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-167884
    PF-1367550
    Inhibitor
    PF-1367550 is a pan-JAK inhibitor. PF-1367550 can decrease the levels of release of CXCL9, CXCL10 and CXCL11 from primary airway epithelial cells.
    PF-1367550
  • HY-101024R
    PF-06263276 (Standard)
    Inhibitor
    PF-06263276 (Standard) is the analytical standard of PF-06263276 (HY-101024). This product is intended for research and analytical applications. PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively. PF-06263276 inhibits pSTAT3 and TYK2 pathway. PF-06263276 has a protective effect against ear skin inflammation.
    PF-06263276 (Standard)
  • HY-123939
    JAK1/3-IN-1
    Inhibitor
    JAK1/3-IN-1 is a selective, orally active JAK1/3 inhibitor with IC50 values of 1.9 nM and 0.9 nM, respectively. JAK1/3-IN-1 significantly reduces the mean arterial blood pressure and significantly increases the heart rate in rabbits. JAK1/3-IN-1 decreases the mean arterial blood pressure in conscious telemetered rats and induces lethal cardiovascular effects.
    JAK1/3-IN-1
  • HY-100538R
    DTP3 (Standard)
    Inhibitor
    DTP3 (Standard) is the analytical standard of DTP3 (HY-100538). This product is intended for research and analytical applications. DTP3 TFA is a potent and selective GADD45β/MKK7 inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.
    DTP3 (Standard)
  • HY-107429R
    Abrocitinib (Standard)
    Inhibitor
    Abrocitinib (Standard) is the analytical standard of Abrocitinib. This product is intended for research and analytical applications. Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease.
    Abrocitinib (Standard)
  • 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-109148R
    Izencitinib (Standard)
    Inhibitor
    Izencitinib (Standard) is the analytical standard of Izencitinib (HY-109148). This product is intended for research and analytical applications. Izencitinib (TD-1473) is an orally active, non-selective and gut-restricted JAK inhibitor. Izencitinib (TD-1473) can be used in the study for ulcerative colitis.
    Izencitinib (Standard)
  • 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-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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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