JAK

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. JAK3/BTK Inhibitor

    JAK3/BTK-IN-4 is a potent inhibitor targeting both JAK3 and BTK kinases, which are critical in the modulation of immune responses involved in autoimmune diseases. By simultaneously inhibiting the BTK/JAK3 signaling pathway, JAK3/BTK-IN-4 demonstrates synergistic effects, making it a valuable tool for studying JAK3 and BTK-related pathologies. This compound is particularly relevant for research applications focused on therapeutic strategies for autoimmune disorders.
  9. JAK1 Inhibitor

    JAK1-IN-10 is a selective inhibitor of Janus kinase 1 (JAK1), characterized by its cyano-substituted cyclic hydrazine structure. This compound exhibits potent inhibition of JAK1 activity, making it a valuable tool for investigating the role of JAK1 in various cellular signaling pathways. Its application is particularly relevant in research areas such as immunology, oncology, and inflammatory diseases, where modulation of JAK1 can influence disease progression and therapeutic outcomes.
  10. TYK2/JAK2 Inhibitor

    JAK2/TYK2-IN-1 is a selective inhibitor targeting TYK2 and JAK2, demonstrating IC50 values of 9 nM for TYK2 and 157 nM for JAK2. This compound exhibits notable anti-inflammatory activity, making it valuable for research into inflammatory diseases and immune responses. Its specificity for TYK2 highlights its potential in understanding signal transduction pathways and therapeutic interventions in related conditions.
  11. JAK3 Inhibitor

    JAK3-IN-14 is a selective JAK3 inhibitor that demonstrates potent activity with an IC50 of 38 nM for JAK3 and 600 nM for JAK2. This compound effectively inhibits IL-4 and IL-3 induced proliferation of TF-1 cells, exhibiting IC50 values of 600 nM and 500 nM, respectively. JAK3-IN-14 is valuable for research applications related to cytokine signaling and immune response modulation.
  12. SYK/JAK Inhibitor

    SYK/JAK-IN-1 is a dual inhibitor targeting SYK and JAK2, exhibiting IC50 values of less than 5 nM for both kinases. This compound demonstrates significant anti-inflammatory and anti-proliferative activities, making it a valuable tool for research involving hematological malignancies and autoimmune disorders. Its potent inhibition profile allows for the exploration of signaling pathways associated with SYK and JAK2, facilitating studies in cancer biology and immunology.
  13. JAK1 Inhibitor

    MMT3-72 is a selective inhibitor of Janus kinase 1 (JAK1), demonstrating effective modulation of the JAK-STAT signaling pathway. This compound significantly reduces phosphorylated STAT3 (p-STAT3) levels in models of dextran sulfate sodium (DSS)-induced colitis, highlighting its potential role in inflammatory bowel disease research. MMT3-72 serves as a valuable tool for studying JAK1-related signaling mechanisms and therapeutic interventions in related conditions.
  14. JAK1 Inhibitor

    JAK1-IN-17 is a highly selective inhibitor of Janus kinase 1 (JAK1), exhibiting a Ki of 1.9 nM. This compound maintains effective potency in whole blood due to its low whole blood shift, making it a valuable tool for hematological studies. Additionally, JAK1-IN-17 is a nitrile-containing analogue that displays weak reversible inhibition of CYP3A4, demonstrated by an IC50 of 7.9 μM. Researchers can utilize JAK1-IN-17 in cancer research to explore the therapeutic potential of JAK1 inhibition in various malignancies.
  15. JAK3 Inhibitor

    JAK3-IN-12 is a potent inhibitor of Janus kinase 3 (JAK3), exhibiting IC50 values of 9.5 nM, 18 nM, and 42 nM for JAK3, JAK1, and JAK2, respectively. This compound serves as a valuable tool for investigating the role of JAK3 in various biological processes, particularly in the context of autoimmune diseases such as rheumatoid arthritis. Its selective inhibition can facilitate understanding of JAK3's function and its potential as a therapeutic target in related research applications.
  16. JAK inhibitor

