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SH5-07

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Chemical Structure| 1456632-41-9 同义名 : -
CAS号 : 1456632-41-9
货号 : A427567
分子式 : C29H28F5N3O5S
纯度 : 97%
分子量 : 625.607
MDL号 : MFCD30718177
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(79.92 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：
生物活性
靶点

  • STAT3
描述 The signal transducer and activator of transcription (STAT) proteins mediate cytokine and growth factor responses, including promoting cell growth and differentiation, and immune responses[1]. STAT3 is a central transcription factor that is activated by phosphorylation of a conserved tyrosine residue (Tyr705) in response to extracellular cytokines and growth factors and is an attractive target for anticancer drug discovery[2]. SH5-07 is an inhibitor of STAT3 with IC50 of 3.9 ± 0.6 μM[3]. 72-h treatment with SH5-07 of cultured tumor cells harboring variable Stat3 activities inhibited viability to different degrees, with IC50 of 1.0-2.7 μM for glioma U251MG and U87MG cells (most sensitive), 3.8-4.5 μM for breast cancer, MDA-MB-231 (231) cells, 3.8-7.4 μM for glioma, U373MG and SF295 cells, 5.3-5.8 μM for DU145 prostate cancer cells, 4.1-9.2 μM for NIH3T3/v-Src (vSrc), and 9.6-10.3 μM for the least sensitive human pancreatic cancer, Panc-1 cells[3]. Tail vein injection of SH5-07 (5-6 mg/kg every 2-3 days) inhibited growth of 90-150 mm3 established subcutaneous mouse xenografts of human glioma (U251MG) and breast (MDA-MB-231) tumors that harbor aberrantly-active Stat3, with decreased c-Myc, Mcl-1 and Cyclin D1 expression. No significant changes in body weights, blood cell counts, or the gross anatomy of organs, or obvious signs of toxicity were observed[3].
作用机制 SH5-07 blocks STAT3 DNA binding activity.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
127EF cells Cytotoxicity assay Cytotoxicity against human 127EF cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=0.1955 μM 24900612
147EF cells Function assay 2 to 72 hrs Inhibition of STAT3 in human 147EF cells assessed as reduction of phosphorylated Bcl-xL level after 2 to 72 hrs by Western blotting analysis 24900612
25EF cells Cytotoxicity assay Cytotoxicity against human 25EF cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=1.1205 μM 24900612
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.60mL

0.32mL

0.16mL

7.99mL

1.60mL

0.80mL

15.98mL

3.20mL

1.60mL
参考文献

[1]Bromberg J, Darnell JE Jr. The role of STATs in transcriptional control and their impact on cellular function. Oncogene. 2000 May 15;19(21):2468-73. doi: 10.1038/sj.onc.1203476. PMID: 10851045.

[2]Darnell JE Jr, Kerr IM, Stark GR. Jak-STAT pathways and transcriptional activation in response to IFNs and other extracellular signaling proteins. Science. 1994 Jun 3;264(5164):1415-21. doi: 10.1126/science.8197455. PMID: 8197455.

[3]Yue P, Lopez-Tapia F, Paladino D, Li Y, Chen CH, Namanja AT, Hilliard T, Chen Y, Tius MA, Turkson J. Hydroxamic Acid and Benzoic Acid-Based STAT3 Inhibitors Suppress Human Glioma and Breast Cancer Phenotypes In Vitro and In Vivo. Cancer Res. 2016 Feb 1;76(3):652-63. doi: 10.1158/0008-5472.CAN-14-3558. Epub 2015 Jun 18. PMID: 26088127; PMCID: PMC4684502.