1. Signaling Pathways
  2. Epigenetics
    JAK/STAT Signaling
    Stem Cell/Wnt
  3. JAK

JAK

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:

  • JAK1

  • JAK2

  • JAK3

  • Tyk2

  • JAK

JAK Related Products (90):

Cat. No. Product Name Effect Purity
  • HY-50856
    Ruxolitinib Inhibitor 99.99%
    Ruxolitinib is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3.
  • HY-15315
    Baricitinib Inhibitor 99.93%
    Baricitinib is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
  • HY-40354
    Tofacitinib Inhibitor 99.96%
    Tofacitinib is a JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
  • HY-19569
    Upadacitinib Inhibitor 99.96%
    Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders.
  • HY-40354A
    Tofacitinib citrate Inhibitor 99.92%
    Tofacitinib citrate is a JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
  • HY-107429
    Abrocitinib Inhibitor 99.79%
    Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease.
  • HY-50867
    Lestaurtinib Inhibitor >99.0%
    Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively.
  • HY-111745
    Tyk2-IN-5 Inhibitor 99.78%
    Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα. Highly effective in inhibiting IFNγ production in a rat pharmacodynamics model and fully efficacious in a rat adjuvant arthritis model.
  • HY-10409
    Fedratinib Inhibitor 98.62%
    Fedratinib (TG-101348) is a selective inhibitor of JAK2 with an IC50 of 3 nM, showing 35- and 334-fold selectivity over JAK1 and JAK3, respectively.
  • HY-10193
    AZD-1480 Inhibitor 99.37%
    AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50s of 1.3 and <0.4 nM, respectively.
  • HY-16379
    Pacritinib Inhibitor 99.66%
    Pacritinib is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).
  • HY-18960
    CHZ868 Inhibitor 98.33%
    CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.
  • HY-15312
    WP1066 Inhibitor 99.67%
    WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.
  • HY-10961
    Momelotinib Inhibitor 98.11%
    Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
  • HY-117287
    BMS-986165 Inhibitor 99.76%
    BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. BMS-986165 inhibits IL-12/23 and type I IFN pathways.
  • HY-18300
    Filgotinib Inhibitor 99.64%
    Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
  • HY-16997
    Itacitinib Inhibitor 99.87%
    Itacitinib is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis.
  • HY-50514
    AT9283 Inhibitor 99.13%
    AT9283 is a multitargeted kinase inhibitor which potently inhibits aurora kinase A/B, JAK2/3 (IC50=1.2 nM, 1.1 nM).
  • HY-15999
    Cerdulatinib Inhibitor 99.00%
    Cerdulatinib (PRT062070) is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.
  • HY-15166
    SB1317 Inhibitor 99.96%
    SB1317 is a potent inhibitor of CDK2, JAK2, and FLT3 for the treatment of cancer, with IC50 of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively.
Isoform Specific Products

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