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

JAK

Janus kinase

JAK

Related Products

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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-10409AR
    Fedratinib hydrochloride hydrate (Standard)
    		Inhibitor
    Fedratinib (hydrochloride hydrate) (Standard) is the analytical standard of Fedratinib (hydrochloride hydrate). This product is intended for research and analytical applications. Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.
    Fedratinib hydrochloride hydrate (Standard)
  • HY-100754R
    Ritlecitinib (Standard)
    		Inhibitor
    Ritlecitinib (Standard) is the analytical standard of Ritlecitinib (HY-100754). This product is intended for research and analytical applications. Ritlecitinib (PF-06651600) is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE).
    Ritlecitinib (Standard)
  • HY-169758
    CEE321
    		Inhibitor
    CEE321 is a potent pan-JAK inhibitor with an IC50 value of 54 nM. CEE321 potently inhibits biomarkers associated with atopic dermatitis.
    CEE321
  • HY-103018R
    Gusacitinib (Standard)
    		Inhibitor
    Gusacitinib (Standard) is the analytical standard of Gusacitinib (HY-103018). This product is intended for research and analytical applications. 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 (Standard)
  • HY-12538R
    Graveoline (Standard)
    		Inhibitor
    Graveoline (Standard) is the analytical standard of Graveoline (HY-12538). This product is intended for research and analytical applications. Graveoline (Rutamine) is an orally active alkaloid with various activities such as antifungal, antiparasitic, anti-inflammatory, and antitumor effects. Graveoline can induce tumor cell apoptosis and autophagy through a reactive oxygen species-mediated pathway. Graveoline has an MIC of 500 μg/mL for Candida albicans. Graveoline can be used in the research of various diseases such as tumors and liver injury.
    Graveoline (Standard)
  • HY-B0072S
    Tropisetron-d5
    		Inhibitor
    Tropisetron-d5 (SDZ-ICS-930-d5 (free base)) is deuterium labeled Tropisetron. Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT3R antagonists with a Ki of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC50 of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects.
    Tropisetron-d<sub>5</sub>
  • HY-107361R
    Golidocitinib (Standard)
    		Inhibitor
    Golidocitinib (Standard) (AZD4205 (Standard)) is the analytical standard of Golidocitinib (HY-107361). This product is intended for research and analytical applications. Golidocitinib (AZD4205) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM).
    Golidocitinib (Standard)
  • HY-161912
    5TTU
    		Inhibitor
    5TTU is a covalent JAK3 inhibitor. 5TTU not only forms a covalent bond with CYS909 but also establishes a hydrogen bond with the NH group of CYS909.
    5TTU
  • HY-107459R
    (E/Z)-AG490 (Standard)
    		Inhibitor
    (E/Z)-AG490 (Standard) is the analytical standard of (E/Z)-AG490 (HY-107459). This product is intended for research and analytical applications. (E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine Kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
    (E/Z)-AG490 (Standard)
  • HY-19631AR
    Ilginatinib (Standard)
    		Inhibitor
    Ilginatinib (Standard) is the analytical standard of Ilginatinib. This product is intended for research and analytical applications. Ilginatinib (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
    Ilginatinib (Standard)
  • HY-164454
    AJI-100
    		Inhibitor
    AJI-100 is a dual-target inhibitor of Aurora kinase A and JAK2 with IC50 values of 12.7 nM and 18.5 nM, respectively. AJI-100 directly blocks Aurora kinase A to inhibit T cell mitosis and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-100 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD).
    AJI-100
  • HY-100754BR
    (2R,5S)-Ritlecitinib (Standard)
    		Inhibitor
    (2R,5S)-Ritlecitinib (Standard) is the analytical standard of (2R,5S)-Ritlecitinib (HY-100754B). This product is intended for research and analytical applications. (2R,5S)-Ritlecitinib (2R,5S)-PF-06651600) is a JAK3 inhibitor (IC50=144.8 nM).
