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ITK

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).

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  • ITK degrader 2
    Cat. No.
    A84601
    CAS No.
    2858738-65-3

    ITK degrader 2

    ITK Degrader 2 is a PROTAC-based compound that specifically targets and degrades the interleukin-2-inducible T-cell kinase (ITK) with a DC50 value of less than 10 nM. In pharmacokinetic studies in mice, this orally active degrader demonstrates a maximum concentration (Cmax) of 0.87 μM and achieves peak plasma levels (Tmax) at 2 hours post-administration. At a dosage of 90 mg/kg, ITK Degrader 2 effectively reduces ITK levels by 20% within 6 hours, making it a valuable tool for exploring ITK-related signaling pathways and their implications in immune responses.

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