SH-4-54 demonstrates remarkable effectiveness in killing glioblastoma brain cancer stem cells (BTSCs) by strongly inhibiting STAT3 phosphorylation and its downstream transcriptional activities at low nanomolar concentrations. Exhibiting significant cytotoxicity against human BTSCs while sparing human fetal astrocytes, SH-4-54 effectively inhibits pSTAT3 with nanomolar IC50s, showing specific action without detectable off-target effects at therapeutic levels[1].
SH-4-54 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
human 127EF cells
Cytotoxic assay
3 days
Cytotoxicity against human 127EF cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=66 nM
24900612
human 147EF cells
Function assay
2-72 h
Inhibition of STAT3 in human 147EF cells assessed as reduction of phosphorylated cyclin D1 level after 2 to 72 hrs by Western blotting analysis
24900612
human 25EF cells
Cytotoxic assay
3 days
Cytotoxicity against human 25EF cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=0.234 μM
24900612
human 30M cells
Cytotoxic assay
3 days
Cytotoxicity against human 30M cells assessed as cell viability after 3 days by Alamar Blue assay, EC50=0.1 μM
24900612
SH-4-54 动物研究
Animal study
SH-4-54 penetrates the blood-brain barrier to significantly reduce glioma growth and pSTAT3 in vivo, underscoring the potential of STAT3 inhibitors in treating BTSCs and endorsing the use of a STAT3 inhibitor in glioblastoma multiforme (GBM) clinical settings. SH-4-54 reduces pSTAT3 in tumor cells and seems to lessen tumor proliferation while enhancing apoptosis in treated mice[1].
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