    JAK kinase-IN-1 is a selective inhibitor of Janus kinase (JAK) family members, effectively targeting TYK2, JAK1, JAK2, and JAK3 with IC50 values of 4.2 nM, 32 nM, 27 nM, and 3473 nM, respectively. This compound demonstrates significant biological activity in modulating JAK-mediated signaling pathways, making it a valuable reagent for research on immune responses and inflammatory diseases. Its specificity and potency contribute to its utility in investigating the role of JAK kinases in various cellular processes and therapeutic applications.
  17. JAK1 Inhibitor

    JAK1-IN-19 is a potent inhibitor of Janus kinase 1 (JAK1), demonstrating IC50 values of 0.02 nM for JAK1, 0.5 nM for JAK2, 91 nM for JAK3, and 0.2 nM for TYK2. This compound exhibits enhanced intrinsic clearance in both rat and human models. JAK1-IN-19 is applicable for research in atopic dermatitis and other autoimmune diseases, facilitating the investigation of JAK1 signaling pathways and their role in inflammatory responses.
  18. JAK1/2/3 Inhibitor

    INCB16562 is a selective inhibitor targeting JAK1 and JAK2, with a notable preference for JAK1 over JAK3. It effectively inhibits interleukin-6 (IL-6)-induced phosphorylation of STAT3, thereby blocking the proliferation and survival of myeloma cells reliant on IL-6 for growth. Furthermore, INCB16562 demonstrates antitumor activity in vivo by reducing the growth of myeloma xenografts in murine models. This compound shows potential for advancing research in multiple myeloma therapies.
  19. JAK1/2 Inhibitor

    JAK1/2-IN-2 is a highly selective inhibitor of the Janus kinase 1 and 2 (JAK1/2) pathways, demonstrating Ki values of 2 nM and 0.6 nM, respectively. This compound is instrumental in research focused on the modulation of cytokine signaling pathways and holds potential for therapeutic applications in autoimmune diseases and hematological malignancies. Its potent inhibition of JAK1/2 makes it a valuable tool for understanding the role of these kinases in various biological processes.
  20. JAK2 Inhibitor

    Tkip is a selective inhibitor of JAK2, targeting the JAK2 autophosphorylation site. It effectively inhibits JAK2 autophosphorylation and the phosphorylation of the IFN-γ receptor subunit IFNGR-1, thereby reducing the antiviral effects of IFN-γ and downregulating MHC Class I molecule expression. Tkip is a valuable tool for investigating the IFN-γ signaling pathway and its implications in various biological processes.
  21. BET/JAK2/FLT3 Inhibitor

    SG3-179 is a selective inhibitor of BET bromodomain proteins, with additional activity against JAK2 and FLT3. This compound effectively reduces HOXB13 protein expression, demonstrating potential relevance in the study of multiple myeloma (MM1.S). SG3-179 is a valuable tool for research involving epigenetic regulation and signaling pathways associated with hematological malignancies.
  22. JAK3/BTK Inhibitor

    JAK3/BTK-IN-1 is a potent dual inhibitor targeting JAK3 and BTK, key proteins implicated in autoimmune diseases. By simultaneously blocking the BTK/JAK3 signaling pathway, this compound demonstrates synergistic effects that could enhance therapeutic outcomes. JAK3/BTK-IN-1 is suitable for research into JAK3 kinase and BTK-related diseases, facilitating the exploration of innovative treatment strategies in immunology and related fields.
  23. JAK Inhibitor

    Tyk2-IN-17 is a selective inhibitor of the Janus kinase 2 (TYK2). This compound effectively impedes the activity of TYK2, which is crucial in various signaling pathways associated with immune regulation and inflammation. Tyk2-IN-17 is primarily used in research focusing on autoimmune diseases, inflammatory disorders, and cancer biology, providing insights into therapeutic strategies for conditions mediated by aberrant JAK signaling.
  24. JAK Inhibitor

    PF-1367550 is a pan-JAK inhibitor that selectively targets Janus kinase enzymes. It is demonstrated to reduce the release of pro-inflammatory cytokines CXCL9, CXCL10, and CXCL11 from primary airway epithelial cells. This compound is valuable for research in inflammatory diseases and the modulation of immune responses.
  25. JAK Inhibitor

