JAK

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  1. JAK3 Inhibitor

    JANEX-1 hydrochloride is a selective inhibitor of Janus kinase 3 (JAK3), exhibiting a Ki value of 2.3 μM and an IC50 of 78 μM for JAK3 inhibition. This compound does not inhibit JAK1 or JAK2, making it a valuable tool for studying JAK3-specific signaling pathways. JANEX-1 hydrochloride is suitable for research applications focused on immune responses and hematological disorders where JAK3 plays a critical role.
  2. JAK1 Inhibitor

    JAK1-IN-20 is a selective inhibitor of Janus kinase 1 (JAK1) with an IC50 of less than 0.5 nM, demonstrating potent inhibition of its enzymatic activity. By reducing the production of proinflammatory cytokines such as TNF-α and IL-6, JAK1-IN-20 effectively suppresses the phosphorylation of STAT3. This compound shows promise in ameliorating ulcerative colitis and serves as a valuable tool in the research of inflammatory bowel disease.
  3. CDK2/JAK2/FLT3 Inhibitor

    Zotiraciclib hydrochloride is a novel small molecule inhibitor targeting cyclin-dependent kinase 2 (CDK2), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase 3 (FLT3). This reagent demonstrates anti-tumor activity by downregulating the Myc oncogene through CDK9 inhibition, contributing to reduced tumor growth. Zotiraciclib hydrochloride is particularly relevant for research into cancers capable of crossing the blood-brain barrier, and elevated levels of the MCL-1 protein may indicate its potential as a prognostic marker and therapeutic target in cancer studies.
  4. JAK2/STAT3 Pathway Inhibitor

    WP1193 is a potent inhibitor of the JAK2/STAT3 signaling pathway. It effectively suppresses the phosphorylation of both JAK2 and STAT3, leading to a decrease in the expression of key stem cell markers such as CD133 and c-myc. This compound is valuable for research into glioblastoma and other cancers associated with aberrant activation of the JAK2/STAT3 pathway.
  5. JAK1/JAK2 Inhibitor

    Momelotinib dihydrochloride is a selective JAK1/JAK2 inhibitor that also targets ACVR1, resulting in decreased Hepcidin expression which enhances iron availability for erythropoiesis. This compound has demonstrated efficacy in reducing transfusion dependency and alleviating splenomegaly associated with myelofibrosis. Its unique mechanism and biological activity make Momelotinib dihydrochloride a valuable tool for research in myelofibrosis and related hematological conditions.
  6. JAK3 Inhibitor

    Thi-DPPY is a potent and orally active inhibitor of JAK3, exhibiting IC50 values of 62.4 nM for BTK and 1.38 nM for JAK. This compound demonstrates significant anti-proliferative effects on human bronchial epithelial (HBE) cells and possesses anti-inflammatory properties in vivo. Thi-DPPY is a valuable tool for investigating potential therapeutic applications in idiopathic pulmonary fibrosis (IPF).
  7. TYK2/JAK1 Inhibitor

    JAK1/TYK2-IN-3 is a selective, orally bioavailable dual inhibitor of TYK2 and JAK1, exhibiting IC50 values of 6 nM and 37 nM, respectively. This compound demonstrates notable selectivity towards JAK2 and JAK3, with IC50 values of 140 nM and 362 nM, respectively. JAK1/TYK2-IN-3 is recognized for its significant anti-inflammatory effects through the modulation of TYK2/JAK1-regulated genes and the differentiation of Th1, Th2, and Th17 cells, making it a valuable tool for research in autoimmune diseases and inflammation.
  8. JAK Inhibitor

    PF-00956980 is a reversible pan-JAK inhibitor that demonstrates inhibitory activity with IC50 values of 2.2 μM for JAK1, 23.1 μM for JAK2, and 59.9 μM for JAK3. This compound is utilized in research focusing on lung and skin inflammatory diseases, providing valuable insights into JAK signaling pathways and their role in inflammatory responses. Its broad inhibitory profile makes it a suitable tool for studying the therapeutic potential of JAK inhibition.
  9. Tyk2 Inhibitor

