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SH-4-54
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SH-4-54图片
CAS NO:1456632-40-8
规格:98%
分子量:610.59
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
STAT inhibitor, potent
CAS:1456632-40-8
分子式:C29H27F5N2O5S
分子量:610.59
纯度:98%
存储:Store at -20°C

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.