    CEE321 is a potent pan-JAK inhibitor that exhibits an IC50 value of 54 nM. It effectively inhibits key biomarkers associated with atopic dermatitis, making it a valuable tool for research in inflammatory skin conditions and related therapeutic studies. Its broad activity against various JAK isoforms facilitates investigations into the signaling pathways involved in immune responses.
  26. Aurora Kinase A/JAK2 Inhibitor

    AJI-100 is a dual-target inhibitor that selectively inhibits Aurora kinase A and JAK2 with IC50 values of 12.7 nM and 18.5 nM, respectively. By directly blocking Aurora kinase A, AJI-100 disrupts T cell mitosis and cell polarity, while its inhibitory effect on JAK2 activation prevents STAT3 phosphorylation. This compound is valuable for research focused on modulating immune responses and has potential applications in the prevention of graft-versus-host disease (GVHD).
  27. JAK2-STAT5 Activator

    Methionyl-methionine (Met-Met) functions as a JAK2-STAT5 activator, enhancing intracellular substrate availability. This compound has been shown to significantly promote the expression of α-s1 casein (αS1-CN) in mammary explants, mediated through the activation of JAK2-STAT5 and mTOR signaling pathways. Its role in modulating these critical pathways makes it a valuable tool for research in lactation biology and protein synthesis studies.
  28. JAK3 Inhibitor

    CP-690550A is a selective inhibitor targeting Janus kinase 3 (JAK3), with notable efficacy against JAK2 as well. This compound exhibits significant immunosuppressive properties and is primarily utilized in research focused on autoimmune diseases and transplant rejection. Its ability to modulate cytokine signaling pathways makes it a valuable tool for studying immune response mechanisms.
  29. JAK2 Inhibitor

    NMS-P953 is a potent orally active inhibitor of JAK2, exhibiting an IC50 of 0.008 μM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. It is particularly useful in studies focusing on JAK2-related signaling pathways and therapeutic applications in hematological malignancies.
  30. JAK2 Inhibitor

    BVB808 is a selective JAK2 inhibitor, exhibiting approximately 10-fold selectivity for JAK2 over other JAK family members in vitro. This compound effectively inhibits JAK2 activity, leading to a reduction in STAT5 phosphorylation, which in turn disrupts JAK2-dependent cell proliferation and survival signaling pathways. BVB808 is utilized in cancer research, particularly in studies focusing on malignancies driven by JAK2 signaling dysregulation.
  31. JAK3/Syk Inhibitor

    R-348 choline is a potent, orally active inhibitor of Janus kinase 3 (JAK3) and spleen tyrosine kinase (Syk). This compound effectively reduces the expression levels of pro-inflammatory cytokines, including interferon-gamma (IFN-γ), interleukin-6 (IL-6), and interleukin-10 (IL-10). R-348 choline is primarily utilized in research related to acute cardiac allograft rejection and other autoimmune conditions where JAK3 and Syk signaling play critical roles.
  32. JAK3 Inhibitor

    JAK3-IN-19 is a selective inhibitor of Janus kinase 3 (JAK3), a critical component in cytokine signaling pathways. Inhibition of JAK3 has been shown to affect the proliferation and survival of cancer cells. This compound is valuable for research applications focused on understanding the role of JAK3 in various malignancies and exploring its potential as a therapeutic target in cancer treatment.
  33. JAK Inhibitor

    (3S,4R)-Tofacitinib is a less active enantiomer of Tofacitinib, primarily targeting Janus kinase 3 (JAK3) as a potent inhibitor. It exhibits an IC50 of 1 nM, highlighting its potential for modulating immune responses and inflammatory processes. This compound is valuable for research in immunology and the development of therapies targeting JAK-mediated signaling pathways.
  34. JAK Inhibitor

    AS2553627 is a selective JAK inhibitor, exhibiting IC50 values of 0.46 nM for JAK1, 0.30 nM for JAK2, 0.14 nM for JAK3, and 2.0 nM for TYK2. This compound effectively inhibits the proliferation of human and rat T cells in response to IL-2, with IC50 values of 2.4 nM and 4.3 nM, respectively. In preclinical studies, AS2553627 has demonstrated a capacity to mitigate cardiac allograft vasculopathy and fibrosis in rat heart transplant models, thereby improving survival rates and showing potential for use in preventing acute and chronic rejection in heart transplantation.
  35. JAKs Inhibitor

