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-149296
    JAK1-IN-12
    Inhibitor
    JAK1-IN-12 is a selective inhibitor of JAK1, with IC50 of 0.0246 μM. And IC50s of 0.423 μM, 0.410 μM and 1.12 μM for JAK2, JAK3 and TYK2. JAK1-IN-12 promotes hair growth in mice. JAK1-IN-12 can be used for research of immune and inflammatory diseases.
    JAK1-IN-12
  • HY-168893
    K882
    Inhibitor
    K882 (Compound 4e) is a Src inhibitor, with KD of 0.315 μM. K882 induces Apoptosis. K882 inhibits XIAP and Survivin. K882 inhibits the activation of PI3K/Akt/mTOR, Jak1/Stat3, Ras/MAPK signaling pathways. K882 shows anti-tumor activity against non-small cell lung cancer.
    K882
  • HY-169290
    JAK/HDAC-IN-4
    Inhibitor
    JAK/HDAC-IN-4 (compound 11 i) is a JAK/HDAC inhibitor with the IC50 values of 0.49 nM and 12 nM for JAK2 and HDAC6, respectively. JAK/HDAC-IN-4 inhibits the cell proliferation and the production of nitric oxide. JAK/HDAC-IN-4 ameliorates psoriasis-like skin lesions in an Imiquimod (HY-B0180)-induced murine model with low toxicity.
    JAK/HDAC-IN-4
  • HY-161139
    JAK1-IN-14
    Inhibitor
    JAK1-IN-14 (Compound 12a) is a potent and selective JAK1 inhibitor. JAK1-IN-14 inhibits JAK1 and JAK2 with an IC50 value of 12.6 nM and 135 nM. JAK1-IN-14 suppresses hepatic fibrosis levels and can be used for the research of liver fibrosis and inflammatory diseases.
    JAK1-IN-14
  • HY-169986S
    TyK2-IN-21-d3
    Inhibitor
    TyK2-IN-21-d3 (Compound 3c) is the orally active prodrug of the tyrosine kinase 2. TyK2-IN-21-d3 exhibits good chemical stability in aqueous system under different pHs. TyK2-IN-21-d3 alleviates the effect of gastric acid changes on drug absorption and improve the drug bioavailability in rat model.
    TyK2-IN-21-d3
  • HY-144440
    JAK1-IN-9
    Inhibitor
    JAK1-IN-9 (compound 23a) is a potent and selective JAK1 inhibitor with an IC50 of 72 nM. JAK1-IN-9 shows selective against other JAKs by 12 times or more.
    JAK1-IN-9
  • HY-RS07017
    Jak1 Rat Pre-designed siRNA Set A
    Inhibitor

    Jak1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Jak1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Jak1 Rat Pre-designed siRNA Set A
    Jak1 Rat Pre-designed siRNA Set A
  • HY-169242
    JAK1-IN-16
    Inhibitor
    JAK1-IN-16 (compound 4l) is an inhibitor of JAK1/STAT3 and effectively downregulates TLR4 protein expression..
    JAK1-IN-16
  • HY-N0527R
    Pentagalloylglucose (Standard)
    Inhibitor
    Pentagalloylglucose (Standard) is the analytical standard of Pentagalloylglucose. This product is intended for research and analytical applications. Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is an orally active gallic tannin compound and an inducer of apoptosis and autophagy. Pentagalloglucose induces cell apoptosis and autophagy through the GSK3β/β-catenin pathway. Pentagalloglucose has antioxidant, anti mutagenic, anti-inflammatory, anticonvulsant, cardioprotective, anti allergic, cholesterol lowering, and anti-tumor activities.
    Pentagalloylglucose (Standard)
  • HY-144057
    JAK-IN-17
    Inhibitor
    JAK-IN-17 is a potent inhibitor of JAK. JAK-IN-17 is useful for the research of multiple diseases, particularly ocular, skin, and respiratory diseases (extracted from patent WO2021185305A1, compound 9-1).
    JAK-IN-17
  • HY-161354
    JAK3 covalent inhibitor-2
    Inhibitor
    JAK3 covalent inhibitor-2 (compound J1b) is a selective, orally potent JAK3 inhibitor (IC50=7.2 nM) with low toxicity, anti-inflammatory activity and good bioavailability.
    JAK3 covalent inhibitor-2
  • HY-123099
    MS-1020
    Inhibitor
    MS-1020 is a potent and ATP-competitive JAK3 inhibitor. MS-1020 inhibits JAK3/STAT signaling and induces apoptosis. MS-1020 promotes cell death. MS-1020 decreases the expression of tyrosine phosphorylated STAT3 levels. MS-1020 has the potential for the research of cancers harboring aberrant JAK3 signaling.
    MS-1020
  • HY-117287A
    Deucravacitinib hydrochloride
    Inhibitor
    Deucravacitinib hydrochloride (BMS-986165 hydrochloride) is a highly selective all-site inhibitor with potent inhibitory activity against TYK2. Deucravacitinib hydrochloride can effectively block IL-12, IL-23 and type I interferon signaling. Deucravacitinib hydrochloride demonstrates significant efficacy in preclinical models of inflammatory bowel disease. Deucravacitinib hydrochloride demonstrated superiority over placebo and apremilast on multiple efficacy endpoints in moderate to severe plaque psoriasis. Deucravacitinib hydrochloride was well tolerated in inhibition.
    Deucravacitinib hydrochloride
  • HY-143720
    JAK3/BTK-IN-5
    Inhibitor
    JAK3/BTK-IN-5 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-5 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147953A1, example 35)
    JAK3/BTK-IN-5
  • HY-10961S8
    Momelotinib-d4 dihydrochloride hydrate
    Momelotinib-d4 (CYT387-d4) dihydrochloride hydrate is a deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50s of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
    Momelotinib-d<sub>4</sub> dihydrochloride hydrate
  • HY-100849
    JAK 3i
    Inhibitor
    JAK3i is a highly selective JAK3 inhibitor (IC50: 0.43 nM). JAK3i forms a covalent bond with a cysteine in JAK3, but not the closely related kinase domains in JAK1, JAK2, or TYK2. JAK3i abolishes IL-2-driven T-cell proliferation in vivo and has the potential for  autoimmune disease research.
    JAK 3i
  • HY-50856S2
    Ruxolitinib-d9
    Inhibitor
    Ruxolitinib-d9 (INCB18424-d9) is deuterium labeled Ruxolitinib. Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy.
    Ruxolitinib-d<sub>9</sub>
  • HY-155746
    JAK2-IN-9
    Inhibitor
    JAK2-IN-9 (Compound A8) is a selective JAK2 inhibitor (IC50: 5 nM). JAK2-IN-9 inhibits the phosphorylation of JAK2, STAT3, and STAT5. JAK2-IN-9 has metabolic stabilities. JAK2-IN-9 induces apoptosis. JAK2-IN-9 can be used for research of myeloproliferative neoplasms (MPNs).
    JAK2-IN-9
  • HY-18293
    NSC 33994
    Inhibitor
    NSC 33994 (G6) is a selective JAK2 inhibitor, with an IC50 of 60 nM.
    NSC 33994
  • HY-18949
    JI6
    Inhibitor
    JI6 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ~40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, with IC50s of ~250 and ~500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia.
    JI6
Cat. No. Product Name / Synonyms Species Source
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