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MedChemExpress - Model SH-4-54 - 1456632-40-8
SH-4-54 is a STAT inhibitor that binds to STAT3 and STAT5 with KDs of 300, 464 nM, respectively.MCE products for research use only. We do not sell to patients.
SH-4-54
MCE China:SH-4-54
Brand:MedChemExpress (MCE)
Cat. No.HY-16975
CAS:1456632-40-8
Purity:99.45%
Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Shipping:Room temperature in continental US; may vary elsewhere.
Description:SH-4-54 is a STAT inhibitor that binds to STAT3 and STAT5 with KDs of 300, 464 nM, respectively.
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[1].
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[1].
IC50 & Target:STAT3 300 nM (Kd) STAT5 464 nM (Kd)
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References:
[1]. Haftchenary S, et al. Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma. ACS Med Chem Lett. 2013 Sep 8;4(11):1102-1107. [Content Brief]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world;
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas;
• The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects;
• Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services;
• It has a professional experimental center and strict quality control and verification system;
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products;
• The biological activity of the products has been verified by the experiments of customers in various countries;
• A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers;
• Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world;
• It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。