    JAK-IN-34 is a potent inhibitor of Janus kinases (JAKs), demonstrating low nanomolar IC50 values of 0.40 nM for JAK1, 0.83 nM for JAK2, 2.10 nM for JAK3, and 1.95 nM for TYK2. This compound effectively reduces joint swelling, indicating its potential application in inflammatory diseases and autoimmune disorders. Its favorable safety profile makes it a valuable tool for research focused on JAK signaling pathways and related therapeutic interventions.
  36. JAK Inhibitor

    JAK3-IN-7 is a potent and selective inhibitor of Janus kinase 3 (JAK3) with an IC50 of less than 0.01 μM. This compound effectively modulates JAK3-mediated signaling pathways, which are critical for immune response and hematopoiesis. JAK3-IN-7 is valuable for research applications focused on autoimmune diseases, inflammatory disorders, and hematological malignancies.
  37. JAK/HDAC Inhibitor

    JAK/HDAC-IN-2 is a dual-target inhibitor of Janus kinase (JAK) and histone deacetylase (HDAC), specifically inhibiting HDAC3/6 and JAK1/2 with nanomolar potency. This compound demonstrates proapoptotic activity by inhibiting histone deacetylation and STAT3 phosphorylation, contributing to its mechanism of action. JAK/HDAC-IN-2 exhibits significant antiproliferative effects in various hematological malignancies and solid tumors, making it a valuable tool for cancer research and therapeutic studies.
  38. JAK2/Bcr-Abl/FLT3 Inhibitor

    LS-104 is a non-ATP-competitive inhibitor targeting JAK2, Bcr-Abl, and FLT3. It effectively induces apoptosis in JAK2V617F-positive cells while inhibiting JAK2 autophosphorylation and downstream signaling pathways. Additionally, LS-104 demonstrates significant cytotoxic effects and inhibits the proliferation of FLT3-expressing leukemic cells. This hydroxystyryl-acrylonitrile compound holds potential for research into myeloproliferative disorders and refractory or relapsed hematologic malignancies.
  39. JAK3 Inhibitor

    PRN-371 is a potent and selective inhibitor of JAK3. By disrupting the JAK3-STAT signaling pathway, PRN-371 effectively suppresses the proliferation of natural killer and T-cell lymphoma cells, inducing apoptosis in these malignancies. This compound demonstrates significant antitumor activity and is applicable in the research of various cancer types, particularly hematological malignancies.
  40. JAK2 Inhibitor

    JAK2-IN-14 is a highly selective JAK2 inhibitor with an IC50 of 2 nM, demonstrating significant selectivity with 89.5-fold over JAK1, 80.5-fold over JAK3, and 51-fold over TYK2. This compound effectively inhibits the STAT5 signaling pathway, leading to tumor cell cycle arrest and apoptosis. JAK2-IN-14 is a valuable tool for investigating myeloproliferative neoplasms (MPNs) and their underlying mechanisms.
  41. JAK3 Inhibitor

    NSC114792 is a selective inhibitor of Janus kinase 3 (JAK3), which plays a critical role in immune signaling pathways. This compound effectively induces apoptosis in target cells and significantly reduces the protein expression of phosphorylated JAK3 and phosphorylated STAT5. NSC114792 is primarily utilized in research focused on immune responses and related signaling cascades.
  42. DPP

    JAK2/STAT3 Inhibitor

    DPP is a Platinum(IV) complex featuring a pterostilbene-derived axial ligand that specifically targets the JAK2/STAT3 signaling pathway. This compound displays significant antiproliferative activity against breast cancer cells by inducing apoptosis through the activation of caspase-3 and cleavage of poly ADP-ribose polymerase. Additionally, DPP enhances the maturation and antigen presentation capability of dendritic cells, demonstrating favorable safety profiles in in vivo studies, making it a promising candidate for cancer immunotherapy research.
  43. FLT3/JAK2 Inhibitor

