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

Itk (IL-2诱导的T细胞激酶)

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 相关产品 (8):

目录号 产品名 作用方式 纯度
  • HY-11092
    BMS-509744 Inhibitor
    BMS-509744是有效、选择性的、ATP竞争性的 Itk 激酶抑制剂,IC50值为 19 nM。
  • HY-12680
    PRN694 Inhibitor ≥99.0%
    PRN694 是一种不可逆的,高效选择性的,有效共价结合的白介素 2 诱导细胞激酶 ITK、 静息淋巴细胞激酶 RLK 双重抑制剂,抑制 ITK、RLK 的IC50 分别为 0.3 nM 和 1.4 nM。PRN694 延长靶向停留时间,使效应细胞在体内外持久衰减。
  • HY-109078
    Vecabrutinib Inhibitor 99.85%
    Vecabrutinib (SNS-062) 是一种有效的,非共价的 BTKITK 抑制剂,Kd 值分别为 0.3 nM 和 2.2 nM。Vecabrutinib 对 ITKIC50 值为 24 nM。
  • HY-108691
    PF-06465469 Inhibitor 98.31%
    PF-06465469 是 ITK 的共价抑制剂,IC50 值为 2 nM。
  • HY-128726
    ITK inhibitor 2 Inhibitor
    ITK inhibitor 2 是一种有效的选择性 ITK 抑制剂,IC50值为 2 nM。详细信息请参考专利文献 WO2011065402A1 中的化合物 4。
  • HY-13232
    ITK antagonist Inhibitor
    ITK antagonist (compound 10 n) 是一种有效且选择性的,具有口服活性的 ITK (白细胞介素-2诱导型T细胞激酶) 拮抗剂 (在不同的分析中, IC50=1和20 nM)。ITK antagonist 抑制胰岛素受体激酶 (IRK),IC50 为 160 nM。
  • HY-141864
    ITK/TRKA-IN-1 Inhibitor
    ITK/TRKA-IN-1 是一种ITK/TRKA双重抑制剂,ITK的IC50值为1.0 nM,TRKA的抑制率为 96%。
  • HY-16984
    GNE-4997 Inhibitor
    GNE-4997 是一种有效选择性的白细胞介素 2 诱导的 T 细胞激酶 (ITK) 抑制剂,Ki 为 0.09 nM,GNE-4997 中可溶性元素碱度与靶外抗增殖作用的相关性降低了细胞毒性。
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