SMI-4a (TCS-PIM-1-4a) is a potent, selective, cell-permeable, and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 μM. It also inhibits Pim-2 (IC50 of 100 μM) but does not significantly inhibit other serine/threonine- or tyrosine-kinases. SMI-4a exhibits anticancer activity.
- Potent, selective, cell-permeable, and ATP-competitive Pim-1 inhibitor.
- Inhibits Pim-2.
- Has anticancer activity.
- Attenuates the autophosphorylation of tagged Pim-1 in intact cells at 0.5 μM.
- Causes a dose-dependent reduction in Pim-1-induced 4E-BP1 phosphorylation, with an IC50 of approximately 125 nM in HEK-293T cells.