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

JAK

Janus kinase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-40354S1
    Tofacitinib-13C3,15N
    Inhibitor
    Tofacitinib-13C3,15N (Tasocitinib-13C3,15N) is 13C and 15N labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
    Tofacitinib-<sup>13</sup>C<sub>3</sub>,<sup>15</sup>N
  • HY-123289
    CP-690550A
    Inhibitor
    CP-690550A is an analogue of Tofacitinib (HY-40354). CP-690550A is a dual inhibitor of JAK2 and JAK3.
    CP-690550A
  • HY-10961R
    Momelotinib (Standard)
    Inhibitor
    Momelotinib (Standard) is the analytical standard of Momelotinib. This product is intended for research and analytical applications. 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.
    Momelotinib (Standard)
  • HY-129679
    NMS-P953
    Inhibitor
    NMS-P953 (compound 28) is an orally active JAK2 inhibitor (IC50=0.008 μM) with antitumor activity.
    NMS-P953
  • HY-110102
    Atiprimod hydrochloride
    Inhibitor
    Atiprimod hydrochloride (SKF 106615) is an orally active immunomodulatory agent that causes phospholipid (PL) accumulation in macrophages.
    Atiprimod hydrochloride
  • HY-120604
    BVB808
    Inhibitor
    BVB808 (NVP_BVB808) is a selective JAK2 inhibitor with approximately 10-fold selectivity for JAK2 over other JAK family members (such as JAK1, JAK3 or TYK2) in vitro. BVB808 inhibits the activity of JAK2 and reduces the phosphorylation of STAT5, thereby blocking the JAK2-dependent cell proliferation and survival signaling pathways. BVB808 can be used in cancer research.
    BVB808
  • HY-10962R
    Momelotinib sulfate (Standard)
    Inhibitor
    Momelotinib (sulfate) (Standard) is the analytical standard of Momelotinib (sulfate). This product is intended for research and analytical applications. Momelotinib sulfate (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).
    Momelotinib sulfate (Standard)
  • HY-123625
    R-348 choline
    Inhibitor
    R-348 (R-932348) choline is a potent and orally active JAK3 and Syk inhibitor. R-348 reduces IFN-γ, IL-6, and IL-10 expression. R-348 effectively diminishes acute cardiac allograft rejection.
    R-348 choline
  • HY-100618R
    Hispidin (Standard)
    Inhibitor
    Hispidin (Standard) is the analytical standard of Hispidin. This product is intended for research and analytical applications. Hispidin, a PKC inhibitor and a phenolic compound can be found in Phellinus linteus, has been shown to possess strong anti-oxidant, anti-cancer, anti-diabetic, and anti-dementia properties[1][2][3][4][5][6][7].
    Hispidin (Standard)
  • HY-W740378
    1,2,3,4-Tetrahydro Staurosporin
    Inhibitor
    1,2,3,4-Tetrahydrostaurosporine is a derivative of Staurosporine (HY-15141) and an inhibitor of mutant EGFR (IC50=74 nM for EGFRT790M). It is selective for EGFRT790M over wild-type EGFR (IC50=390 nM). It also binds to Janus kinase 3 (JAK3).
    1,2,3,4-Tetrahydro Staurosporin
  • HY-16379R
    Pacritinib (Standard)
    Inhibitor
    Pacritinib (Standard) is the analytical standard of Pacritinib. This product is intended for research and analytical applications. Pacritinib (SB1518) 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).
    Pacritinib (Standard)
  • HY-14435R
    Pyridone 6 (Standard)
    Inhibitor
    Pyridone 6 (Standard) is the analytical standard of Pyridone 6. This product is intended for research and analytical applications. 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.
    Pyridone 6 (Standard)
  • HY-164393
    ON044580
    Inhibitor
    ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling.
    ON044580
  • HY-122101
    NSC114792
    Inhibitor
    NSC114792 is a selective JAK3 inhibitor. NSC114792 induces apoptosis. NSC114792 decreases the protein expression of p-JAK3 and p-STAT5.
    NSC114792
  • HY-40354AR
    Tofacitinib citrate (Standard)
    Inhibitor
    Tofacitinib (citrate) (Standard) is the analytical standard of Tofacitinib (citrate). This product is intended for research and analytical applications. Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
    Tofacitinib citrate (Standard)
  • HY-N12473
    25-Deacetylcucurbitacin A
    Inhibitor
    25-Deacetylcucurbitacin A is a Cucurbitane-Type triterpenoid and has the potential to be an anti-cancer agent and JAK/STAT3 signaling pathway inhibitor.
    25-Deacetylcucurbitacin A
  • HY-40354B
    (3S,4R)-Tofacitinib
    Inhibitor
    (3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
    (3S,4R)-Tofacitinib
  • HY-10409R
    Fedratinib (Standard)
    Inhibitor
    Fedratinib (Standard) is the analytical standard of Fedratinib. This product is intended for research and analytical applications. Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.
    Fedratinib (Standard)
  • HY-123187
    AS2553627
    Inhibitor
    AS2553627 is a type of JAK inhibitor, with IC50 values of 0.46, 0.30, 0.14, and 2.0 nM for JAK1, JAK2, JAK3 and TYK2, respectively. AS2553627 can inhibit the proliferation of human and rat T cells stimulated by IL-2, with IC50 values of 2.4 and 4.3 nM, respectively. AS2553627 can reduce cardiac allograft vasculopathy and fibrosis in a rat heart transplant model, effectively extending survival rates. AS2553627 can be used to prevent acute and chronic rejection in heart transplants.
    AS2553627
  • HY-119009
    TM-233
    Inhibitor
    TM-233 is an inhibitor of the JAK/STAT and NF-κB signaling pathways, exhibiting significant antitumor activity. TM-233 reduces the expression of the anti-apoptotic protein Mcl-1 by inhibiting the phosphorylation of JAK2 and STAT3, and regulates its transcription by directly binding to the Mcl-1 gene promoter. Additionally, TM-233 prevents the translocation of NF-κB from the cytoplasm to the nucleus by inhibiting its DNA-binding activity, thereby reducing nuclear NF-κB expression. TM-233 shows potential in overcoming Bortezomib (HY-10227) resistance and can be applied in research related to multiple myeloma.
    TM-233
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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