PeptideDB

GNE-955

CAS No.: 1527523-39-2

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, respe
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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.