| In Vitro |
EC359 (0-100 nM; 3 days; BT-549, SUM-159, MDA-MB-231, MDA-MB-468, and HCC1806 cells) treatment reduces cell viability in a dose-dependent manner[1]. EC359 (20 nM, 25 nM; 72 hours; MDA-MB-231 and BT-549 cells) treatment significantly increases caspase-3/7 activity and Annexin V-positive cells in both MDAMB-231 and BT-549 cells. EC359 exhibits significant inhibitory activity on invasion and promotes apoptosis of TNBC cells[1]. EC359 (100 nM; 12 hours; BT549 cells) treatment significantly reduces the expression of several (such as STAT1 TGFB1, JUNB, MCL-1, etc) known STAT3 target genes[1]. EC359(100 nM; 1 hour; MDA-MB-231 and BT-549 cells) treatment substantially reduces the LIF activation of STAT3, also reduces the STAT3 activation by OSM and CNTF. EC359 treatment substantially decreases the phosphorylation of AKT, mTOR, S6, and ERK1/2 in MDA-MB231 and BT-549 cells. EC359 treatment also increases the phosphorylation of proapoptotic p38MAPK in BT549 cells[1]. Cell Viability Assay[1] Cell Line: BT-549, SUM-159, MDA-MB-231, MDA-MB-468, and HCC1806 cells Concentration: 0 nM, 1.5 nM, 12.5 nM, 25 nM, 50 nM, 100 nM Incubation Time: 3 days Result: Reduced cell viability in a dose-dependent manner. Apoptosis Analysis[1] Cell Line: MDA-MB-231 and BT-549 cells Concentration: 20 nM, 25 nM Incubation Time: 72 hours Result: Promoted apoptosis of TNBC cells. RT-PCR[1] Cell Line: BT549 cells Concentration: 100 nM Incubation Time: 12 hours Result: Reduced the expression of several known STAT3 target genes. Western Blot Analysis[1] Cell Line: MDA-MB-231 and BT-549 cells Concentration: 100 nM Incubation Time: 1 hour Result: Substantially reduced the LIF activation of STAT3, reduced the STAT3 activation by OSM and CNTF, decreased the phosphorylation of AKT, mTOR, S6, and ERK1/2 in both BT-549 and MDA-MB-231 cells and increased the phosphorylation of proapoptotic p38MAPK in BT549 cells.
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