1. Signaling Pathways
  2. Epigenetics
    JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
    Stem Cell/Wnt
  3. JAK

JAK

Janus kinase

Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. Since members of the type I and type II cytokine receptor families possess no catalytic kinase activity, they rely on the JAK family of tyrosine kinases to phosphorylate and activate downstream proteins involved in their signal transduction pathways. The receptors exist as paired polypeptides, thus exhibiting two intracellular signal-transducing domains. JAKs associate with a proline-rich region in each intracellular domain, which is adjacent to the cell membrane and called a box1/box2 region. After the receptor associates with its respective cytokine/ligand, it goes through a conformational change, bringing the two JAKs close enough to phosphorylate each other. The JAK autophosphorylation induces a conformational change within itself, enabling it to transduce the intracellular signal by further phosphorylating and activating transcription factors called STATs. The activated STATs dissociate from the receptor and form dimers before translocating to the cell nucleus, where they regulate transcription of selected genes.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15814
    HG-7-85-01
    Inhibitor 99.94%
    HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.
    HG-7-85-01
  • HY-19631
    Ilginatinib maleate
    Inhibitor 99.87%
    Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
    Ilginatinib maleate
  • HY-131906
    JAK2-IN-7
    Inhibitor 99.15%
    JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.
    JAK2-IN-7
  • HY-148785
    Nimucitinib
    Inhibitor 99.27%
    Nimucitinib is a Janus kinase (JAK) inhibitor.
    Nimucitinib
  • HY-139807
    JAK-IN-14
    Inhibitor 99.15%
    JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC50 of <5 μM. JAK-IN-14 is >8-fold more selective for JAK1 than JAK2 and JAK3 (Patent WO2016119700A1, compound 16).
    JAK-IN-14
  • HY-N4126
    6-Demethoxytangeretin
    Inhibitor 99.37%
    6-Demethoxytangeretin is a flavonoid compound that can be isolated from Citrus reticulata. 6-Demethoxytangeretin has anti-inflammatory and anti-allergic activities and can inhibit the production of IL-6 and the expression of related genes in human mast cells through the ALK and MAPK pathways. 6-Demethoxytangeretin can promote CRE-mediated transcription in hippocampal neurons.
    6-Demethoxytangeretin
  • HY-112391
    SD-1029
    Inhibitor
    SD-1029 is a JAK2/STAT3 inhibitor. SD-1029 inhibits STAT3 nuclear translocation. SD-1029 is an inhibitor of STAT3 activation due to inhibition of JAK2 phosphorylation.
    SD-1029
  • HY-161683
    Tyk2-IN-19
    Inhibitor 98.62%
    Tyk2-IN-19 (Compound 1) is an orally active and blood-brain barrier (BBB) permeable Tyk2 inhibitor. Tyk2-IN-19 can be used for study of neurodegenerative diseases.
    Tyk2-IN-19
  • HY-139837
    GDC-4379
    Inhibitor 98.23%
    GDC-4379 is a JAK1 inhibitor that can be used for the research of asthma.
    GDC-4379
  • HY-120469
    2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
    Inhibitor 99.80%
    GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
    2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
  • HY-18316
    RO495
    Inhibitor 98.59%
    RO495 is a potent inhibitor of non-receptor tyrosine-protein kinase 2 (TYK2 kinase).
    RO495
  • HY-156423
    Tubulin/JAK2-IN-1
    Inhibitor 99.14%
    Tubulin/JAK2-IN-1 (compound 7g) is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. Tubulin/JAK2-IN-1 has potent antiproliferative activity against the cancer cells.
    Tubulin/JAK2-IN-1
  • HY-125019
    iJak-381
    Inhibitor 99.86%
    iJak-381 is a JAK1/2 inhibitor with anti-inflammatory activity. iJak-381 blocks IL-13 signaling and also inhibits IL-4 and IL-6 signaling pathways. iJak-381 also reduced p-STAT6 levels and inhibited the influx of inflammatory cells into the lungs of mice. iJak-381 inhibits airway hyperresponsiveness (AHR).
    iJak-381
  • HY-150720
    TYK2-IN-12
    Inhibitor 98.81%
    TYK2-IN-12 (compound 30) is an orally active, potent and selective TYK2 (tyrosine kinase 2) inhibitor, with a Ki of 0.51 nM. TYK2-IN-12 inhibits IL-12 induced IFNγ, with IC50 values of 2.7 and 7.0 μM in human and mouse whole blood, respectively. TYK2-IN-12 can be used for psoriasis research.
    TYK2-IN-12
  • HY-143444
    JAK-IN-20
    Inhibitor 99.63%
    JAK-IN-20 is a potent, pan and orally active JAK inhibitor with an IC50s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo.
    JAK-IN-20
  • HY-110002
    LFM-A13
    Inhibitor 99.65%
    LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research
    LFM-A13
  • HY-N9942
    Physalin A
    Inhibitor 99.22%
    Physalin A is a biologically active withanolide. Physalin A shows anti-inflammatory, antifibrotic and ameliorative effects on autophagy in models of disc degeneration. Physalin A has antitumor activity and can induce apoptosis, ROS production and G2/M phase cell cycle arrest. Besides. Physalin A can significantly increase the activity of quinone reductase and increase the expression of detoxifying enzymesc.
    Physalin A
  • HY-40354D
    (3R,4S)-Tofacitinib
    Inhibitor 99.88%
    (3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
    (3R,4S)-Tofacitinib
  • HY-126242S
    Tyk2-IN-7
    Inhibitor 99.62%
    Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model.
    Tyk2-IN-7
  • HY-116505
    JAK1-IN-4
    Inhibitor 99.26%
    JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM).
    JAK1-IN-4
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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