    Tyk2-IN-20 is a highly potent inhibitor of Tyk2, exhibiting an IC50 of less than 5 nM. Additionally, it demonstrates inhibitory activity against JAK1, JAK2, and JAK3 with IC50 values under 100 nM. This compound is valuable for investigating inflammatory diseases and related signaling pathways, making it a critical tool for research in immunology and therapeutic development.
  10. JAK Inhibitor

    JAK-IN-18 is a potent Janus kinase (JAK) inhibitor that disrupts JAK signaling pathways. This reagent demonstrates significant biological activity in research applications related to various diseases, including ocular, skin, and respiratory disorders. Its ability to modulate JAK activity makes it a valuable tool for studying the underlying mechanisms and potential treatments for these conditions.
  11. JAK Inhibitor

    TK4b is a potent Janus kinase (JAK) inhibitor, exhibiting IC50 values of 19.40 nM for JAK2 and 18.42 nM for JAK3. This compound demonstrates significant anti-proliferative effects and is relevant for research in lymphoid-derived diseases and leukemia. Its selective inhibition of JAK2 and JAK3 makes TK4b a valuable tool for studying the role of JAK signaling pathways in cancer biology.
  12. JAK2 Inhibitor

    JAK2-IN-18 is a selective JAK2 inhibitor that disrupts JAK-STAT signaling pathways with an IC50 of less than 100 nM for pSTAT5 in HEL9217 cells. This reagent effectively inhibits the proliferation of aberrantly proliferating myeloid cells, making it a valuable tool for studying myeloproliferative disorders, such as essential thrombocythemia. Its specificity and potency facilitate research aimed at understanding the molecular mechanisms underlying these conditions.
  13. JAK/STAT Inhibitor

    JAK-STAT-IN-1 is a selective inhibitor of the JAK-STAT signaling pathway. This compound exhibits potent inhibitory activity, making it a valuable tool in the investigation of autoimmune disorders. Its specificity for JAK-STAT modulation facilitates research into the underlying mechanisms of inflammation and immune response regulation.
  14. JAK3 Inhibitor

    JAK3-IN-9 is a selective inhibitor of JAK3, exhibiting an IC50 value of 1.7 nM, making it a potent candidate for the treatment of arthritis. This compound demonstrates low toxicity and high oral bioavailability, contributing to its effectiveness in anti-arthritic applications. JAK3-IN-9 is suitable for use in research focused on autoimmune diseases, particularly those involving JAK3 signaling pathways.
  15. JAK Inhibitor

    Delgocitinib ethanolate is a selective inhibitor of Janus kinases (JAKs), demonstrating IC50 values of 2.8 nM for JAK1, 2.6 nM for JAK2, 13 nM for JAK3, and 58 nM for Tyk2. This compound effectively modulates signaling pathways associated with inflammatory responses and immune regulation. It is primarily used in research applications involving autoimmune diseases and other conditions where JAK signaling is implicated.
  16. JAK3/BTK Inhibitor

    JAK3/BTK-IN-2 is a potent dual inhibitor of Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK). By simultaneously targeting the BTK/JAK3 signaling pathway, this compound demonstrates synergistic effects that may enhance therapeutic outcomes in autoimmune diseases. JAK3/BTK-IN-2 is suitable for research applications focused on JAK3 and BTK-related pathologies, facilitating studies on their roles in immune regulation and disease progression.
  17. JAK Inhibitor

    HAT-SIL-TG-1&AT is a Janus tyrosine kinase (JAK) inhibitor designed to selectively target JAK-STAT signaling pathways in tumor tissues. This hypoxia-activated prodrug exhibits significant antitumor activity by inhibiting cell proliferation in HEL cells and reducing levels of phosphorylated STAT3 and STAT5 under hypoxic conditions. HAT-SIL-TG-1&AT is relevant for researchers investigating the impact of JAK inhibition in cancer therapies and the underlying mechanisms of tumor hypoxia.
  18. JAK2 Inhibitor

