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

JAK

Janus kinase

JAK

Related Products

PDF 2.38 MB

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-162317
    AMPK-IN-5
    		Inhibitor
    AMPK-IN-5 (compound 7m) is a Osthole (HY-N0054) derivative, and blocks MAPK signal transduction by inhibiting the phosphorylation of JNK and p38, thereby inhibiting the release of inflammatory cytokines. AMPK-IN-5 reduce DSS-induced ulcerative colitis and LPS (HY-D1056)-induced acute lung injury.
    AMPK-IN-5
  • HY-138222
    JANEX-1 hydrochloride
    		Inhibitor
    JANEX-1 (WHI-P131) hydrochloride is a potent and specific JAK3 inhibitor (Ki=2.3 μM). JANEX-1 hydrochloride shows potent JAK3 inhibitory activity (IC50=78 μM), does not inhibit JAK1 and JAK2.
    JANEX-1 hydrochloride
  • HY-181528
    JAK1/CDK7-IN-1
    		Inhibitor
    JAK1/CDK7-IN-1 is a JAK1/CDK7 inhibitor. JAK1/CDK7-IN-1 forms a stable and tightly bound complex with JAK1. JAK1/CDK7-IN-1 disrupts the cell cycle, induces G2/M phase arrest, and increases the proportion of pre-G1 phase cells. JAK1/CDK7-IN-1 induces cellular apoptosis (apoptosis) and necrosis. JAK1/CDK7-IN-1 is applicable to research related to breast cancer and prostate cancer.
    JAK1/CDK7-IN-1
  • HY-158340
    TYK2 ligand 1
    		Inhibitor
    TYK2 ligand 1 is a TYK2 ligand in the synthesis of PROTAC-based TYK2 degrader (CPD-155, HY-158142).
    TYK2 ligand 1
  • HY-181872
    JAK1-IN-20
    		Inhibitor
    JAK1-IN-20 (Compound 38) is a gut-restricted, orally active, selective JAK1 inhibitor with an IC50 of <0.5 nM. JAK1-IN-20 inhibits the enzymatic activity of JAK1, reduces the production of proinflammatory cytokines (TNF-α, IL-6), and suppresses the phosphorylation of STAT3. JAK1-IN-20 ameliorates ulcerative colitis. JAK1-IN-20 can be used for the research of inflammatory bowel disease.
    JAK1-IN-20
  • HY-178448
    EGFR-IN-178
    		Inhibitor
    EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC50 = 3.4 nM), L858R/T790 M (IC50 = 2.9 nM), and Del19/T790 M (IC50 = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC50 = 55.6 nM) and JAK3 (IC50 = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC).
    EGFR-IN-178
  • HY-15163A
    Zotiraciclib hydrochloride
    		Inhibitor
    Zotiraciclib hydrochloride is a novel small molecule multi-target enzyme inhibitor with activity in inhibiting tumor growth. Zotiraciclib hydrochloride exerts its anti-tumor effect by reducing the level of Myc through inhibiting cyclin-dependent kinase 9 (CDK9). Zotiraciclib hydrochloride may be useful for inhibiting cancers that cross the blood-brain barrier. The high protein level of MCL-1 of Zotiraciclib hydrochloride is associated with survival, suggesting that it may serve as a prognostic factor and inhibitory target in further studies.
    Zotiraciclib hydrochloride
  • HY-129341
    WP1193
    		Inhibitor
    WP1193 is a novel JAK2/STAT3 pathway inhibitor. WP1193 suppresses phosphorylation of JAK2 and STAT3. WP1193 decreases expression of stem cell markers including CD133 and c-myc. WP1193 can be used in the research of glioblastoma.
    WP1193
  • HY-N2409R
    Delphinidin chloride (Standard)
    		Inhibitor
