STAT3-IN-32 is a potent inhibitor of dual phosphorylation of STAT3, targeting the SH2 domain with a dissociation constant (KD) of 21.3 nM. It effectively inhibits STAT3 phosphorylation at tyrosine 705 and serine 727, leading to the disruption of nuclear transcription and mitochondrial oxidative phosphorylation functions. In cellular assays, STAT3-IN-32 demonstrates an IC50 of 5.3 nM for STAT3 luciferase activity in HEK293T cells and 4.2 nM for ATP production inhibition in BxPC-3 cells. Additionally, STAT3-IN-32 exhibits significant anti-tumor effects in pancreatic cancer xenograft models, making it a valuable compound for cancer research.
STAT3-IN-32 is a potent inhibitor of dual phosphorylation of STAT3, targeting the SH2 domain with a dissociation constant (KD) of 21.3 nM. It effectively inhibits STAT3 phosphorylation at tyrosine 705 and serine 727, leading to the disruption of nuclear transcription and mitochondrial oxidative phosphorylation functions. In cellular assays, STAT3-IN-32 demonstrates an IC50 of 5.3 nM for STAT3 luciferase activity in HEK293T cells and 4.2 nM for ATP production inhibition in BxPC-3 cells. Additionally, STAT3-IN-32 exhibits significant anti-tumor effects in pancreatic cancer xenograft models, making it a valuable compound for cancer research.
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