1. Epigenetics
    JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
    Stem Cell/Wnt
  2. JAK

JAK

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 Related Products (311):

Cat. No. Product Name Effect Purity
  • HY-15315
    Baricitinib Inhibitor
    Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
  • HY-50856
    Ruxolitinib Inhibitor 99.99%
    Ruxolitinib (INCB18424) is a potent 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[1]. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy[3].
  • HY-19569
    Upadacitinib Inhibitor 99.98%
    Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research[1][2].
  • HY-40354
    Tofacitinib Inhibitor 99.99%
    Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
  • HY-117287
    Deucravacitinib Inhibitor 99.87%
    Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis[1][2].
  • 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[1][2][3][4].
  • HY-118310
    Xylocydine Inhibitor
    EP009 is a JAK3 inhibitor. In vitro studies have shown that EP009 is a low-micromolar JAK3 inhibitor that selectively inhibits IL-2-mediated JAK3 tyrosine phosphorylation in Kit225 cells (cellular IC50=10-20 μM) without affecting IL-3-induced JAK2 phosphorylation in BaF/3 cells (up to 50 μM). EP009 significantly reduced Kit225 cell viability (LD50=5.0 μM at 72 hr) while having no effect on BaF/3 cells[1].
  • HY-18200A
    Atopaxar hydrochloride Inhibitor
    Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC50 of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC50=7.02 μM), arrests the cell cycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease[1][2][3].
  • HY-18301
    JAK-IN-35 Inhibitor
    JAK-IN-35 (compound TG46) is a JAK2 inhibitor that canb be used in cancer research[1].
  • HY-161259
    JAK-IN-36 Inhibitor
    JAK-IN-36 (Compound 12e) is a potent and selective inhibitor of Janus Kinase 1 (JAK1) with a IC50 value of 2.2 nM. JAK-IN-36 can be used in the study of autoimmune diseases[1].
  • HY-153058
    LRRK2-IN-8 Inhibitor
    LRRK2-IN-8 is a LRRK2 inhibitor. LRRK2-IN-8 inhibits LRRK2 (wt) and LRRK2 (G2019) with IC50s lower than 10 nM, and inhibits TYK2 and NUAK1 with IC50s of 10-100 nM[1].
  • HY-18709
    Tyk2-IN-3 Inhibitor
    Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of 485 nM.
  • HY-19569A
    Upadacitinib tartrate tetrahydrate Inhibitor
    Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib tartrate tetrahydrate displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research[1][2].
  • HY-14722C
    NVP-BSK805 trihydrochloride Inhibitor
    NVP-BSK805 trihydrochloride trihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively[1].
  • HY-15166B
    (E/Z)-Zotiraciclib citrate Inhibitor 98.06%
    (E/Z)-Zotiraciclib citrate is a potent CDK2, JAK2, and FLT3 inhibitor[1].
  • HY-N1356
    Reticuline Inhibitor 98.91%
    Reticuline shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3[1]. Reticuline exhibits cardiovascular effects[2].
  • HY-116505
    JAK1-IN-4 Inhibitor
    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)[1].
  • HY-163314S
    Tyk2-IN-18-d3 Inhibitor
    Tyk2-IN-18-d3 (Compound 18) is a Tyk2 inhibitor with an IC50 value of < 30 nM for both IL-23 and IFNα. Tyk2-IN-18-d3 can be used for research on autoimmune diseases[1].
  • HY-102055
    JAK2 JH2 Tracer 98.03%
    JAK2 JH2 Tracer (Tracer 5) is a fluorescent probe for JAK2 JH2 domain, with a Kd of value 0.2 μM[1][2].
  • HY-130247
    JAK2/FLT3-IN-1 Inhibitor 99.79%
    JAK2/FLT3-IN-1 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. JAK2/FLT3-IN-1 has anti-cancer activity[1].