    Delphinidin (chloride) (Standard) is the analytical standard of Delphinidin (chloride). This product is intended for research and analytical applications. Delphinidin chloride is an anthocyanin isolated from berries and red wine. Delphinidin chloride exhibits endothelium-dependent vasodilation and anticancer activity. Delphinidin chloride also modulates JAK/STAT3 and MAPK signaling, thereby inducing apoptosis in HCT116 cells. Delphinidin chloride is also a potent inhibitor of EGFR (IC50: 1.3 μM), shutting down downstream signaling cascades.
    Delphinidin chloride (Standard)
  • HY-W064657
    Momelotinib dihydrochloride
    		Inhibitor
    Momelotinib (dihydrochloride) is a JAK1/JAK2 inhibitor that also antagonizes ACVR1, leading to downregulation of Hepcidin expression and increased availability of iron for erythropoiesis. Momelotinib (dihydrochloride) can reduce transfusion burden and spleen enlargement caused by myelofibrosis, showing potential value in research and application within the field of myelofibrosis.
    Momelotinib dihydrochloride
  • HY-139649
    Ten01
    		Inhibitor
    Ten01 has 5.0 nM activity against JAK1 kinase.
    Ten01
  • HY-149892S
    TYK2 JH2-IN-1-d3
    		Inhibitor
    TYK2?JH2-IN-1-d3 is the a deuterated, orally active and selective TYK2 inhibitor (compound 4h), targeting to JH2 domain (IC50=0.1 nM).
    TYK2 JH2-IN-1-d<sub>3</sub>
  • HY-147742
    Thi-DPPY
    		Inhibitor
    Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF).
    Thi-DPPY
  • HY-143885
    JAK1/TYK2-IN-3
    		Inhibitor
    JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells.
    JAK1/TYK2-IN-3
  • HY-108342
    PF-00956980
    		Inhibitor
    PF-00956980 is a reversible pan-JAK inhibitor with IC50 values of 2.2, 23.1 and 59.9 μM for JAK1, JAK2 and JAK3, respectively. PF-00956980 can be used in the research of lung and skin inflammatory diseases.
    PF-00956980
  • HY-172957
    JNN-5
    		Inhibitor
    JNN-5 is a potent and selective JAK2 inhibitor with an IC50 of 0.41 nM. JNN-5 shows strong antiproliferative activities in the TNBC cell lines (MDA-MB-468, MDA-MB-213, HCC70, MDA-MB-157).
    JNN-5
  • HY-168269
    Tyk2-IN-20
    		Inhibitor
    Tyk2-IN-20 (Example 289) is a potent Tyk2 inhibitor with an IC50 of <5 nM. Tyk2-IN-20 als inhibits JAK1, JAK2, and JAK3 with IIC50 values of <100 nM. Tyk2-IN-20 can be used for the study of inflammatory diseases.
    Tyk2-IN-20
  • HY-144058
    JAK-IN-18
    		Inhibitor
    JAK-IN-18 is a potent inhibitor of JAK. JAK-IN-18 is useful for the research of multiple diseases, particularly ocular, skin, and respiratory diseases (extracted from patent WO2018204238A1, compound 1).
    JAK-IN-18
  • HY-182314
    JAK3-IN-20
    		Inhibitor
    JAK3-IN-20 is a selective and orally active JAK3 inhibitor with an IC50 of 0.7473 nM. JAK3-IN-20 forms a covalent bond with JAK3 Cys909, outcompetes ATP for catalytic site binding, and blocks JAK-STAT pathway activation. JAK3-IN-20 inhibits migration, proliferation, and tumor growth of Bortezomib (HY-10227)-resistant cancer cells. JAK3-IN-20 induces dose-dependent apoptosis. JAK3-IN-20 can be used for the research of Bortezomib-resistant multiple myeloma.
    JAK3-IN-20
  • HY-19568S
    Peficitinib-d3
    		Inhibitor
    Peficitinib-d3 (ASP015K-d3) is the deuterium labeled Peficitinib (HY-19568). Peficitinib (ASP015K) is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
    Peficitinib-d<sub>3</sub>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
JAK Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.