STAT5-IN-1( Signal Transducers and Activators of Transcription 5 )

Catalog No. M13870 CAS No. 285986-31-4

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Product Name

STAT5-IN-1
Note

Research use only, not for human use.
Brief Description

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

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.
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.
In Vivo

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Synonyms

Signal Transducers and Activators of Transcription 5
Pathway

JAK/STAT Signaling
Target

STAT
Recptor

STAT5β
Research Area

Other Indications
Indication

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CAS Number

285986-31-4
Formula Weight

293.28
Molecular Formula

C16H11N3O3
Purity

>98% (HPLC)
Solubility

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

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

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

1. Müller J, et al. Chembiochem. 2008 Mar 25; 9(5):723-7.

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