CAS No. : 285986-31-4
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|Cat. No. :||CS-6859|
|CAS No. :||285986-31-4|
|M. Wt. :||293.28|
|Solubility:||DMSO: ≥23.0 mg/mL|
STAT5-IN-1 is a STAT5 inhibitor with an IC50 of 47 μM for STAT5β isoform. IC50 & Target: IC50: 47 μM (STAT5β) In Vitro: The signal transducer and activator of transcription 5 (STAT5) is a member of the STAT family of proteins, implicated in cell growth and differentiation. STAT5-IN-1 inhibits STAT5 by binding to the SH2 domain. The functions of the SH2 domains of STAT3, STAT1, and of the tyrosine kinase Lck are inhibited to a lesser extent (IC50>500 µM). STAT5-IN-1 block STAT5/STAT5 DNA binding in K562 nuclear extracts. Substitution of the hydrogen at C6 of the chromone ring by an ethyl group does not affect activity of STAT5-IN-1 against STAT5β, but leads to complete loss of selectivity against other STAT family members.
Müller J, et al. Discovery of chromone-based inhibitors of the transcription factor STAT5. Chembiochem. 2008 Mar 25;9(5):723-7.
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