    (2R,5S)-Ritlecitinib (Standard)
  • HY-N1939R
    Icariside I (Standard)
    Icariside I (Standard) is the analytical standard of Icariside I (HY-N1939). This product is intended for research and analytical applications. Icariside I (GH01) is an orally active metabolite of icalin. Icariside I improves estrogen deficiency-induced osteoporosis by simultaneously regulating osteoblast and osteoclast differentiation. Icariside I promotes ATP (HY-B2176) or Nigericin (HY-127019)-induced mtROS production and NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Icariside I does not alter the activation of NLRC4 and AIM2 inflammasomes. Icariside I inhibits breast cancer proliferation, apoptosis, invasion, and metastasis by targeting the IL-6/STAT3 pathway. Icariside I is a kynurenine-AhR pathway inhibitor that alleviates cancer by blocking tumor immune escape.
    Icariside I (Standard)
  • HY-14986
    JAK-IN-32
    		Inhibitor
    JAK-IN-32 (XC) is a bi-aryl meta-pyrimidine inhibitor of JAK kinase.
    JAK-IN-32
  • HY-10410R
    TG101209 (Standard)
    		Inhibitor
    TG101209 (Standard) is the analytical standard of TG101209 (HY-10410). This product is intended for research and analytical applications. TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
    TG101209 (Standard)
  • HY-113402B
    Gamma-glutamylcysteine ammonium
    		Inhibitor
    Gamma-glutamylcysteine ammonium (γ-Glu-Cys ammonium) is an orally active, blood-brain barrier permeable dipeptide. Gamma-glutamylcysteine ammonium activates AMPK, SIRT1, IL-4/STAT6, AC/cAMP/PI3K, IGF-1R/IRS1/PI3K, and Nrf2 signaling pathways; it inhibits NF-κB, JAK1/STAT1/3, MAPKs, cadmium-induced p38 MAPK, JNK, and PI3K/Akt signaling pathways. Gamma-glutamylcysteine ammonium regulates macrophage polarization, modulates the trafficking of CD36 and GLUT4, induces glutathione synthesis, improves metabolic dysfunction, reduces lipid deposition, ameliorates glucose homeostasis, inhibits apoptosis (Apoptosis), stabilizes mitochondria, suppresses lipid peroxidation, iron accumulation and ferroptosis (Ferroptosis), reduces ds-HMGB1 levels, reverses mechanical hyperalgesia, and alleviates hepatic lipid droplet formation. Gamma-glutamylcysteine ammonium is applicable to research related to inflammatory bowel disease, type 2 diabetes, cadmium-induced neurotoxicity, Alzheimer's disease, cerebral ischemia/reperfusion injury, neuropathy, and alcoholic liver disease.
    Gamma-glutamylcysteine ammonium
  • HY-15315AR
    Baricitinib phosphate (Standard)
    		Inhibitor
    Baricitinib (phosphate) (Standard) is the analytical standard of Baricitinib (phosphate). This product is intended for research and analytical applications. Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
    Baricitinib phosphate (Standard)
  • HY-10193AR
    (1R)-AZD-1480 (Standard)
    		Inhibitor
    (1R)-AZD-1480 (Standard) is the analytical standard of (1R)-AZD-1480 (HY-10193A). This product is intended for research and analytical applications. (1R)-AZD-1480 is the (1R) chiral isomer of AZD-1480, an ATP competitive JAK1 and JAK2 inhibitor.
    (1R)-AZD-1480 (Standard)
  • HY-N8098
    Pulchinenoside E2
    		Inhibitor 99.28%
    Pulchinenoside E2 is a triterpenoid saponin. Pulchinenoside E2 inhibits the phosphorylation of STAT3 and JAK2, blocks the nuclear translocation and transcriptional activity of STAT3, and suppresses STAT3-dependent mitochondrial oxidative phosphorylation. Pulchinenoside E2 inhibits invasion, migration and autophagy of triple-negative breast cancer cells. Pulchinenoside E2 can be used in research related to triple-negative breast cancer.
    Pulchinenoside E2
  • HY-15343R
    CEP-33779 (Standard)
    		Inhibitor
    CEP-33779 (Standard) is the analytical standard of CEP-33779. This product is intended for research and analytical applications. CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
    CEP-33779 (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
JAK Isoform Comparison

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