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-19544
    JAK3-IN-1
    Inhibitor 99.31%
    JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).
    JAK3-IN-1
  • HY-101976
    JAK3-IN-6
    Inhibitor 99.48%
    JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.
    JAK3-IN-6
  • HY-18300A
    Filgotinib maleate
    Inhibitor 99.88%
    Filgotinib maleate (GLPG0634 maleate) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib maleate can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values ​​of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib maleate also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib maleate can be used in the study of rheumatoid arthritis and inflammatory bowel disease.
    Filgotinib maleate
  • HY-14722A
    NVP-BSK805 dihydrochloride
    Inhibitor 99.36%
    NVP-BSK805 dihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
    NVP-BSK805 dihydrochloride
  • HY-153568
    JAK1-IN-11
    Inhibitor 98.27%
    JAK1-IN-11 (compound 11) is a potent inhibitor of JAK,with IC50s of 0.02 nM (JAK1),and 0.44 nM (JAK2),respectively. JAK1-IN-11 has high selectivity against JAK1 over JAK2.
    JAK1-IN-11
  • HY-101762
    TyK2-IN-2
    Inhibitor 99.05%
    TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TyK2-IN-2 also inhibits phosphodiesterase 4 (PDE4) with an IC50 of 62 nM. TyK2-IN-2 can be used for the research of inflammatory and autoimmune diseases.
    TyK2-IN-2
  • HY-16640
    TCJL37
    Inhibitor 99.89%
    TCJL37 is a potent, selective, and orally bioavailable TYK2 inhibitor with a Ki of 1.6 nM. TCJL37 can be used for the research of inflammatory bowel diseases (IBD).
    TCJL37
  • HY-40354C
    (3S,4S)-Tofacitinib
    Inhibitor 99.75%
    (3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
    (3S,4S)-Tofacitinib
  • HY-126242S
    Tyk2-IN-7
    Inhibitor 99.58%
    Tyk2-IN-7 is an orally active TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 can inhibit the IL-23 and IFN-α signaling pathways. Tyk2-IN-7 is commonly used in the study of inflammatory conditions such as colitis.
    Tyk2-IN-7
  • HY-15999A
    Cerdulatinib hydrochloride
    Inhibitor 98.96%
    Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies.
    Cerdulatinib hydrochloride
  • HY-153701S
    Envudeucitinibum
    Inhibitor 99.56%
    Envudeucitinibum (Envudeucitinib) is a highly selective, allosteric and orally active TYK2 inhibitor binding to the JH2 domain of TYK2. Envudeucitinibum has no off-target effects on other kinases (JAK1-3). Envudeucitinibum reduces signaling and production of proinflammatory cytokines including IL-12, IL-23, IL-17, and type I interferons (IFNs). Envudeucitinibum can be used for the research of plaque psoriasis, systemic lupus erythematosus (SLE), and other immune-mediated diseases.
    Envudeucitinibum
  • HY-16379B
    Pacritinib citrate
    Inhibitor 99.68%
    Pacritinib (SB1518) citrate is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib citrate also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM). Pacritinib citrate can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF).
    Pacritinib citrate
  • HY-15166B
    (E/Z)-Zotiraciclib citrate
    Inhibitor 99.83%
    (E/Z)-Zotiraciclib citrate is a potent CDK2, JAK2, and FLT3 inhibitor.
    (E/Z)-Zotiraciclib citrate
  • HY-174280
    Modzatinib
    Inhibitor
    Modzatinib (ITK kinase-IN-1) is an oral active, selective, covalent ITK/JAK3 dual-target inhibitor with IC50 values of 8 nM and 23 nM, respectively. Modzatinib exhibits anti-inflammatory activity and can be used in the research of autoimmune and inflammatory diseases.
    Modzatinib
  • HY-13827
    JAK-IN-1
    Inhibitor 98.39%
    JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.
    JAK-IN-1
  • HY-N3011
    Iridin
    Inhibitor 99.72%
    Iridin is an orally active natural isoflavone. Iridin inhibits the PI3K/AKT and PKM2 signaling pathways, and downregulates the JAK/STAT and NF-κB pathways. Iridin induces Fas-mediated extrinsic apoptosis, G2/M cell cycle arrest, and inhibits cell proliferation. Iridin reduces inflammation, inhibits ROS production, suppresses glycolysis, and also exhibits antioxidant and antidiabetic activities. Iridin can be used in research related to gastric cancer and acute lung injury.
    Iridin
  • HY-147330B
    SJ1008030 formic
    Inhibitor 98.91%
    SJ1008030 (compound 8) formic is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 formic inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 formic can be used for the research of leukemia.
    SJ1008030 formic
  • HY-178500A
    WCY-8-67 TFA
    Inhibitor 99.40%
    WCY-8-67 TFA is an orally active and selective USP5 inhibitor, with an IC50 value of 1.33 μM. WCY-8-67 TFA induces apoptosis and suppresses JAK/STAT3 and PI3K/AKT signaling pathways. WCY-8-67 TFA inhibits proliferation of AE-positive AML cells, induces G1 phase arrest and differentiation of AML cells. WCY-8-67 TFA demonstrates potent anti-leukemic efficacy in mice. WCY-8-67 TFA can be used for the study of acute myeloid leukemia.
    WCY-8-67 TFA
  • HY-153050
    JAK-IN-24
    Inhibitor 99.35%
    JAK-IN-24 is a JAK inhibitor, with IC50s of 0.534 and 24 nM at the presence of 4 μM or 1mM ATP, respectively. JAK-IN-24 also inhibits PBMC IL-15 induced STAT5 phosphorylation with an IC50 of 86.171 nM. JAK-IN-24 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    JAK-IN-24
  • HY-13895
    WHI-P154
    Inhibitor 98.77%
    WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively.
    WHI-P154
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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