1. Protein Tyrosine Kinase/RTK
  2. Itk

Itk

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 (18):

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
    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[1].
  • HY-108691
    PF-06465469 Inhibitor 99.48%
    PF-06465469 is a covalent inhibitor of ITK with an IC50 of 2 nM[1].
  • HY-128726
    ITK inhibitor 2 Inhibitor 99.66%
    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-109078
    Vecabrutinib Inhibitor 99.76%
    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[1][2].
  • HY-150298
    Soquelitinib Inhibitor
    Soquelitinib (CPI-818) is a highlyl selective covalent ITK inhibitor. Soquelitinib decreases DNA replication and cell cycle signaling[1].
  • 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[1].
  • 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[1].
  • 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 agent metabolism and pharmacokinetics profile[1].
  • HY-12410
    GNE-9822 Inhibitor
    GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM, and an EC50 value of 354.5 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma[1][2].
  • 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[1].
  • HY-101321A
    Immepip dihydrobromide Degrader 99.89%
    Immepip dihydrobromide is a H3 agonist. Immepip dihydrobromide can reduce cortical histamine release. Immepip dihydrobromide can be used for the research of neurological diseases[1].
  • HY-149917
    ITK degrader 1 Degrader
    ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice). ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 also shows good plasma exposure levels[1].
  • 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-153322
    ITK degrader 2 Degrader
    ITK degrader 2 (compound 30) is a modulator of targeted ubiquitination and a targeted protein degrading molecule. ITK degrader 2 degrades ITK[1].
  • 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[1].
  • 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[1].