STAT5-IN-1

Research use only, not for human use.

A selective, small molecule inhibitor of the transcription factor STAT5 with IC50 of 47±17 uM in FP assays.

A selective, small molecule inhibitor of the transcription factor STAT5 with IC50 of 47±17 uM in FP assays; shows little to no inhibition for STAT1, STAT3 and Lck (<40% inhibition at 500 uM); selectively inhibits the function of the STAT5b domain and STAT5 DNA binding in vitro, and selectively inhibits activation of STAT5 in K562 cells.

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.

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Signal Transducers and Activators of Transcription 5

JAK/STAT Signaling

STAT

STAT5β

Other Indications

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285986-31-4

293.28

C16H11N3O3

>98% (HPLC)

DMSO: ≥23.0 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(N/N=C/C1=COC2=C(C=CC=C2)C1=O)C3=CN=CC=C3

3-Pyridinecarboxylic acid, [(4-oxo-4H-1-benzopyran-3-yl)methylene]hydrazide (9CI)

(-20℃)

With Ice Pack

≥ 2 years