    JAK2-IN-1 is a selective JAK2 inhibitor designed to modulate signaling pathways associated with various diseases. This compound demonstrates potential in the treatment of proliferative disorders, inflammatory diseases, and renal pathologies by inhibiting JAK2 activity. It serves as a valuable tool for researchers investigating the role of JAK2 in cellular processes and disease mechanisms.
  19. Multi-kinase Inhibitor

    Debio 0617B is a multi-kinase inhibitor that targets key kinases involved in the regulation of STAT3/STAT5 signaling, including JAK, SRC, ABL, and class III/V receptor tyrosine kinases. This compound effectively reduces the maintenance and self-renewal of primary human acute myeloid leukemia (AML) CD34+ stem/progenitor cells. Additionally, Debio 0617B has demonstrated efficacy in preclinical models of STAT3-driven solid tumors, making it a valuable tool for cancer research and therapeutic development.
  20. JAK3 Inhibitor

    JAK3-IN-11 is a potent, irreversible inhibitor of Janus kinase 3 (JAK3) with an IC50 value of 1.7 nM, demonstrating exceptional selectivity with over 588-fold distinction from other JAK isoforms. This orally active compound covalently binds to the ATP-binding pocket of JAK3, effectively attenuating JAK3-dependent signaling pathways and T cell proliferation. JAK3-IN-11 is a valuable reagent for investigating autoimmune diseases and related immunological research.
  21. JAK Inhibitor

    JAK-IN-31 is a potent JAK inhibitor targeting JAK1, JAK2, JAK3, and Tyk2 with IC50 values of ≤0.01 µM for JAK1, JAK2, and Tyk2, and 0.01-0.1 µM for JAK3. This compound demonstrates significant activity in inhibiting JAK signaling pathways, making it a valuable tool for investigating the role of JAKs in various cancers. JAK-IN-31 is suitable for applications in cancer research, particularly in studies focused on JAK-mediated signaling and its implications in tumor biology.
  22. JAK2/3 Inhibitor

    JAK-2/3-IN-2 is a selective inhibitor of JAK2 and JAK3, exhibiting IC50 values of 23.85 nM and 18.9 nM, respectively. This compound effectively modulates the JAK-STAT signaling pathway, which is critical in hematopoiesis and immune response. JAK-2/3-IN-2 is primarily utilized in research focused on inflammatory diseases, autoimmune disorders, and hematological malignancies.
  23. JAK2 V617F Inhibitor

    JAK2-IN-16 is a selective inhibitor of the JAK2 V617F mutation, a prominent target in the treatment of various hematological malignancies. This compound demonstrates potent inhibitory activity against JAK2, making it a valuable tool for elucidating the role of JAK2 signaling in cancer pathogenesis. Research applications include the investigation of JAK-STAT pathway modulation and potential therapeutic strategies for JAK2-dependent tumors.
  24. JAK1/TYK2 Inhibitor

    JAK1/TYK2-IN-5 is a potent inhibitor of JAK1 and TYK2, exhibiting Ki values of 0.0044 nM for TYK2 JH2 and 0.02 nM for JAK1 JH2, demonstrating high specificity and potency. This compound effectively inhibits interferon-alpha (IFNα) induced activation of the STAT signaling pathway mediated by TYK2 and JAK1. JAK1/TYK2-IN-5 is useful in research applications focused on cytokine signaling, immune response modulation, and the development of therapies targeting autoimmune diseases and inflammatory conditions.
  25. JAK Inhibitor

