Name: SH-4-54
Price: 356.00 USD

- Overview
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    Background
    
    SH-4-54 is a potent inhibitor of STAT3 with KD values of 300 and 464 nM for STAT3 and STAT5, respectively [1].
    STAT3 is a transcription factor that belongs to the STAT transcription factor family. STAT3 signaling plays an important role in the survival and proliferation of brain tumor stem cells (BTSCs) and glioblastoma (GBM) [1].
    SH-4-54 is a potent STAT inhibitor. SH-4-54 inhibited interactions between STAT3 and phosphopeptide with Ki value of 10-30 μM. SH-4-54 exhibited selectivity for STAT3 against STAT1 by >10-fold. SH-4-54 inhibited pSTAT3 (Y705) in a concentration-dependent way with no effect on pSTAT3 (S727), suggesting that SH-4-54 bound to the STAT3 SH2 domain. Also, SH-4-54 reduced pSTAT3 levels and inhibited the downstream targets Cyclin D1 and Bcl-xL, which were involved in cell growth and survival [1].
    In mice, intraperitoneal injection of SH-4-54 (10 mg/kg) caused a concentration of 700 nM after 30 min in the brain. In NOD-SCID mice xenografted with 105 BT73 glioma cells, SH-4-54 (10 mg/kg) reduced tumor cells and pSTAT3 expression. Also, SH-4-54 inhibited proliferation and induced apoptosis [1].
- Properties
  - CAS Number
    
    1456632-40-8
    
    Molecular Formula
    
    C29H27F5N2O5S
    
    Molecular Weight
    
    610.59
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥20.25 mg/mL in DMSO; ≥24.2 mg/mL in EtOH
    
    Storage
    
    Desiccate at -20°C
    
    * For Research Use Only
- Reference
  - 1. Memarzadeh K, Savage DJ, et al. "Low UBE4B expression increases sensitivity of chemoresistant neuroblastoma cells to EGFR and STAT5 inhibition." Cancer Biol Ther. 2019 Sep 1:1-14. PMID:31475882
    2. Litvinchuk A, Wan YW, et al. "Complement C3aR Inactivation Attenuates Tau Pathology and Reverses an Immune Network Deregulated in Tauopathy Models and Alzheimer's Disease." Neuron. 2018 Dec 19;100(6):1337-1353.e5. PMID:30415998

SH-4-54

SH-4-54

Background

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