Pim

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. Phase 1.

SIM-4a is a Pim kinase inhibitor that blocks mTORC1 activity via activation of AMPK. Mostly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases.

TCS PIM-1 4a is a selective and ATP-competitive Pim kinase inhibitor (IC50 values = 24 and 100 nM for Pim-1 and Pim-2, respectively).

CX-6258 is a potent, selective, and orally efficacious pan-Pim kinases inhibitor.

AZD1208 is orally available, small molecule inhibitor of PIM kinases with potential antineoplastic activity.

Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC50 of 2.71 μM.

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.

CX-6258 hydrochloride hydrate is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.

AZD1208 hydrochloride is a novel, orally bioavailable, highly selective PIM kinases inhibitor.

SMI-16a is a selective Pim kinase inhibitor with IC50 values of 0.15, 0.02 and 48 μM for Pim1, Pim2 and PC3 cells, respectively.

TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.