    JAK-IN-33 is a selective Janus kinase (JAK) inhibitor that effectively modulates JAK signaling pathways. This compound demonstrates potent biological activity in inhibiting cytokine-driven signaling, making it a valuable tool for research in autoimmune diseases and hematological disorders. Its specificity for JAK pathways allows for targeted investigation into JAK-related mechanisms in various cellular contexts.
  26. JAK1 Inhibitor

    JAK1-IN-18 is a selective inhibitor of Janus kinase 1 (JAK1), exhibiting an IC50 of 0.15 nM for JAK1 while demonstrating significantly reduced activity against JAK2 and JAK3. This compound has been shown to effectively diminish inflammation in preclinical models of ulcerative colitis and Crohn's disease. It is suitable for research applications targeting autoimmune diseases, viral infections, and hematological malignancies, making it a valuable tool in the study of these conditions.
  27. JAK2 Inhibitor

    AC-430 is a selective inhibitor of JAK2, targeting the Janus kinase signaling pathway. It demonstrates significant biological activity in modulating cytokine signaling, making it a valuable tool for investigating inflammatory processes. AC-430 is particularly relevant for research applications related to rheumatoid arthritis and other autoimmune diseases.
  28. JAK Inhibitor

    Milpecitinib is a selective Janus tyrosine kinase (JAK) inhibitor that exhibits significant anti-inflammatory activity. This compound has shown promise in the exploration of various cancers and inflammatory disorders. Its ability to modulate JAK signaling pathways makes it a valuable tool for research in pathologies associated with dysregulated immune responses.
  29. JAK1 Inhibitor

    JAK1-IN-12 is a selective inhibitor of Janus kinase 1 (JAK1), exhibiting an IC50 of 0.0246 μM, and demonstrating weaker inhibition of JAK2, JAK3, and TYK2 with IC50 values of 0.423 μM, 0.410 μM, and 1.12 μM, respectively. This compound has been shown to promote hair growth in murine models. JAK1-IN-12 is a valuable tool for investigating immune and inflammatory diseases, providing insights into JAK1-mediated signaling pathways.
  30. Tyk2 Inhibitor

    Tyk2-IN-23 is a selective TYK2 inhibitor with an IC50 of 18 nM, demonstrating over 70-fold selectivity against JAK isoforms 1, 2, and 3. This compound effectively inhibits phosphorylated STAT3 in TYK2-dependent signaling pathways activated by interferon-alpha (IFN-α) and interleukin-10 (IL-10). Additionally, Tyk2-IN-23 significantly reduces IFN-α-induced STAT1 phosphorylation in H9 cells, making it a valuable tool for the investigation of alopecia areata and allergic rhinitis.
  31. PTPN2/1 Dual Inhibitor

    PTPN2/1-IN-4 is a potent dual inhibitor of PTPN1 and PTPN2, exhibiting IC50 values of 12.8 nM and 5.8 nM, respectively. This compound effectively modulates the IFNγ-JAK-STAT signaling pathway, resulting in enhanced CD8+ T-cell infiltration into tumors. PTPN2/1-IN-4 demonstrates significant anticancer activity, inhibiting tumor growth both as a standalone treatment and in combination with anti-PD-1 antibodies in B16-OVA syngeneic mouse models, making it a valuable tool for cancer research.
  32. JAK1 Inhibitor

    JAK1-IN-9 is a potent and selective inhibitor of Janus kinase 1 (JAK1), with an IC50 of 72 nM. This compound demonstrates notable selectivity over other JAK family members, exhibiting an inhibition of 12-fold or more. JAK1-IN-9 is valuable for research applications focused on unraveling the roles of JAK1 in cellular signaling pathways and the development of therapeutic strategies for diseases involving JAK1 dysregulation.
  33. TYK2/JAK2 Inhibitor

    Soficitinib is a selective inhibitor of tyrosine kinase 2 (TYK2) and Janus kinase 2 (JAK2), exhibiting IC50 values of 0.5 nM and 1.2 nM, respectively. This compound is primarily utilized in research related to autoimmune diseases, such as psoriasis and rheumatoid arthritis, as well as inflammatory conditions. Soficitinib's potent inhibition profiles make it a valuable tool for studying the underlying mechanisms of these diseases and evaluating potential therapeutic strategies.
  34. JAK3 Inhibitor

