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

JAK

Janus kinase

JAK

Related Products

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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.

JAK Isoform Specific Products:

JAK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-156466
    QL-1200186
    		Inhibitor 99.95%
    QL-1200186 is anorally activeand selective inhibitor ofTYK2. Oral administration of QL-1200186, dose-dependently inhibitsinterferon-γ(IFNγ) production afterinterleukin-12(IL-12) challenge and significantly ameliorates skin lesions in psoriatic mice.
    QL-1200186
  • HY-19631B
    Ilginatinib hydrochloride
    		Inhibitor 98.92%
    Ilginatinib hydrochloride (NS-018 hydrochloride) 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 hydrochloride
  • HY-111750
    JAK-IN-3
    		Inhibitor 98.92%
    JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively.
    JAK-IN-3
  • HY-18300A
    Filgotinib maleate
    		Inhibitor 99.88%
    Filgotinib maleate (GLPG0634 maleate) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib maleate can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values ​​of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib maleate also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib maleate can be used in the study of rheumatoid arthritis and inflammatory bowel disease.
    Filgotinib maleate
  • HY-100754B
    (2R,5S)-Ritlecitinib
    		Inhibitor 99.77%
    (2R,5S)-Ritlecitinib ((2R,5S)-PF-06651600) is a potent and selective JAK3 inhibitor (IC50=144.8 nM) extracted from patent US20150158864A1, example 68.
    (2R,5S)-Ritlecitinib
  • HY-109179A
    Itacnosertib (hydrocholide)
    		Inhibitor 99.43%
    Itacnosertib hydrocholide is an inhibitor of JAK2, ACVR1 (ALK2) and ALK5.
    Itacnosertib (hydrocholide)
  • HY-158142
    PROTAC TYK2 degrader-1
    		Degrader 99.55%
    PROTAC TYK2 degrader-1 (CPD-155) is a PROTAC targeting degrader to TYK2 with Dmax >60%. (Structure Note: PINK, TYK2 ligand 1 (HY-158340); Blue, VHL ligand Thalidomide (HY-14658); Black, linker)
    PROTAC TYK2 degrader-1
  • HY-151385A
    (R,R)-VVD-118313
    		Inhibitor 99.54%
    (R,R)-VVD-118313 is the isomer of VVD-118313 (HY-151385). VVD-118313 is a selective JAK1 inhibitor and blocks JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer. (R,R)-VVD-118313 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    (R,R)-VVD-118313
  • HY-153568
    JAK1-IN-11
    		Inhibitor 98.27%
    JAK1-IN-11 (compound 11) is a potent inhibitor of JAK，with IC50s of 0.02 nM (JAK1)，and 0.44 nM (JAK2)，respectively. JAK1-IN-11 has high selectivity against JAK1 over JAK2.
    JAK1-IN-11
  • 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-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[1].
    Tyk2-IN-7
  • 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-156961
    GLPG3667
    		Inhibitor 99.81%
    GLPG3667 is a reversible, ATP-competitive and orally active TYK2 inhibitor with an IC50 of 2.3 nM. GLPG3667 inhibits IFNα/pSTAT1, and the IC50 values ​​in human peripheral blood mononuclear cell (PBMC) and whole blood assays are 70 nM and 623 nM, respectively. GLPG3667 has the potential for the study of inflammatory and autoimmune diseases.
    GLPG3667
  • HY-148791
    Pumecitinib
    		Inhibitor 99.81%
    Pumecitinib is a Janus kinase (JAK) inhibitor with anti-inflammatory activity.
    Pumecitinib
  • 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-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-156621
    Lepzacitinib
    		Inhibitor 99.30%
    Lepzacitinib is a Janus kinase inhibitor targeting to JAK 1/3. Lepzacitinib exhibits anti-inflammatory effect and inhibits atopic dermatitis and other skin diseases.
    Lepzacitinib
  • 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-W062700
    STS-E412
    		Activator 99.72%
    STS-E412 is a selective activator of tissue-protective EPO receptor (including EPOR and CD131). STS-E412 can be used for research of neurodegenerative diseases and organ protection.
    STS-E412
  • HY-139837
    GDC-4379
    		Inhibitor 99.51%
    GDC-4379 is a JAK1 inhibitor that can be used for the research of asthma.
    GDC-4379
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
JAK Isoform Comparison

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