    JAK2/FLT3-IN-3 is a potent dual inhibitor of FLT3 and JAK2, exhibiting IC50 values of 2.01 nM for JAK2, 0.51 nM for FLT3, and 104.40 nM for JAK3. This compound induces apoptosis in cancer cells and demonstrates significant antitumor activity. Its ability to inhibit both FLT3 and JAK2 pathways makes it a valuable tool for research related to hematological malignancies and targeted cancer therapies.
  44. JAK2/STAT3 Inhibitor

    Cernuumolide J is a selective inhibitor of JAK2/STAT3 signaling pathway. It induces G2/M phase arrest and apoptosis in HEL leukemia cells by downregulating the phosphorylation of JAK2, STAT3, and Erk, while promoting the phosphorylation of JNK and p38 MAPK. Cernuumolide J exhibits a concentration-dependent growth inhibition of HEL leukemia cells, with an IC50 value of 1.79 μM, making it a valuable compound for research in anti-cancer therapy.
  45. JAK3-Inhibitor

    JAK3 covalent inhibitor-2 is a selective covalent inhibitor targeting Janus kinase 3 (JAK3), exhibiting an IC50 of 7.2 nM. This compound demonstrates anti-inflammatory activity, low toxicity, and favorable bioavailability, making it suitable for research applications involving autoimmune diseases and inflammatory disorders. Its specificity for JAK3 supports investigations into therapeutic strategies aimed at modulating immune responses.
  46. JAK3 Inhibitor

    JAK3-IN-13 is a selective and orally bioavailable inhibitor of JAK3, exhibiting IC50 values of 4728, 2039, 8, and 365 nM against NK1, JNK2, JNK3, and Tyk2, respectively. This compound demonstrates significant antiproliferative effects and induces cell cycle arrest in the G0/G1 phase. JAK3-IN-13 is particularly relevant for research applications focused on tumor biology and the modulation of immune responses.
  47. JAK/STAT Inhibitor

    Phenylpyropene C is a JAK/STAT pathway inhibitor known to effectively inhibit interferon-gamma (IFN-γ) mediated expression of reporter genes, with an IC50 range of 5.4 to 10.8 μM. Additionally, it serves as an inhibitor of acyl-CoA, exhibiting an IC50 of 16.0 μM. This compound is valuable for research applications focusing on the modulation of immune responses and the exploration of cytokine signaling pathways.
  48. JAK1 Inhibitor

    YYSW001 is a selective Janus kinase 1 (JAK1) inhibitor with an IC50 of 6 nM, demonstrating significant efficacy in blocking JAK1-mediated phosphorylation of STAT6 as well as IL-6-induced phosphorylation of STAT3. This compound effectively suppresses pro-inflammatory cytokine levels, reduces paw swelling, and lowers clinical arthritis scores, thereby alleviating joint damage and diminishing bone loss. YYSW001 is particularly valuable for research related to rheumatoid arthritis and inflammation-related disorders.
  49. JAK3 Inhibitor

    JAK3-IN-20 is a selective and orally active JAK3 inhibitor, demonstrating an IC50 of 0.7473 nM. By covalently binding to JAK3 Cys909 and outcompeting ATP at the catalytic site, JAK3-IN-20 effectively blocks JAK-STAT pathway activation. This compound exhibits anti-tumor properties by inhibiting migration, proliferation, and growth of Bortezomib-resistant cancer cells, as well as inducing dose-dependent apoptosis. JAK3-IN-20 is a valuable tool for researching Bortezomib-resistant multiple myeloma.
  50. JAK1 Inhibitor

    oJak-989 is a selective inhibitor of Janus kinase 1 (JAK1), demonstrating a Ki of 2.8 nM for JAK1, 110 nM for JAK3, and 31 nM for TYK2. This compound is particularly relevant in the study of inflammatory diseases, as it may help elucidate the role of JAK1 in various pathological conditions and facilitate the development of targeted therapeutics. Research applications include investigating JAK1-mediated signaling pathways and the potential therapeutic impact on autoimmune disorders.

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