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Pim-1/2 kinase inhibitor 2 (compound 5b) is a competitive PIM-1 and PIM-2 kinase inhibitor with IC50s of 1.31 μM and 0.67 μM, respectively. Pim-1/2 kinase inhibitor 2 shows in-vitro low cytotoxicity against normal human lung fibroblast Wi-38 cell line and potent in-vitro anticancer activity against myeloid leukaemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2) cancer cell lines[1]. | [IC 50]
PIM1: 1.31 μM (IC50); PIM2: 0.67 μM (IC50) | [References]
[1] Mostafa M M El-Miligy, et al. Discovery of new pyridine-quinoline hybrids as competitive and non-competitive PIM-1 kinase inhibitors with apoptosis induction and caspase 3/7 activation capabilities. J Enzyme Inhib Med Chem. 2023 Dec;38(1):2152810. DOI:10.1080/14756366.2022.2152810 |
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