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Country: China (Mainland)
Business Type:Lab/Research institutions
SH-4-54 is a most potent, small molecule, nonphosphorylated STAT3 inhibitor, strongly binds to STAT3 protein (KD = 300 nM), is selective for STAT3 over STAT1. IC50 value: 300 nM (KD, for STAT3) Target: STAT3 in vitro: SH-4-54 potently kills glioblastoma brain cancer stem cells (BTSCs) and effectively suppresses STAT3 phosphorylation and its downstream transcriptional targets at low nM concentrations.SH-4-54 shows unprecedented cytotoxicity in human BTSCs, displayed no toxicity in human fetal astrocytes, potently suppressed pSTAT3 with nanomolar IC50s, inhibited STAT3's downstream targets, and showed no discernible off-target effects at therapeutic doses. in vivo: SH-4-54 exhibits blood-brain barrier permeability, potently controlled glioma tumor growth, and inhibited pSTAT3 in vivo. SH-4-54 demonstrates the power of STAT3 inhibitors for the treatment of BTSCs and validates the therapeutic efficacy of a STAT3 inhibitor for GBM clinical application.SH-4-54 decreases pSTAT3 expression in tumor cells of treated mice. SH-4-54 appears to decrease proliferation and increase apoptosis of treated tumors.