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抑制剂/激动剂
囊泡 肿瘤
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JAK-STAT-Signaling 外泌体 帕金森与阿尔茨海默症 肿瘤干细胞 PPARs
/ STAT / SH-4-54

SH-4-54 {[allProObj[0].p_purity_real_show]}

货号：A627552

SH-4-54 is a potent, small molecule, nonphosphorylated STAT3 inhibitor with KD of 300 nM and 464 nM for STAT3 and STAT5, respectively.

SH-4-54 化学结构 CAS号：1456632-40-8
SH-4-54 化学结构
CAS号：1456632-40-8
SH-4-54 3D分子结构
CAS号：1456632-40-8
SH-4-54 化学结构 CAS号：1456632-40-8
SH-4-54 3D分子结构 CAS号：1456632-40-8
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SH-4-54 纯度/质量文件 产品仅供科研

货号：A627552 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 STAT1 ↓ STAT3 ↓ STAT5 ↓ 其他靶点 纯度
Nifuroxazide ✔ 98%
Fludarabine ✔ 98%
Artesunate ✔ 98%
BP-1-102 +++

STAT3, Kd: 504 nM

 		99%+
Niclosamide ++

STAT3, IC50: 0.7 μM

 		98%
Napabucasin ✔ 98%
Cryptotanshinone ++

STAT3, IC50: 4.6 μM

 		98%
Stattic +

STAT3, IC50: 5.1 μM

 		98%
NSC 74859 +

STAT3, IC50: 86 μM

 		99%+
Ochromycinone ✔ 98%
HO-3867 ✔ 97%
C188-9 ++++

STAT3, Kd: 4.7 nM

 		99%+
HJC0152 ✔ 98%
SH5-07 ✔ 97%
SH-4-54 ++++

STAT3, Kd: 300 nM

 		+++

STAT5, Kd: 464 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

SH-4-54 生物活性

靶点

  • STAT3

    STAT3, Kd:300 nM

  • STAT5

    STAT5, Kd:464 nM
描述 SH-4-54 demonstrates remarkable effectiveness in killing glioblastoma brain cancer stem cells (BTSCs) by strongly inhibiting STAT3 phosphorylation and its downstream transcriptional activities at low nanomolar concentrations. Exhibiting significant cytotoxicity against human BTSCs while sparing human fetal astrocytes, SH-4-54 effectively inhibits pSTAT3 with nanomolar IC50s, showing specific action without detectable off-target effects at therapeutic levels[1].
体内研究

SH-4-54 penetrates the blood-brain barrier to significantly reduce glioma growth and pSTAT3 in vivo, underscoring the potential of STAT3 inhibitors in treating BTSCs and endorsing the use of a STAT3 inhibitor in glioblastoma multiforme (GBM) clinical settings. SH-4-54 reduces pSTAT3 in tumor cells and seems to lessen tumor proliferation while enhancing apoptosis in treated mice[1].
体外研究

SH-4-54 demonstrates remarkable effectiveness in killing glioblastoma brain cancer stem cells (BTSCs) by strongly inhibiting STAT3 phosphorylation and its downstream transcriptional activities at low nanomolar concentrations. Exhibiting significant cytotoxicity against human BTSCs while sparing human fetal astrocytes, SH-4-54 effectively inhibits pSTAT3 with nanomolar IC50s, showing specific action without detectable off-target effects at therapeutic levels[1].

SH-4-54 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
human 127EF cells Cytotoxic assay 3 days Cytotoxicity against human 127EF cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=66 nM 24900612
human 147EF cells Function assay 2-72 h Inhibition of STAT3 in human 147EF cells assessed as reduction of phosphorylated cyclin D1 level after 2 to 72 hrs by Western blotting analysis 24900612
human 25EF cells Cytotoxic assay 3 days Cytotoxicity against human 25EF cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=0.234 μM 24900612
human 30M cells Cytotoxic assay 3 days Cytotoxicity against human 30M cells assessed as cell viability after 3 days by Alamar Blue assay, EC50=0.1 μM 24900612

SH-4-54 动物研究

Dose Mice: 3 mg/kg - 6 mg/kg[3] (p.o.); 10 mg/kg[4] (i.v.), 20 mg/kg[4] (i.p.)
Administration p.o., i.v., i.p.

SH-4-54 参考文献

[1]Haftchenary S, et al. Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma. ACS Med Chem Lett. 2013 Sep 8;4(11):1102-1107.

SH-4-54 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.64mL

0.33mL

0.16mL

8.19mL

1.64mL

0.82mL

16.38mL

3.28mL

1.64mL

SH-4-54 技术信息

CAS号1456632-40-8
分子式C29H27F5N2O5S
分子量 610.592
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 105 mg/mL(171.96 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: SH-4-54 | 1456632-40-8 | STAT3/5 Inhibitor | JAK/STAT Signaling | Stem Cell/Wnt | STAT | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | SH-4-54 纯度/质量文件 | SH-4-54 亚型比较 | SH-4-54 生物活性 | SH-4-54 细胞研究 | SH-4-54 动物研究 | SH-4-54 参考文献 | SH-4-54 实验方案 | SH-4-54 技术信息

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