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 Related Products (49):

Cat. No. Product Name Effect Purity
  • HY-50856
    Ruxolitinib Inhibitor 99.83%
    Ruxolitinib(INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.
  • HY-50858
    Ruxolitinib phosphate Inhibitor 99.89%
    Ruxolitinib phosphate(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.
  • HY-40354A
    Tofacitinib citrate Inhibitor 99.94%
    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-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-15312
    WP1066 Inhibitor 99.60%
    WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2, but not JAK1 and JAK3.
  • 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-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-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-10193
    AZD-1480 Inhibitor 99.37%
    AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1.
  • 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).
  • HY-18300
    GLPG0634 Inhibitor 99.66%
    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-10961
    CYT387 Inhibitor 98.02%
    CYT387 is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
  • HY-13034
    LY2784544 Inhibitor 98.44%
    LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM.
  • HY-10409
    TG-101348 Inhibitor 98.28%
    TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3, TG-101348 also inhibit BRD4 with IC50 of 340 nM.
  • HY-15999
    Cerdulatinib Inhibitor
    Cerdulatinib is a novel, orally available, ATP-competitive inhibitor that demonstrates selective inhibition of SYK and JAK kinases with IC50 of 32 nM for SYK and 0.5-12 nM for JAKs.
  • HY-12469
    Decernotinib Inhibitor 99.12%
    Decernotinib(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.
  • HY-15343
    CEP-33779 Inhibitor 99.37%
    CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
  • 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-15166
    SB1317 Inhibitor >98.0%
    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.
  • HY-16997
    Itacitinib Inhibitor 99.87%
    Itacitinib (INCB039110) is an oral selective JAK1 inhibitor.