1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. Itk

Itk

Interleukin-2 inducible T-cell kinase; IL2 inducible T-cell kinase

Itk (Interleukin-2-inducible T-cell kinase) is a Tec family tyrosine kinase that mediates signaling processes after T cell receptor engagement. Activation of Itk requires recruitment to the membrane via its pleckstrin homology domain, phosphorylation of Itk by the Src kinase, Lck, and binding of Itk to the SLP-76/LAT adapter complex. After activation, Itk phosphorylates and activates phospholipase C-gamma1 (PLC-gamma1), leading to production of two second messengers, DAG and IP3. IP3 and DAG stimulate the release of calcium ions from the endoplasmic reticulum and activate Protein Kinase C, respectively. In addition, Itk regulates the development of Th2 cells and their subsequent cytokine secretion, thereby modulating the immune response.

Studies have shown that ITK is involved in the pathogenesis of autoimmune diseases as well as in carcinogenesis. The loss of ITK or its activity either by mutation or by the use of inhibitors led to a beneficial outcome in experimental models of asthma, inflammatory bowel disease and multiple sclerosis among others. In humans, biallelic mutations in the ITK gene locus result in a monogenetic disorder leading to T cell dysfunction, etc. These findings put ITK in the strong focus as a target for drug development.

Itk Related Products (13):

Cat. No. Product Name Effect Purity
  • HY-11092
    BMS-509744
    Inhibitor
    BMS-509744 is a potent, selective and ATP competitive Itk inhibitor with an IC50 of 19 nM.
  • HY-12680
    PRN694
    Inhibitor 99.36%
    PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo.
  • HY-109078
    Vecabrutinib
    Inhibitor 99.85%
    Vecabrutinib (SNS-062) is a potent, noncovalent BTK and ITK inhibitor, with Kd values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib shows an IC50 of 24 nM for ITK.
  • HY-108691
    PF-06465469
    Inhibitor 98.31%
    PF-06465469 is a covalent inhibitor of ITK with an IC50 of 2 nM.
  • 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 drug metabolism and pharmacokinetics profile.
  • HY-146672
    ITK inhibitor 6
    Inhibitor
    ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities.
  • HY-146671
    ITK inhibitor 5
    Inhibitor
    ITK inhibitor 5 (compound 27) is a potent and selective ITK inhibitor with IC50s of 5.6, 25 nM for ITK, BTK, respectively.
  • HY-16984
    GNE-4997
    Inhibitor
    GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity.
  • HY-128726
    ITK inhibitor 2
    Inhibitor
    ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor extracted from patent WO2011065402A1, compound 4, with an IC50 of 2 nM.
  • HY-141864
    ITK/TRKA-IN-1
    Inhibitor
    ITK/TRKA-IN-1 is a dual inhibitor of IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA) with an IC50 value of 1.0 nM and 96 % inhibition, respectively.
  • HY-120559
    GSK-2250665A
    Inhibitor
    GSK-2250665A (Compound 13) is a selective Itk inhibitor with a pKi of 9.2.
  • HY-143901
    EGFR-IN-40
    Inhibitor
    EGFR-IN-40 (compound 3z) is a potent BTK, EGFR, and ITK inhibitor with IC50 values of 1.2 nM, 5.3 nM, and 46.1 nM, respectively.
  • HY-13232
    ITK antagonist
    Inhibitor
    ITK antagonist (compound 10 n) is a potent, orally active and selective ITK (Interleukin-2 inducible T-cell kinase) antagonist (IC50=1 and 20 nM in different assays). ITK antagonist inhibits insulin receptor kinase (IRK) with an IC50 of 160 nM.