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-100754CR
    Ritlecitinib tosylate (Standard)
    Inhibitor
    Ritlecitinib (tosylate) (Standard) is the analytical standard of Ritlecitinib (tosylate) (HY-100754C). This product is intended for research and analytical applications. Ritlecitinib (PF-06651600) tosylate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib tosylate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib tosylate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE).
    Ritlecitinib tosylate (Standard)
  • HY-128854R
    Dimethyl biphenyl-4,4'-dicarboxylate (Standard)
    Dimethyl biphenyl-4,4'-dicarboxylate (Biphenyl dimethyl dicarboxylate) (Standard) is the analytical standard of Dimethyl biphenyl-4,4'-dicarboxylate. This product is intended for research and analytical applications. Dimethyl biphenyl-4,4'-dicarboxylate is a hepatoprotectant that can be obtained from Schizandra fructus and may induce a signal transduction similar to that associated with IFN. Dimethyl biphenyl-4,4'-dicarboxylate can be synthesized from bio-derived 4,4’-Dimethylbiphenyl.
    Dimethyl biphenyl-4,4'-dicarboxylate (Standard)
  • HY-10411R
    AZ960 (Standard)
    Inhibitor
    AZ960 (Standard) is the analytical standard of AZ960 (HY-10411). This product is intended for research and analytical applications. AZ960 is a potent and specific inhibitor of the JAK2 kinase with a Ki of 0.45 nM.
    AZ960 (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-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-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 99.80%
    (3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
    (3S,4R)-Tofacitinib
  • HY-109053R
    Delgocitinib (Standard)
    Inhibitor
    Delgocitinib (Standard) is the analytical standard of Delgocitinib (HY-109053). This product is intended for research and analytical applications. Delgocitinib (JTE-052) is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
    Delgocitinib (Standard)
  • 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
  • HY-N6069R
    Raspberry ketone glucoside (Standard)
    Activator
    Raspberry ketone glucoside (Standard) is the analytical standard of Raspberry ketone glucoside (HY-N6069). Raspberry ketone glucoside is a melanogenesis inhibitor. Raspberry ketone glucoside inhibits melanogenesis by activating the IL6/JAK1/STAT3 pathway, inhibiting the transcriptional activity of MITFa, and its downstream expression levels of the TYR and TYRP1a genes. Raspberry ketone glucoside shows remarkable whitening activity on both B16F10 cells in vitro and zebrafish model in vivo.
    Raspberry ketone glucoside (Standard)
  • HY-108264R
    TCS 21311 (Standard)
    Inhibitor
    TCS 21311 (Standard) is the analytical standard of TCS 21311 (HY-108264). This product is intended for research and analytical applications. 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 (Standard)
  • HY-N0484R
    Liensinine (Standard)
    Inhibitor
    Liensinine (Standard) is the analytical standard of Liensinine (HY-N0484). This product is intended for research and analytical applications. Liensinine is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine suppresses autophagy and apoptosis, clears , and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine activates AMPK and inhibits the expression of HIF-1α and VEGF, thereby suppressing angiogenesis. Liensinine exerts anti-tumor effects through ROS-mediated inhibition of the JAK2/STAT3 signaling pathway. Liensinine can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke.
    Liensinine (Standard)
  • HY-50514R
    AT9283 (Standard)
    Inhibitor
    AT9283 (Standard) is the analytical standard of AT9283. This product is intended for research and analytical applications. AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.
    AT9283 (Standard)
  • HY-157121
    JAK-IN-34
    Inhibitor
    JAK-IN-34 (compound 11n) is a potent against of JAKs with IC50 values of 0.40, 0.83, 2.10, 1.95 nM target JAK1, JAK2, JAK3, TYK2, respectively. JAK-IN-34 reduces joint swelling with good safety.
    JAK-IN-34
  • HY-U00390
    JAK3-IN-7
    Inhibitor
    JAK3-IN-7 is a potent and selective JAK3 inhibitor extracted from patent WO2011013785A1, has an IC50 of <0.01 μM.
    JAK3-IN-7
Cat. No. Product Name / Synonyms Species Source
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