Table 1.
PIM kinase inhibitors.
| Name of Inhibitors | Class | IC50 or Ki | Preclinical or Clinical Studies |
|---|---|---|---|
| INCB053914 | Adenosine triphosphate(ATP)-competitive inhibitor | PIM1: 0.24 nM PIM2: 30 nM PIM3: 0.12 nM |
Preclinical [22] |
| LGB321 | 3-S-aminopiperidine pyridyl carboxamide | PIM1: 0.001 nM PIM2: 0.002 nM PIM3: 0.0008 nM |
Preclinical [62] |
| LGH447 (PIM447) |
3-S-aminopiperidine pyridyl carboxamide | PIM1: 5.8 pM PIM2: 18 pM PIM3: 9.3 pM |
Phase I/II [63,64] |
| SGI-1776 | Imidazopyridine | PIM1: 7 nM PIM2: 363 nM PIM3: 69 nM |
Phase I [65] |
| IBL-202 | Inhibitor of the PI3 kinases | NA | Preclinical [66,67] |
| SEL24-B489 | FLT3-ITD inhibitor | PIM: 2 nM PIM2: 2 nM PIM3: 3 nM |
Phase I/II [68] |
| AZD1897 | Thiazolidine | PIM1: 3 nM PIM2: 3 nM PIM3: 3 nM |
Preclinical [69] |
| AZD1208 | Thiazolidine | PIM: 0.4 nM PIM2: 5 nM PIM3: 1.9 nM |
Phase I (terminated) [70] |
| JP11646 | Non-ATP competitive inhibitor | PIM1: 24 nM PIM2: 0.5 nM PIM3: 1 nM |
Preclinical [71] |
| GDC-0339 (Compound 16) |
Diaminopyrazole | PIM1: 0.03 nM PIM2: 0.1 nM PIM3: 0.02 nM |
Preclinical [72,73] |
| SMI-4a | benzylidene-thiazolidene-2,4-dione | PIM1: 21 nM PIM2: 100 nM |
Preclinical [74] |