【CAS号】 1456632-40-8

【目录编号】 2H-43

【纯度】 >98%

【分子式】 C29H27F5N2O5S

【分子量】 610.59

【简介】 SH-4-54是一种高效的STAT抑制剂,其作用STAT3和STAT5的KD分别为300 nM和464 nM。

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SH-4-54 详细介绍

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.

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