| S8005 |
SMI-4a |
SMI-4a (TCS PIM-1 4a) is a potent inhibitor of Pim1 with IC50 of 17 nM, modestly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases. |
Selective |
Pim1, IC50: 17 nM |
| S1050 |
TCS PIM-1 1 |
TCS PIM-1 1 (SC 204330) is a potent and selective inhibitor of ATP-competitive Pim-1 kianse with IC50 of 50 nM, shows good selectivity over Pim-2 and MEK1/MEK2 with IC50 > 20000 nM. |
Selective |
Pim1, IC50: 50 nM |
| S3296 |
Hispidulin |
Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway. |
Selective |
Pim-1, IC50: 2.71 μM |
| S7985 |
PIM447 (LGH447) |
PIM447 (LGH447) is a novel pan-PIM kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>105-fold differential relative to the Ki on PIMs). PIM447 induces apoptosis. |
Pan |
Pim1, Ki: 6 pM |
| S7104 |
AZD1208 |
AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1. |
Pan |
Pim1, IC50: 0.4 nM |
| S7041 |
CX-6258 HCl |
CX-6258 HCl is a potent, orally efficacious pan-Pim kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively.
|
Pan |
Pim1, IC50: 5 nM |
| S6774 |
TP-3654 |
TP-3654 is the second-generation PIM inhibitor with Ki values of 5 nM, 239 nM, and 42 nM for PIM-1, PIM-2 and PIM-3, respectively. |
Pan |
Pim1, Ki: 5 nM |
| S2198 |
SGI-1776 free base |
SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. SGI-1776 induces apoptosis and autophagy. |
Pan |
Pim1, IC50: 7 nM |
| S6497 |
SMI-16a |
SMI-16a is a selective Pim kinase inhibitor with IC50 values of 150 nM and 20 nM for Pim1 and Pim2 respectively. |
Pan |
Pim1, IC50: 150 nM |
