1. Epigenetics
    JAK/STAT Signaling
    Stem Cell/Wnt
  2. 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 Related Products (60):

Cat. No. Product Name Effect Purity
  • HY-50856
    Ruxolitinib Inhibitor 99.85%
    Ruxolitinib is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, and has > 130-fold selectivity for JAK1/2 versus JAK3.
  • HY-50858
    Ruxolitinib phosphate Inhibitor 99.89%
    Ruxolitinib (phosphate) is the first potent JAK1/2 inhibitor with IC50 values of 3.3 nM/2.8 nM, more than 130-fold selectivity for JAK1/2 versus JAK3.
  • HY-15315
    Baricitinib Inhibitor 99.70%
    Baricitinib is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
  • HY-40354A
    Tofacitinib citrate Inhibitor 99.92%
    Tofacitinib citrate inhibits JAK3 with IC50 of 1 nM while inhibiting JAK2, JAK1, Rock-II and Lck with IC50 values of 20 nM, 112 nM, 3,400 nM and 3,870 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-109053
    Delgocitinib Inhibitor 99.14%
    Delgocitinib is a novel and specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
  • HY-100754
    PF-06651600 Inhibitor 99.98%
    PF-06651600 is a potent JAK3-selective inhibitor with an IC50 of 33.1 nM.
  • HY-16997A
    Itacitinib adipate Inhibitor 98.78%
    Itacitinib adipate is a selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.
  • HY-19569
    Upadacitinib Inhibitor 99.40%
    Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders with an IC50 of 43 nM.
  • HY-10961
    CYT387 Inhibitor 98.11%
    CYT387 is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
  • HY-15312
    WP1066 Inhibitor 99.67%
    WP1066 is a novel inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.
  • HY-10193
    AZD-1480 Inhibitor 99.37%
    AZD-1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of < 0.4 nM, selectively against JAK3 and Tyk2, and to a smaller extent against JAK1.
  • HY-40354
    Tofacitinib Inhibitor 99.62%
    Tofacitinib inhibits JAK3 with IC50 of 1 nM while inhibiting JAK2, JAK1, Rock-II and Lck with IC50 values of 20, 112, 3400 and 3870 nM, respectively.
  • HY-50514
    AT9283 Inhibitor 99.13%
    AT9283 is a multi-targeted inhibitor with IC50s of 1.2 nM, 1.1 nM for JAK2 and JAK3, respectively, and is also potent to Aurora A, Aurora B and Abl(T315I).
  • 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; used in the research of myelofibrosis.
  • HY-18300
    GLPG0634 Inhibitor 99.64%
    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-15999
    Cerdulatinib Inhibitor 99.00%
    Cerdulatinib is a novel, orally available, ATP-competitive JAK and SYK inhibitor that demonstrates selective inhibition of TYK2 and SYK with an IC50 of 0.5 nM and 32 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-10409
    TG-101348 Inhibitor 98.28%
    TG-101348 is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3.
  • HY-13034
    LY2784544 Inhibitor 98.06%
    LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM. LY2784544 also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM.
Isoform Specific Products

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