SMI-4a
PIM1 inhibitor / 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 kinases1. Induces cell cycle arrest in leukemia and prostate cancer cells2. 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 sensitive3. A useful tool for exploring the involvement of Pim in cellular signaling4. Cell permeable.
Biochemicals & reagents
438190-29-5
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
-20°C
TARGET: Kinase -- PATHWAY: Cell cycle; Transcription -- DISEASE AREA: Cancer