SMI-4a (438190-29-5) is a selective, ATP-competitive inhibitor of the Pim protein kinases (IC50 = 24 and 100 nM for Pim-1 and Pim-2 respectively). Selective over a panel of ~50 other kinases.1 Induces cell cycle arrest in leukemia and prostate cancer cells.2 Blocks the growth of a wide range of myeloid and lymphoid cell lines with precursor T-cell lymphoblastic leukemia/lymphoma (pre-T-LBL/T-ALL) being highly sensitive.3 SMI-4a is a useful tool for exploring the involvement of Pim in cellular signaling.4 Cell permeable.
1) Xia et al. (2009), Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases; J. Med. Chem., 52 74
2) Beharry et al. (2009), Novel benzylidene-thiazolidine-2,4-diones inhibit Pim protein kinase activity and induce cell cycle arrest in leukemia and prostate cancer cells; Mol. Cancer Ther., 8 1473
3) Lin et al. (2010), A small molecule inhibitor of Pim protein kinases blocks the growth of precursor T-cell lymphoblastic leukemia/lymphoma; Blood, 115 824
4) Zhang et al. (2009), PIM1 protein kinase regulates PRAS40 phosphorylation and mTOR activity in FDCP1 cells; Cancer Biol. Ther., 8 846