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-12538
    Graveoline
    		Inhibitor 99.96%
    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
  • HY-15814
    HG-7-85-01
    		Inhibitor 99.94%
    HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.
    HG-7-85-01
  • HY-19631B
    Ilginatinib hydrochloride
    		Inhibitor 98.92%
    Ilginatinib hydrochloride (NS-018 hydrochloride) 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 hydrochloride
  • HY-112809
    GSK2646264
    		Inhibitor 98.39%
    GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin.
    GSK2646264
  • HY-16997A
    Itacitinib adipate
    		Inhibitor 99.18%
    Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.
    Itacitinib adipate
  • HY-148791
    Pumecitinib
    		Inhibitor 99.81%
    Pumecitinib is a Janus kinase (JAK) inhibitor. Pumecitinib shows anti-inflammatory activity.
    Pumecitinib
  • HY-131906
    JAK2-IN-7
    		Inhibitor 99.15%
    JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.
    JAK2-IN-7
  • HY-111750
    JAK-IN-3
    		Inhibitor 98.92%
    JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively.
    JAK-IN-3
  • HY-100754B
    (2R,5S)-Ritlecitinib
    		Inhibitor 99.77%
    (2R,5S)-Ritlecitinib (2R,5S)-PF-06651600) is a JAK3 inhibitor (IC50=144.8 nM).
    (2R,5S)-Ritlecitinib
  • HY-100754C
    Ritlecitinib tosylate
    		Inhibitor 99.77%
    Ritlecitinib (PF-06651600) tosylate 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 tosylate 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 tosylate 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 tosylate
  • HY-156621
    Lepzacitinib
    		Inhibitor 99.30%
    Lepzacitinib is a Janus kinase inhibitor targeting to JAK 1/3. Lepzacitinib exhibits anti-inflammatory effect and inhibits atopic dermatitis and other skin diseases.
    Lepzacitinib
  • HY-147330A
    SJ1008030 TFA
    		Inhibitor 99.81%
    SJ1008030 (compound 8) TFA is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 TFA inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 TFA can be used for the research of leukemia.
    SJ1008030 TFA
  • HY-120469
    2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
    		Inhibitor 99.80%
    GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
    2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
  • HY-156423
    Tubulin/JAK2-IN-1
    		Inhibitor 99.14%
    Tubulin/JAK2-IN-1 (compound 7g) is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. Tubulin/JAK2-IN-1 has potent antiproliferative activity against the cancer cells.
    Tubulin/JAK2-IN-1
  • HY-162248
    JAK1/2-IN-1
    		Inhibitor 98.36%
    JAK1/2-IN-1 is a potent JAK1 and JAK2 inhibitor with IC50 values of 0.4 nM and 8.1 nM, respectively. JAK1/2-IN-1 also inhibits IL-4 and IL-13 with IC50s of 136.5 nM and 19.1 nM, respectively (WO2023244775A1; Example 33a).
    JAK1/2-IN-1
  • HY-139423
    JAK1-IN-8
    		Inhibitor
    JAK1-IN-8, a potent JAK1 inhibitor (IC50<500 nM), compound 28, extracted from patent WO2016119700A1.
    JAK1-IN-8
  • HY-150720
    TYK2-IN-12
    		Inhibitor 98.81%
    TYK2-IN-12 (compound 30) is an orally active, potent and selective TYK2 (tyrosine kinase 2) inhibitor, with a Ki of 0.51 nM. TYK2-IN-12 inhibits IL-12 induced IFNγ, with IC50 values of 2.7 and 7.0 μM in human and mouse whole blood, respectively. TYK2-IN-12 can be used for psoriasis research.
    TYK2-IN-12
  • HY-110002
    LFM-A13
    		Inhibitor 99.65%
    LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research
    LFM-A13
  • HY-19631
    Ilginatinib maleate
    		Inhibitor 99.87%
    Ilginatinib maleate (NS-018 maleate) 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 maleate
  • HY-156409
    ABBV-712
    		Inhibitor 99.94%
    ABBV-712 is a selective and orally active inhibitor of Tyrosine kinase 2 (TYK2). ABBV-712 has EC50 values of 0.01, 0.19, and 0.17 μM for TYK2 JH2, TYK2 cells and human whole blood, respectively. ABBV-712 has anti-inflammatory activity and can be used in the research of autoimmune diseases.
    ABBV-712
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
JAK Isoform Comparison

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