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
    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
    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
    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
    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-10193
    AZD-1480 Inhibitor
    AZD-1480 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-10411
    AZ960 Inhibitor
    AZ960 is a potent and specific inhibitor of the JAK2 kinase with a Ki of 0.45 nM.
  • HY-15312
    WP1066 Inhibitor
    WP1066 is a novel inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.
  • HY-16379
    Pacritinib Inhibitor
    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-10961
    CYT387 Inhibitor
    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
    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.
  • HY-50514
    AT9283 Inhibitor
    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-10409
    TG-101348 Inhibitor
    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, and also inhibits BRD4 with IC50 of 340 nM.
  • HY-15343
    CEP-33779 Inhibitor
    CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
  • HY-15508
    JANEX-1 Inhibitor
    JANEX-1 is a potent and specific JAK3 inhibitor (estimated Ki=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2.
  • HY-15166
    SB1317 Inhibitor
    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-14435
    Pyridone 6 Inhibitor
    Pyridone 6 is a pan-JAK inhibitor, which potently inhibits the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, 5 nM for JAK3, and 15 nM for JAK1, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.
  • HY-10410
    TG101209 Inhibitor
    TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations; TG101209 inhibit BRD4 activity with IC50 of 130 nM.
  • HY-10962
    CYT387 sulfate salt Inhibitor
    CYT387 sulfate salt is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
  • HY-15270
    BMS-911543 Inhibitor
    BMS-911543 is a potent and selective small-molecule inhibitor of JAK2, displays potent anti-proliferative and pharmacodynamic (PD) effects in cell lines dependent upon JAK2 signaling.
  • HY-14722
    NVP-BSK805 Inhibitor
    NVP-BSK805 is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM; >20-fold selectivity towards JAK1, JAK3 and TYK2.