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-116505
    JAK1-IN-4
    Inhibitor 99.26%
    JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM).
    JAK1-IN-4
  • HY-150023
    BI-1622
    Inhibitor 98.97%
    BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.
    BI-1622
  • HY-148785
    Nimucitinib
    Inhibitor 99.27%
    Nimucitinib is a Janus kinase (JAK) inhibitor.
    Nimucitinib
  • HY-130247A
    Flonoltinib TFA
    Inhibitor 98.94%
    Flonoltinib TFA 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 TFA has anti-cancer activity.
    Flonoltinib TFA
  • HY-W062703S
    (Rac)-Ruxolitinib-d9
    Inhibitor 99.44%
    (Rac)-Ruxolitinib D9 ((Rac)-INCB18424 D9) is the deuterium labeled (Rac)-Ruxolitinib. (Rac)-Ruxolitinib is a JAK2 inhibitor.
    (Rac)-Ruxolitinib-d<sub>9</sub>
  • HY-112391
    SD-1029
    Inhibitor
    SD-1029 is a JAK2/STAT3 inhibitor. SD-1029 inhibits STAT3 nuclear translocation. SD-1029 is an inhibitor of STAT3 activation due to inhibition of JAK2 phosphorylation.
    SD-1029
  • HY-W394903
    GS-829845
    Inhibitor 99.91%
    GS-829845 is a major, active metabolite of Filgotinib (HY-18300). GS-829845 is a JAK1 preferential inhibitor but is approximately 10-fold less potent than the parent and with a longer half-life.
    GS-829845
  • HY-139837
    GDC-4379
    Inhibitor 98.23%
    GDC-4379 is a JAK1 inhibitor that can be used for the research of asthma.
    GDC-4379
  • HY-167846
    YLIU-4-105-1
    Inhibitor 99.39%
    YLIU-4-105-1 is a Type II JAK2 inhibitor. YLIU-4-105-1 binds to the ATP-binding pocket of JH1. YLIU-4-105-1 has in vivo pharmacodynamic activity as evidenced by inhibiting pSTAT5, reducing spleen to body weight, and lowering blood reticulocyte counts in a dose-dependent manner.
    YLIU-4-105-1
  • HY-18316
    RO495
    Inhibitor 98.59%
    RO495 is a potent inhibitor of non-receptor tyrosine-protein kinase 2 (TYK2 kinase).
    RO495
  • HY-124727
    ZT55
    Inhibitor 99.51%
    ZT55 is an orally active and highly-selective JAK2 inhibitor with an IC50 value of 0.031 μM. ZT55 inhibits the proliferation of JAK2V617F-expressing HEL cell lines and induces apoptosis and cycle arrest. ZT-55 also effectively inhibits the growth of HEL xenograft tumours in a mice model. ZT-55 can be used in studies of myeloproliferative neoplasms, polycythemia vera and primary thrombocythemia.
    ZT55
  • HY-125019
    iJak-381
    Inhibitor 99.86%
    iJak-381 is a JAK1/2 inhibitor with anti-inflammatory activity. iJak-381 blocks IL-13 signaling and also inhibits IL-4 and IL-6 signaling pathways. iJak-381 also reduced p-STAT6 levels and inhibited the influx of inflammatory cells into the lungs of mice. iJak-381 inhibits airway hyperresponsiveness (AHR).
    iJak-381
  • HY-40354S
    Tofacitinib-13C3
    Inhibitor 99.77%
    Tofacitinib-13C3 is the 13C-labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
    Tofacitinib-<sup>13</sup>C<sub>3</sub>
  • HY-143444
    JAK-IN-20
    Inhibitor 99.63%
    JAK-IN-20 is a potent, pan and orally active JAK inhibitor with an IC50s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo.
    JAK-IN-20
  • HY-W004283R
    Pentadecanoic acid (Standard)
    Inhibitor
    α-Linolenic acid (Standard) is the analytical standard of α-Linolenic acid. This product is intended for research and analytical applications. α-Linolenic acid, isolated from Perilla frutescens, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.
    Pentadecanoic acid (Standard)
  • HY-RS07018
    JAK2 Human Pre-designed siRNA Set A
    Inhibitor

    JAK2 Human Pre-designed siRNA Set A contains three designed siRNAs for JAK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    JAK2 Human Pre-designed siRNA Set A
  • HY-40354D
    (3R,4S)-Tofacitinib
    Inhibitor 99.88%
    (3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
    (3R,4S)-Tofacitinib
  • HY-153701S
    Envudeucitinibum
    Inhibitor
    Envudeucitinibum (Envudeucitinib) is a Janus kinase inhibitor, with anti-inflammatory effect.
    Envudeucitinibum
  • HY-172581
    Clifutinib
    Inhibitor 99.59%
    Clifutinib is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC50 value of 15.1 nM. Clifutinib exerts strong antiproliferative effects on FLT3-ITD acute myeloid leukemia (AML) cell lines (MV-4-11: IC50 = 1.5 nM; MOLM-13: IC50 = 1.4 nM). Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib demonstrates significant antitumor efficacy in mice bearing MV-4-11 or MOLM-13 xenografts. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia.
    Clifutinib
  • HY-15163
    Zotiraciclib
    Inhibitor 99.88%
    Zotiraciclib (TG02) is an orally active potent inhibitor of CDK2, JAK2 and FLT3 with IC50 values of 13, 73, and 56 nM, respectively. Zotiraciclib can be used for the research of advanced leukemias and multiple myeloma.
    Zotiraciclib
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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