    MS-1020 is a potent ATP-competitive inhibitor of JAK3, targeting the JAK3/STAT signaling pathway. By inhibiting JAK3, MS-1020 effectively induces apoptosis and promotes cell death, alongside decreasing levels of tyrosine phosphorylated STAT3. This compound holds potential for research applications focused on cancers associated with dysregulated JAK3 signaling.
  35. JAK3/BTK Inhibitor

    JAK3/BTK-IN-5 is a potent dual inhibitor targeting Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK). This compound effectively disrupts the BTK/JAK3 signaling pathway, demonstrating potential synergistic effects advantageous for the treatment of autoimmune diseases. JAK3/BTK-IN-5 is valuable for research into conditions related to JAK3 kinase and BTK, making it a crucial tool for studying the pathophysiology of these targets.
  36. JAK2 Inhibitor

    JAK2-IN-9 is a selective JAK2 inhibitor with an IC50 of 5 nM, effectively targeting and inhibiting the phosphorylation of JAK2, as well as downstream signaling proteins STAT3 and STAT5. This compound exhibits metabolic stability and induces apoptosis in targeted cells. JAK2-IN-9 is valuable for research focused on myeloproliferative neoplasms (MPNs) and contributes to elucidating the role of JAK2 signaling in hematological malignancies.
  37. JAK3/TEC Inhibitor

    JAK3-IN-18 is a potent and selective inhibitor of JAK3 and TEC, exhibiting IC50 values of 0.5391 nM and 12.40 nM, respectively. With over 10,000-fold selectivity against AK1, AK2, and TYK2, JAK3-IN-18 shows exceptional efficacy in preclinical models of autoimmune disorders, particularly in the experimental autoimmune encephalomyelitis (EAE) mouse model. This compound is valuable for research applications focused on multiple sclerosis and related autoimmune conditions.
  38. JAK Inhibitor

    JAK-IN-15 is a Janus kinase (JAK) inhibitor that selectively targets JAK family members involved in the signaling pathways of various cytokines. This compound demonstrates significant anti-inflammatory activity and is primarily utilized in research applications focused on autoimmune diseases and hematological malignancies. JAK-IN-15 serves as a valuable tool for studying JAK-mediated signal transduction and exploring potential therapeutic strategies targeting JAK-related disorders.
  39. Tyk-2 Inhibitor

    Tyk2-IN-9 is a selective inhibitor of the tyrosine kinase 2 (Tyk2) with IC50 values of 0.076 nM for TYK2-JH2 and 1.8 nM for JAK1-JH2. This compound demonstrates potent inhibition of Tyk2 activity, making it a valuable tool for investigating the mechanisms underlying inflammatory and autoimmune diseases. Its specificity may enhance research efforts aimed at developing targeted therapies in these areas.
  40. Tyk2 Inhibitor

    Tyk2-IN-22 is a selective inhibitor of tyrosine kinase 2 (Tyk2) with a notable inhibition profile, exhibiting IC50 values of 9.7 nM, 148.6 nM, and 883.3 nM against Tyk2, JAK1, and JAK3, respectively. This compound effectively inhibits downstream phosphorylation of STAT5, making it a valuable tool for studying Tyk2-mediated signaling pathways. Tyk2-IN-22 is suitable for research applications related to autoimmune diseases, inflammatory conditions, and cancer therapies targeting JAK-STAT signaling.
  41. JAK Inhibitor

    (Rac)-TUL01101 is a selective inhibitor of Janus kinases (JAK). This compound plays a significant role in modulating cytokine signaling pathways, making it valuable in the study of inflammatory diseases. Its effectiveness in research applications includes investigations into conditions such as rheumatoid arthritis, atopic dermatitis, and alopecia areata.
  42. JAK/TYK2 Inhibitor

