1557236-81-3
Chemical Structure
GNE-7056
- CAS No.: 1557236-81-3
- Formula:C25H31N5O2S
- Molecular Weight:465.61
InChIKey: TVHDLBOMEGOWNE-UHFFFAOYSA-N
SMILES: O=C(C1=NNC2=C1CCC(C)(C2)C)NC3=CN(C(C4CCS(CC4)=O)C5=CC=CC=C5)N=C3
Biological Activity: GNE-7056 is an orally active interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.2 nM against human kinase, and exhibits high selectivity over LCK kinase. GNE-7056 inhibits PLCγ-1 phosphorylation, suppresses the production of IL-2, IL-4, IL-13 and TH2 cytokines, reduces CD4+ T-cell proliferation, and inhibits activation-induced cell death of CD4+ T cells by decreasing the abundance of FasL. GNE-7056 can be used in asthma-related research[1][2].
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GNE-7056 | GNE-7056 is an orally active interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.2 nM against human kinase, and exhibits high selectivity over LCK kinase. GNE-7056 inhibits PLCγ-1 phosphorylation, suppresses the production of IL-2, IL-4, IL-13 and TH2 cytokines, reduces CD4+ T-cell proliferation, and inhibits activation-induced cell death of CD4+ T cells by decreasing the abundance of FasL. GNE-7056 can be used in asthma-related research. | |||||||||||||||||||||
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References
- [1]. Burch JD, et al. Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo. Journal of medicinal chemistry. 2015 May 14;58(9):3806-16. [Content Brief]
- [2]. Sun Y, et al. Inhibition of the kinase ITK in a mouse model of asthma reduces cell death and fails to inhibit the inflammatory response. Sci Signal. 2015 Dec 1;8(405):ra122.
