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-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-145588S
    Povorcitinib-d6
    Povorcitinib-d6 (INCB54707-d6) is the deuterium labeled Povorcitinib (HY-145588). Povorcitinib (INCB54707) is a potent and selective JAK1 inhibitor that effectively reduces abscesses and inflammatory nodules. Povorcitinib is used to study cutaneous lupus erythematosus (CLE) and lichen planus (LP).
    Povorcitinib-d<sub>6</sub>
  • 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-103018S
    Gusacitinib-d4
    Gusacitinib-d4 (ASN-002-d4) is the deuterium labeled Gusacitinib (HY-103018). Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma.
    Gusacitinib-d<sub>4</sub>
  • 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>
  • HY-153858
    PHI-501
    Inhibitor
    PHI-501 is a dual inhibitor targeting RAF/DDR. PHI-501 exhibits significant anti-proliferative effects in melanoma cell lines and significantly inhibits the colony formation of drug-resistant cells. PHI-501 strongly inhibits ERK and AKT phosphorylation. PHI-501 downregulates the gene sets in drug-resistant cells of TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways as well as the epithelial-mesenchymal transition (EMT) signaling pathways. PHI-501 demonstrates significant anti-tumor effects in the SK-MEL3DR xenograft model. PHI-501 can be used for research on the problem of drug resistance in melanoma.
    PHI-501
  • HY-E70834
    JAK1(JH1) Recombinant Human Active Protein Kinase
    JAK1 is a non-receptor tyrosine kinase that plays a critical role in cell signaling via type I/II cytokines and interferons (IFNs). JAK1(JH1) is a kinase domain. JAK1(JH1) Recombinant Human Active Protein Kinase is a recombinant JAK1(JH1) protein that can be used to study JAK1(JH1)-related functions.
    JAK1(JH1) Recombinant Human Active Protein Kinase
  • HY-N14094
    Tubulosine
    Inhibitor
    Tubulosine is an alkaloid. Tubulosine can be isolated from Pogonopus tubulosus (DC.) Schumann. Tubulosine is an ATP-competitive, selective JAK3 inhibitor with an IC50 value of 9.9 nM. Tubulosine also inhibits the kinase activities of other JAK family members, the extent of inhibition is less than that of JAK3, with IC50 values of 69.5, 84.9 and 76.3 nM for JAK1, JAK2 and TYK2, respectively. Tubulosine selectively inhibits JAK3 signalling by binding to the ATP-binding site of the kinase of JAK3. Tubulosine induces apoptotic and necrotic/autophagic cell death. Tubulosine inhibits the process of peptide chain elongation by eukaryotic polysomes by, specifically preventing the elongation-factor-2-dependent step of translocation. Tubulosine exhibits anticancer activity in breast cancer cells.
    Tubulosine
  • HY-155807
    DPP
    Inhibitor
    DPP is a Platinum(IV) complex, bearing pterostilbene-derived axial ligand. DPP inhibit the JAK2-STAT3 pathway in breast cancer (BC) cells with antiproliferative activity, and activates caspase-3 and cleaved poly ADP-ribose polymerase to induces apoptosis. DPP promotes the maturation and antigen presentation of dendritic cells, and exhibits in vivo safety.
    DPP
  • HY-156959
    Ovalicin
    Inhibitor
    Ovalicin is a multi-target inhibitor that targets MetAP2, HRH2, JAK2 and TRPV1, with anti-inflammatory and anti-atopic dermatitis activities. Ovalicin covalently binds to MetAP2 to inhibit its function, thereby blocking the replication of Enterocytozoon bieneusi and Vittaforma corneae. Ovalicin alleviates intestinal injury and prolongs survival in infected mouse models, without showing obvious hepatorenal toxicity. Ovalicin attenuates LPS-induced calcium influx, reduces the infiltration of macrophages and mast cells in the skin, and regulates the expression of inflammation-related genes such as IL-31, effectively relieving allergic symptoms in mouse models. Ovalicin can be used for the research of microsporidiosis and atopic dermatitis.
    Ovalicin
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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