| Description | GNE-4997 is a potent and selective inhibitor of the interleukin-2-inducible T-cell kinase (Ki: 0.09 nM). The correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects decreases cytotoxicity. |
| In vitro | GNE-4997 inhibits PLC-γ phosphorylation in Jurkat cells by T-cell receptor stimulation (IC50: 4 nM). |
| Target activity | ITK:（ki）0.09 nM |
| molecular weight | 515.58 |
| Molecular formula | C25H27F2N5O3S |
| CAS | 1705602-02-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| 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. J Med Chem. 2015 May 14;58(9):3806-16. |