STAT5-IN-1

285986-31-4

C16H11N3O3

DMSO : 20 mg/mL (68.19 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

JAK/STAT Signaling; Stem Cell/Wnt

STAT5-IN-1 is a STAT5 inhibitor with an IC₅₀ of 47 uM for STAT5beta isoform. IC50 & Target: IC50: 47 uM (STAT5beta)^[1] 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 uM). 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 STAT5beta, but leads to complete loss of selectivity against other STAT family members^[1].