Pim-1 kinase inhibitor 2 is a PIM-1 kinase inhibitor with a human IC50 of 0.63 μM. Pim-1 kinase inhibitor 2 exhibits high selectivity for cancer cells over normal cells. Pim-1 kinase inhibitor 2 induces apoptosis, increases active caspase-3 levels, upregulates BAX, downregulates Bcl-2, and elevates the Bax/Bcl-2 ratio. Pim-1 kinase inhibitor 2 suppresses cancer cell proliferation and induces cell cycle arrest. Pim-1 kinase inhibitor 2 can be used for the research of prostate carcinoma, hepatocellular carcinoma, and breast adenocarcinoma [1].
In Vitro, Pim-1 kinase inhibitor 2 (compound 13) (24 h) potently inhibits proliferation of PC3, HepG2, and MCF-7 cancer cells with IC50 values of 4.82 μM, 5.19 μM, and 16.33 μM respectively, and exhibits high selectivity for cancer cells over normal WI-38 cells[1]. Pim-1 kinase inhibitor 2 potently inhibits PIM-1 kinase with an IC50 of 0.63 μM and 76.43% inhibition at 10 μM[1]. Pim-1 kinase inhibitor 2 (1.96 μM; 24 h) induces G2/M phase arrest and increases apoptotic Pre-G1 phase population in PC3 cells[1]. Pim-1 kinase inhibitor 2 (1.96 μM; 24 h) induces apoptosis in PC3 cells, with 19.64% total apoptotic cells[1]. Pim-1 kinase inhibitor 2 increases active caspase-3 levels in PC3 cells to 352.9 Pg/mL, indicating induction of apoptosis[1]. Pim-1 kinase inhibitor 2 (24 h) upregulates BAX, downregulates Bcl-2, and increases the BAX/Bcl-2 ratio to 115.65 in PC3 cells, promoting apoptosis[1].
References:
[1]. Farrag AM, et al. New cyanopyridine-based scaffold as PIM-1 inhibitors and apoptotic inducers: Synthesis and SARs study. Bioorg Chem. 2020;105:104378.
In Vitro, Pim-1 kinase inhibitor 2 (compound 13) (24 h) potently inhibits proliferation of PC3, HepG2, and MCF-7 cancer cells with IC50 values of 4.82 μM, 5.19 μM, and 16.33 μM respectively, and exhibits high selectivity for cancer cells over normal WI-38 cells[1]. Pim-1 kinase inhibitor 2 potently inhibits PIM-1 kinase with an IC50 of 0.63 μM and 76.43% inhibition at 10 μM[1]. Pim-1 kinase inhibitor 2 (1.96 μM; 24 h) induces G2/M phase arrest and increases apoptotic Pre-G1 phase population in PC3 cells[1]. Pim-1 kinase inhibitor 2 (1.96 μM; 24 h) induces apoptosis in PC3 cells, with 19.64% total apoptotic cells[1]. Pim-1 kinase inhibitor 2 increases active caspase-3 levels in PC3 cells to 352.9 Pg/mL, indicating induction of apoptosis[1]. Pim-1 kinase inhibitor 2 (24 h) upregulates BAX, downregulates Bcl-2, and increases the BAX/Bcl-2 ratio to 115.65 in PC3 cells, promoting apoptosis[1].
References:
[1]. Farrag AM, et al. New cyanopyridine-based scaffold as PIM-1 inhibitors and apoptotic inducers: Synthesis and SARs study. Bioorg Chem. 2020;105:104378.