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SH-4-54

Catalog No.
B4789
STAT inhibitor, potent
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$185.00
In stock
5mg
$130.00
In stock
25mg
$340.00
In stock
100mg
$690.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

SH-4-54 is a potent inhibitor of STAT3 with KD values of 300 and 464 nM for STAT3 and STAT5, respectively [1].

STAT3 is a transcription factor that belongs to the STAT transcription factor family. STAT3 signaling plays an important role in the survival and proliferation of brain tumor stem cells (BTSCs) and glioblastoma (GBM) [1].

SH-4-54 is a potent STAT inhibitor. SH-4-54 inhibited interactions between STAT3 and phosphopeptide with Ki value of 10-30 μM. SH-4-54 exhibited selectivity for STAT3 against STAT1 by >10-fold. SH-4-54 inhibited pSTAT3 (Y705) in a concentration-dependent way with no effect on pSTAT3 (S727), suggesting that SH-4-54 bound to the STAT3 SH2 domain. Also, SH-4-54 reduced pSTAT3 levels and inhibited the downstream targets Cyclin D1 and Bcl-xL, which were involved in cell growth and survival [1].

In mice, intraperitoneal injection of SH-4-54 (10 mg/kg) caused a concentration of 700 nM after 30 min in the brain. In NOD-SCID mice xenografted with 105 BT73 glioma cells, SH-4-54 (10 mg/kg) reduced tumor cells and pSTAT3 expression. Also, SH-4-54 inhibited proliferation and induced apoptosis [1].

Reference:
[1].  Haftchenary S, Luchman HA, Jouk AO, et al. Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma. ACS Med Chem Lett, 2013, 4(11): 1102-1107.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at -20°C
M.Wt610.59
Cas No.1456632-40-8
FormulaC29H27F5N2O5
Solubility≥20.25mg/mL in DMSO
SDFDownload SDF
Canonical SMILESFC(C(S(=O)(N(C)CC(N(C1=CC=C(C(O)=O)C=C1)CC2=CC=C(C=C2)C3CCCCC3)=O)=O)=C(C(F)=C4F)F)=C4F
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control