z-smi-4a

Description: (Z)-SMI-4a (the Z-enantiomer of SMI-4a), a novel benzylidene-thiazolidine-2, 4-dione small molecule, is a potent and selective Pim1 inhibitor with potential antineoplastic activity. It inhibits Pim1 with an IC50 of 17 nM, it is modestly potent to Pim-2, and does not significantly inhibit any other serine/threonine- or tyrosine-kinases. SMI-4a blocks the growth of precursor T-cell lymphoblastic leukemia/lymphoma. SMI-4a was found to induce phosphorylation of extracellular signal-related kinase1/2 (ERK1/2). The serine/threonine Pim kinases are up-regulated in specific hematologic neoplasms, and play an important role in key signal transduction pathways, including those regulated by MYC, MYCN, FLT3-ITD, BCR-ABL, HOXA9, and EWS fusions. SMI-4a kills a wide range of both myeloid and lymphoid cell lines with precursor T-cell lymphoblastic leukemia/lymphoma (pre-T-LBL/T-ALL) being highly sensitive.

References: Mol Cancer Ther. 2009 Jun; 8(6):1473-83; Blood. 2010 Jan 28; 115(4):824-33.

Related CAS: 327033-36-3 (TCS-PIM-1-4a, E and Z-enantiomers)

TCS PIM-1 4a; SMI-4a; SMI4a; SMI 4a

Chemical Name: 5-(3-(trifluoromethyl)benzylidene)thiazolidine-2, 4-dione

InChi Key: NGJLOFCOEOHFKQ-VMPITWQZSA-N

InChi Code: InChI=1S/C11H6F3NO2S/c12-11(13, 14)7-3-1-2-6(4-7)5-8-9(16)15-10(17)18-8/h1-5H, (H, 15, 16, 17)/b8-5+