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-100895
    SAR-20347
    Inhibitor
    SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively.
    SAR-20347
  • HY-125834
    GMB-475
    Inhibitor 98.69%
    GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007)).
    GMB-475
  • HY-132819
    Ilunocitinib
    Inhibitor 98.24%
    Ilunocitinib (compound 27) is a JAK inhibitor (extracted from patent WO2009114512A1).
    Ilunocitinib
  • HY-13775
    XL019
    Inhibitor 99.65%
    XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
    XL019
  • HY-131968
    BMS-986202
    Inhibitor 99.92%
    BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 value of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 value of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research. BMS-986202 is a de novo deuterium.
    BMS-986202
  • HY-109148
    Izencitinib
    Inhibitor 99.67%
    Izencitinib (TD-1473) is an orally active, non-selective and gut-restricted JAK inhibitor. Izencitinib (TD-1473) can be used in the study for ulcerative colitis.
    Izencitinib
  • HY-130247
    Flonoltinib
    Inhibitor 99.48%
    Flonoltinib is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. Flonoltinib has anti-cancer activity.
    Flonoltinib
  • HY-N0918
    Desmethoxyyangonin
    Inhibitor 99.46%
    Desmethoxyyangonin is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC50: 0.123  µM). Desmethoxyyangonin exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin induces CYP3A23 expression and leads to skeletal muscle relaxation.
    Desmethoxyyangonin
  • HY-10962
    Momelotinib sulfate
    Inhibitor 98.06%
    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
  • HY-109178
    Ifidancitinib
    Inhibitor 98.01%
    Ifidancitinib (ATI-50002) is an orally available, potent and selective inhibitor of JAK kinase 1/3 that disrupts γc cytokine signaling. Ifidancitinib is used in the research of allergy, asthma, and autoimmune diseases.
    Ifidancitinib
  • HY-137756
    JAK2-IN-6
    Inhibitor
    JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells.
    JAK2-IN-6
  • HY-18976
    UF010
    99.83%
    UF010 is a selective inhibitor of class I HDAC. UF010 has cytotoxicity to cancer cells and reduces neuroinflammation in the hippocampus. UF010 can be used for the research of neurological diseases.
    UF010
  • HY-18200
    Atopaxar
    Inhibitor 99.87%
    Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease.
    Atopaxar
  • HY-108264
    TCS 21311
    Inhibitor 99.49%
    TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively.
    TCS 21311
  • HY-146066
    α7 nAchR-JAK2-STAT3 agonist 1
    Agonist 99.54%
    α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis.
    α7 nAchR-JAK2-STAT3 agonist 1
  • HY-B0072
    Tropisetron
    Inhibitor 98.72%
    Tropisetron is an orally active 5-HT3R antagonist (Ki = 5.3 nM) as well as being a potent and selective α7 nicotinic partial agonist (EC50 = 1.3 μM). Tropisetron prevents phosphorylation and activation of the p38 MAPK. Tropisetron inhibits both IL-2 gene transcription and IL-2 synthesis in stimulated T cells. Tropisetron inhibits the binding to DNA and the transcriptional activity of NFAT and AP-1. Tropisetron is anti-inflammatory and antiemetic. Tropisetron has antitumor and neuroprotective effects. Tropisetron can be studied in research for diseases including hemorrhagic cystitis, chronic joint inflammation, lung cancer and chronic cerebral hypoperfusion.
    Tropisetron
  • HY-N1356
    Reticuline
    Inhibitor 98.91%
    Reticuline shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3. Reticuline exhibits cardiovascular effects.
    Reticuline
  • HY-146186
    JAK2 JH2 binder-1
    Modulator
    JAK2 JH2 binder-1 (compound 11) is a potent and selective JAK2 JH2 binder, with a Kd of 37.1 nM. JAK2 JH2 binder-1 has the potential for various myeloproliferative neoplasms research.
    JAK2 JH2 binder-1
  • HY-112724
    Ivarmacitinib
    Inhibitor 99.82%
    Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects.
    Ivarmacitinib
  • HY-112708A
    Brepocitinib P-Tosylate
    Inhibitor 99.98%
    Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. Brepocitinib P-Tosylate also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively.
    Brepocitinib P-Tosylate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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