSTAT5a) in a concentration-dependent manner, demonstrating significant inhibition at doses ranging from 0-200 μM, while exhibiting minimal impact on phosphorylated STAT5b (pSTAT5b). Stafia-1-dipivaloyloxymethyl ester is valuable for research applications targeting STAT signaling pathways.
  47. STAT Inhibitor

    Eupalinolide K is a selective STAT3 inhibitor derived from Eupatorium lindleyanum. This sesquiterpene lactone functions as a Michael reaction acceptor, demonstrating significant potential in modulating STAT3 signaling pathways. Its inhibitory activity makes Eupalinolide K useful in research related to cancer biology and inflammatory responses, providing insights into therapeutic strategies targeting the STAT3 pathway.
  48. STAT6 PROTAC Degrader

    PROTAC STAT6 degrader-3 is a highly potent degrader targeting STAT6, exhibiting a DC50 of less than 1 nM. This compound facilitates the targeted degradation of STAT6, making it a valuable tool for investigating allergic and inflammatory diseases as well as various cancers. Its application in research can provide insights into the role of STAT6 in disease pathways and therapeutic interventions.
  49. STAT3 Degrader

    KT-333 ammonium is a selective STAT3 degrader that initiates the proteolytic degradation of the STAT3 protein via the ubiquitin-proteasome pathway. By binding to both STAT3 and the E3 ubiquitin ligase von Hippel-Lindau (VHL), KT-333 ammonium effectively targets and eliminates STAT3, exhibiting significant antitumor activity. This compound is particularly useful in the study of hematologic malignancies, including large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL).
  50. STAT3 Inhibitor

    STAT3-IN-7 is a potent inhibitor targeting Signal Transducer and Activator of Transcription 3 (STAT3). This aryl sulfonamido azetidine compound demonstrates significant anticancer properties, making it a valuable tool for research in cancer biology. It offers applications in studies aimed at elucidating the role of STAT3 signaling in tumor progression and therapeutic resistance.

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