    JAK1/TYK2-IN-4 is a dual inhibitor targeting JAK1 and TYK2, demonstrating IC50 values of 39 nM and 21 nM, respectively. This compound is notable for its oral bioavailability and has potential applications in the study of cytokine signaling and immune responses. It is particularly relevant for research in autoimmune diseases and hematological disorders, providing a valuable tool for elucidating the role of JAK/TYK2 pathways in various biological contexts.
  43. BFAR Inhibitor

    iBFAR2 is a selective inhibitor of the BFAR protein, targeting its role in immune modulation. This compound effectively restores the CD8+ tissue-resident memory T (TRM) cell subset, enhancing anti-tumor immunity in solid tumors. iBFAR2 promotes the association between JAK2 and STAT1 as well as the subsequent phosphorylation of STAT1, contributing to its biological activity in cancer research applications.
  44. JAK2/STAT3 Iinhibitor

    HD-2a is a JAK2/STAT3 inhibitor that functions by downregulating circDcbld2 expression in RAW264.7 cells. This compound is valuable for research into the modulation of the JAK2/STAT3 signaling pathway, which is implicated in various inflammatory and autoimmune disorders. HD-2a can aid in the exploration of therapeutic strategies targeting JAK2/STAT3-mediated processes.
  45. TYK2 Inhibitor

    TYK2 activator-1 is a selective TYK2 activator with an EC50 value of 1.78 μM. This compound also inhibits JAK2 and JAK3, exhibiting IC50 values of 6.8 μM and 6.3 μM, respectively. Due to its unique profile, TYK2 activator-1 is suited for research applications targeting cytokine signaling pathways and immune responses, particularly in the context of autoimmune diseases and inflammatory disorders.
  46. BTK/JAK3 Inhibitor

    JAK3/BTK-IN-6 is a potent dual inhibitor targeting Bruton's Tyrosine Kinase (BTK) and Janus Kinase 3 (JAK3), exhibiting IC50 values of 0.6 nM and 0.4 nM, respectively. This compound demonstrates excellent metabolic stability in human liver microsomes, making it suitable for in vitro studies. JAK3/BTK-IN-6 is valuable in research applications related to hematological disorders and immune system dysfunctions.
  47. JAK Inhibitor

    JAK-IN-27 is a potent inhibitor of the Janus kinase (JAK) family, demonstrating IC50 values of 3.0 nM for TYK2, 7.7 nM for JAK1, and 629.6 nM for JAK3. This compound effectively inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells, with an IC50 of 23.7 nM. JAK-IN-27 is valuable for research applications involving JAK signaling pathways and their role in immune responses and various inflammatory diseases.
  48. JAK Inhibitor

    TK4g is a selective Janus kinase (JAK) inhibitor, exhibiting IC50 values of 12.61 nM for JAK2 and 15.80 nM for JAK3. This compound is crucial for researching lymphoid-derived diseases and various leukemias, providing insights into the role of JAK signaling in cancer biology.
  49. Tyk-2 Inhibitor

    TYK2-IN-11 is a selective inhibitor of Tyk-2, exhibiting IC50 values of 0.016 nM for TYK2-JH2 and 0.31 nM for JAK1-JH2. This compound is valuable for investigating the role of Tyk-2 in inflammatory and autoimmune diseases. Its high potency and selectivity make it a critical tool in the research of signaling pathways associated with these conditions.
  50. JAK Inhibitor

    GDC-9918 is a selective Janus kinase (JAK) inhibitor that modulates JAK signaling pathways, critical for cytokine and growth factor signaling. It demonstrates potent inhibition of JAK activity, making it a valuable tool in investigating immune response and inflammatory processes. This compound is applicable in various research settings, including studies on autoimmune diseases, hematological disorders, and potential oncology applications.

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