| Description | GNE-955 is a potent and orally active inhibitor of pan Pim kinase (Kis: 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively). |
| In vitro | GNE-955 inhibits proliferation of MM.1S cells (IC50: 0.5 μM) after 72 hours treatment. GNE-955 (0.156-5 μM) inhibits the phosphorylation of BAD (s112), S6 (s235/236), S6 (s240/244) and 4EBP (s65). It shows no effect on total BAD, S6 or 4EBP protein levels. |
| Target activity | Pim1:0.018 nM (ki), Pim3:0.08 nM (ki), Pim2:0.11 nM (ki) |
| molecular weight | 416.48 |
| Molecular formula | C22H24N8O |
| CAS | 1527523-39-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Wang X, et al. Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability. J Med Chem. 2017 May 25;60(10):4458-4473. |