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SH-4-54

CAS No. : 1456632-40-8

產(chǎn)品活性：SH-4-54 is a STAT inhibitor that binds to STAT3 and STAT5 with K_Ds of 300, 464 nM, respectively.

研究領(lǐng)域：JAK/STAT Signaling  |  Stem Cell/Wnt

作用靶點：STAT

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, displays no toxicity in human fetal astrocytes, potently suppresses pSTAT3 with nanomolar IC₅₀s, inhibiting STAT3's downstream targets, and shows no discernible off-target effects at therapeutic doses.

In Vivo: SH-4-54 exhibits blood-brain barrier permeability potently controls glioma tumor growth, and inhibits 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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