| Bioactivity | GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity[1]. |
| Target | Ki: 0.09 nM (ITK) |
| Invitro | GNE-4997 inhibits PLC-γ phosphorylation in Jurkat cells by T-cell receptor stimulation with an IC50 of 4 nM [1]. |
| Name | GNE-4997 |
| CAS | 1705602-02-3 |
| Formula | C25H27F2N5O3S |
| Molar Mass | 515.58 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
GNE-4997
CAS: 1705602-02-3 F: C25H27F2N5O3S W: 515.58
GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the c
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