| Description | SMI-16a (PIM1/2 Kinase Inhibitor VI) , a cell-permeable thiazolidinedione compound, acts as an effective, ATP-competitive inhibitor against Pim-1/2 kinases (IC50: 150/20 nM) while exhibiting little or no activity against a panel of 57 other kinases (≤18% inhibition at 5 μM). |
| In vitro | PIM1/2 Kinase Inhibitor VI exhibits antitumor activity in PC3 human prostate cancer cultures in vitro (IC50: 48 μM). |
| In vivo | PIM1/2 Kinase Inhibitor VI exhibits antitumor activity in JC adenocarcinoma-transplanted Balb/C mice in vivo (~46% tumor mass reduction on day 20; 50 mg/kg/day, i.p.). |
| Target activity | Pim1:150 nM, Pim2:20 nM |
| Synonyms | PIM1/2 Kinase Inhibitor VI |
| molecular weight | 263.31 |
| Molecular formula | C13H13NO3S |
| CAS | 587852-28-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 150 mg/mL (569.67 mM) |
| References | 1. Xia Z., et al. Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases. J Med Chem. 2009 Jan 8;52(1):74-86. 2. Hiasa M., et al. Pim-2 kinase is an important target of treatment for tumor progression and bone loss in myeloma. Leukemia. 2015 Jan;29(1):207-17. |