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

JAK

Janus kinase

JAK

Related Products

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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:

JAK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15728S
    Radotinib-d6
    		Inhibitor
    Radotinib-d6 is deuterium labeled Radotinib (HY-15728). Radotinib (IY-5511) is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC50 of 34 nM. Radotinib has anti-prion and anti-tumor activities. Radotinib can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases.
    Radotinib-d<sub>6</sub>
  • HY-144087
    TYK2-IN-11
    		Inhibitor
    TYK2-IN-11 (Compound 5B) is a selective Tyk-2 inhibitor with IC50s of 0.016 and 0.31 nM for TYK2-JH2 and JAK1-JH2, respectively. TYK2-IN-11 can be used for the research of inflammatory or autoimmune disease.
    TYK2-IN-11
  • HY-155808
    STAT3-IN-18
    		Inhibitor
    STAT3-IN-18 (compound SPP) is a platinum (IV) complex with an axial ligand derived from sandalwood. STAT3-IN-18 inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, with anti-proliferative activity. STAT3-IN-18 activates caspase-3 and increases cleaved polyADP-ribose polymerase to induce apoptosis. STAT3-IN-18 promotes maturation and antigen presentation of dendritic cells and demonstrates safety in vivo.
    STAT3-IN-18
  • HY-10409S
    Fedratinib-d9
    		Inhibitor
    Fedratinib-d9 (TG-101348-d9) is deuterium labeled Fedratinib. 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-d<sub>9</sub>
  • HY-173601
    JAK3-IN-17
    		Inhibitor
    JAK3-IN-17 (Compound X15) is an orally active JAK3 inhibitor (IC50: 14.56 nM). JAK3-IN-17 inhibits the production of IL-2 and IL-6 in a DNCB-induced mouse atopic dermatitis model and exhibits anti-inflammatory activity.
    JAK3-IN-17
  • HY-169184
    GDC-9918
    		Inhibitor
    GDC-9918 (compund GDC-9918) is a Janus kinase inhibitor.
    GDC-9918
  • HY-143719
    JAK3/BTK-IN-4
    		Inhibitor
    JAK3/BTK-IN-4 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-4 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147953A1, compound 003)
    JAK3/BTK-IN-4
  • HY-154969
    JAK-IN-29
    		Inhibitor
    JAK-IN-29 (compound 3) is a potent JAK inhibitor.
    JAK-IN-29
  • HY-N0316R
    Mollugin (Standard)
    Mollugin (Standard) is the analytical standard of Mollugin. This product is intended for research and analytical applications. Mollugin is an orally active and potent NF-κB inhibitor. Mollugin induces S-phase arrest of HepG2 cells, and increased intracellular reactive oxygen species (ROS) levels. Mollugin induces DNA damage in HepG2 cells, as well as an increase in the expression of p-H2AX. Mollugin shows anti-cancer effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 (bone morphogenetic protein 2) via the p38-Smad signaling pathway.
    Mollugin (Standard)
  • HY-153566
    JAK1-IN-10
    		Inhibitor
    JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, is a potent and selective JAK1 inhibitor.
    JAK1-IN-10
  • HY-143884
    JAK2/TYK2-IN-1
    		Inhibitor
    JAK2/TYK2-IN-2 is a potent and selective TYK2 inhibitor with IC50 values of 9 and 157 nM for TYK2 and JAK2, respectively. JAK2/TYK2-IN-2 has anti-inflammatory activity.
    JAK2/TYK2-IN-1
  • HY-155951
    JAK3-IN-14
    		Inhibitor 99.32%
    JAK3-IN-14 (compound 1) is a potent JAK3 inhibitor, with IC50 values of 38 and 600 nM for JAK3 and JAK2, respectively. JAK3-IN-14 shows inhibitory of IL-4 and IL-3 induced TF-1 cell proliferation, with IC50 values of 600 and 500 nM, respectively.
    JAK3-IN-14
  • HY-158692
    Tyk2-IN-18
    		Inhibitor
    Tyk2-IN-18 (compound 86) is a potent tyrosine kinase 2 (Tyk2) inhibitor. Tyk2-IN-18 inhibits JAK2-JH2, with an IC50 of ＜10 nM.
    Tyk2-IN-18
  • HY-145029
    SYK/JAK-IN-1
    		Inhibitor
    SYK/JAK-IN-1 is dual SYK/JAK inhibitor with IC50s of <5 nM for SYK and JAK2, respectively.
    SYK/JAK-IN-1
  • HY-N1405R
    Cucurbitacin I (Standard)
    		Inhibitor
    Cucurbitacin I (Standard) is the analytical standard of Cucurbitacin I. This product is intended for research and analytical applications. Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
    Cucurbitacin I (Standard)
  • HY-170772
    Dual Cathepsin L/JAK-IN-1
    		Inhibitor
    Dual Cathepsin L/JAK-IN-1 (Compound A8) is a dual inhibitor of Cathepsin L (CTSL) and JAK, with IC50 values of 0.68 μM, 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for CTSL, JAK1/2/3, and TYK2, respectively. Dual Cathepsin L/JAK-IN-1 effectively blocks the activation of the MAPK, NF-κB, and JAK/STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. Dual Cathepsin L/JAK-IN-1 can be used in research on acute lung injury (ALI).
    Dual Cathepsin L/JAK-IN-1
  • HY-162030
    MMT3-72
    		Inhibitor
    MMT3-72 is a weak inhibitor of JAK1. MMT3-72 has superior efficacy and reduced p-STAT3 in DSS-induced colitis.
    MMT3-72
  • HY-118084
    LS-104
    		Inhibitor
    LS-104 (Tyrene CR-4) is a non-ATP-competitive kinase inhibitor against JAK2, Bcr-Abl and FLT3. LS-104 potently induces apoptosis in JAK2V617F-positive cells and inhibits JAK2 autophosphorylation and downstream signal transduction. LS-104 also inhibits proliferation and induces potent cytotoxic effects in FLT3 expressing leukemic cells. LS-104 is a hydroxystyryl-acrylonitrile compound, which is promising for research of myeloproliferative disorders and refractory/relapsed hematologic malignancies.
    LS-104
  • HY-147975
    JAK3-IN-12
    		Inhibitor
    JAK3-IN-12 (compound 5k) is a highly potent JAK3 inhibitor with IC50 values of 9.5 nM, 18 nM and 42 nM for JAK3, JAK1 and JAK2, respectively. JAK3-IN-12 can be used for researching rheumatoid arthritis.
    JAK3-IN-12
  • HY-156535
    JAK kinase-IN-1
    		Inhibitor
    JAK kinase-IN-1 (Example 1) is a JAK inhibitor. JAK kinase-IN-1 inhibits TYK2, JAK1, JAK2 and JAK3 with IC50 values of 4.2 nM, 32 nM, 27 nM, 3473 nM respectively.
    JAK kinase-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
JAK Isoform Comparison

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