Itk (Interleukin-2-inducible T-cell kinase) is a Tec family tyrosine kinase that regulates signaling after T cell receptor activation. Itk must be phosphorylated by the Src kinase Lck, recruited to the membrane via its pleckstrin homology domain, and then bound to the SLP-76/LAT adapter complex in order to become activated. Following activation, Itk phosphorylates and activates PLC-gamma1, which causes the synthesis of the second messengers DAG and IP3. Protein Kinase C is activated and calcium ions are released from the endoplasmic reticulum in response to IP3 and DAG, respectively. Additionally, Itk controls the maturation of Th2 cells and the cytokine secretion that follows, modifying the immune response.
ITK is involved in both the pathogenesis of cancer and autoimmune diseases, according to studies. Experimental models of multiple sclerosis, inflammatory bowel disease, and asthma all benefited from the loss of ITK or its activity, whether through mutation or the administration of inhibitors. Biallelic mutations in the ITK gene locus in humans cause a monogenetic disorder that causes T cell dysfunction, among other things. These results highlight ITK as a prime target for drug development.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V3466 | BMS-509744 | 439575-02-7 | BMS-509744 (BMS509744) is a novel, potent and selective inhibitor of interleukin-2 inducible T cell kinase (ITK) with the potential for immunosuppressive and inflammatory diseases. |
|
V69734 | Immepip dihydrobromide | 164391-47-3 | Immepip diHBr is an H3 agonist. |
|
V80418 | ITK degrader 1 | ITK degrader 1 is a selective degrader of interleukin 2-induced T-cell kinase (ITK) (DC50=3.6 nM). | |
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V69732 | ITK degrader 2 | 2858738-65-3 | ITK degrader 2 (compound 30) is a modulator of targeted ubiquitination and a targeted protein degradation molecule. |
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V69733 | ITK/TRKA-IN-1 | 2655557-54-1 | ITK/TRKA-IN-1 is an ITK/TRKA dual (bifunctional) inhibitor. |
|
V4445 | PF-06465469 | 1407966-77-1 | PF-06465469 (PF06465469) is a novel, potent and covalent inhibitor of ITK (IL-2 inducible T-cell kinase, a nonreceptor tyrosine kinase) with an IC50 of 2 nM. |
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