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STAT5-IN-1

Names

[ CAS No. ]:
285986-31-4

[ Name ]:
STAT5-IN-1

[Synonym ]:
N'-[(E)-(4-Oxo-4H-chromen-3-yl)methylene]nicotinohydrazide
N'3-[(4-oxo-4H-chromen-3-yl)methylidene]pyridine-3-carbohydrazide
3-Pyridinecarboxylic acid, 2-[(1E)-(4-oxo-4H-1-benzopyran-3-yl)methylene]hydrazide
Stat5 Inhibitor
STAT5-IN-1

Biological Activity

[Description]:

STAT5-IN-1 is a STAT5 inhibitor with an IC50 of 47 μM for STAT5β isoform.

[Related Catalog]:

Signaling Pathways >> JAK/STAT Signaling >> STAT
Signaling Pathways >> Stem Cell/Wnt >> STAT
Research Areas >> Cancer

[Target]

STAT5β:47 μM (IC50)


[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[1].

[References]

[1]. Müller J, et al. Discovery of chromone-based inhibitors of the transcription factor STAT5. Chembiochem. 2008 Mar 25;9(5):723-7.


[Related Small Molecules]

Tyrphostin B42 (AG-490) | Stattic | AS1517499 | S3I-201 | Cryptotanshinone | Napabucasin | Homoharringtonine | WP1066 | Niclosamide | BP-1-102 | Scutellarin | SH-4-54 | HO-3867 | Artesunate | Cucurbitacin I

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C16H11N3O3

[ Molecular Weight ]:
293.277

[ Exact Mass ]:
293.080048

[ LogP ]:
1.76

[ Index of Refraction ]:
1.657

[ Storage condition ]:
2-8℃

Related Compounds