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ITK inhibitors block interleukin-2-inducible T-cell kinase, a Tec family kinase in T-cell receptor signaling. Interleukin-2-inducible T-cell kinase (ITK) is a nonreceptor tyrosine kinase that, after T-cell receptor (TCR) engagement, phosphorylates phospholipase C-γ1 (PLCγ1). Mice lacking Itk, reported in 1995, showed altered TCR signaling and disrupted T-cell development in the thymus. BMS-509744, described in 2004, is a selective ITK inhibitor that reduced T-cell activation and lung inflammation in mice. PRN694 binds covalently and also inhibits resting lymphocyte kinase (RLK), a related Tec kinase, as reported in 2015. PF 06465469 and GNE-4997 are further ITK inhibitors, while modzatinib also blocks Janus kinase 3 (JAK3).
The ITK inhibitor BMS-509744 disrupts several aspects of HIV replication.
PRN694 is a highly selective and potent covalent inhibitor of Tec kinases IL-2-inducible T cell kinase (ITK) and resting lymphocyte kinase (RLK). It inhibits Th1 and Th17 differentiation and cytokine production.
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PF 06465469 is a potent the nonreceptor tyrosine kinase Itk (IL-2 inducible T-cell kinase) inhibitor. It also inhibits BTK.
GSK-2250665A is a Itk inhibitor with pKi = 9.2, it Exhibits selectivity for Itk over Aurora B kinase and Btk (pIC50 values are 6.4 and 6.5, respectively) and a panel of other kinases. Inhibits IFNγ production in PBMCs.
CTA 056 is a potent and selective ITK inhibitor (interleukin-2-inducible T-cell kinase 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.
EGFR-IN-40 is a selective inhibitor targeting Bruton's tyrosine kinase (BTK), epidermal growth factor receptor (EGFR), and IL-2-inducible T-cell kinase (ITK). It exhibits potent inhibitory activity with IC50 values of 1.2 nM for BTK, 5.3 nM for EGFR, and 46.1 nM for ITK. This compound is valuable for research applications focusing on cancer therapeutics and signaling pathways related to these kinases.
Synonyms: ITK kinase-IN-1
Modzatinib is a selective, covalent inhibitor targeting ITK and JAK3, demonstrating IC50 values of 8 nM and 23 nM, respectively. Its potent anti-inflammatory properties make it a valuable tool for research in autoimmune and inflammatory diseases, facilitating the exploration of therapeutic interventions in these areas. Researchers can leverage modzatinib to study the mechanistic roles of ITK and JAK3 in immune responses and disease pathology.
Synonyms: CPI-818
Soquelitinib is a selective covalent inhibitor of interleukin-2-inducible kinase (ITK). It exhibits significant anti-inflammatory activity across multiple models of T cell-mediated inflammatory diseases, including asthma, pulmonary fibrosis, systemic sclerosis, psoriasis, and acute graft-versus-host disease. By inhibiting Th2 cytokine production, Soquelitinib enhances the infiltration of CD8+ T cells into tumors, promoting improved T effector function and potential therapeutic benefits in oncology and immunology research.
GNE-9822 is a potent and selective inhibitor of ITK (Interleukin-2-inducible T-cell kinase) with a Ki value of 0.7 nM and an EC50 value of 354.5 nM. This compound demonstrates favorable ADME properties, making it suitable for in vivo studies. GNE-9822 is primarily utilized in research on asthma and other related immunological conditions, providing insights into the modulation of T-cell signaling pathways.
ITK inhibitor 6 is a highly selective inhibitor of ITK with an IC50 of 4 nM. This compound also demonstrates weaker activity against BTK, JAK3, EGFR, and LCK, with IC50 values of 133 nM, 320 nM, 2360 nM, and 155 nM, respectively. ITK inhibitor 6 effectively inhibits the phosphorylation of PLCγ1 and ERK1/2 pathways and exhibits significant antiproliferative activity. It is a valuable tool for research applications focused on lymphocyte signaling and cancer biology.
ITK-IN-6 is a potent and selective inhibitor of Interleukin-2-inducible T-cell kinase (ITK), with a Kd of 387 nM. It directly targets the ITK kinase domain, effectively blocking the release of pro-inflammatory cytokines and modulating the activation and differentiation of Th2 and Th17 cells. This compound demonstrates significant potential in asthma research by reducing inflammatory cell infiltration, mucus production, and IgE levels, thereby mitigating airway inflammation and improving asthma progression.
ITK inhibitor 5 is a selective inhibitor targeting the interleukin-2-inducible T-cell kinase (ITK) with an IC50 of 5.6 nM. Demonstrating low activity against Bruton's tyrosine kinase (BTK) with an IC50 of 25 nM, this compound is useful in studying T-cell signaling pathways and immune responses. It serves as an effective tool in research aimed at understanding the role of ITK in various hematological disorders and inflammatory diseases.
ITK antagonist is a selective inhibitor of Interleukin-2 inducible T-cell kinase (ITK) with an IC50 value of 1 nM and 20 nM in various assays. This compound is orally active and has shown the ability to inhibit insulin receptor kinase (IRK) with an IC50 of 160 nM. It is valuable for research applications focused on T-cell signaling pathways and the modulation of immune responses.
