BP-1-102 binds to Stat3 with an affinity KD of 504 nM. BP-1-102 inhibits Stat3 DNA-binding activity in vitro, with an IC50 value of 6.8±0.8 μM. It blocks Stat3-phospho-tyrosine peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and KLF-8[1].
BP-1-102 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
147EF cells
0.1-1 μM
Function assay
3 h
Inhibition of AKT phosphorylation in human 147EF cells at 0.1 to 1 uM after 3 hrs by Western blotting analysis
24900612
30M cells
Cytotoxicity assay
3 days
Cytotoxicity against human 30M cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=2 μM
24900612
DU145 cells
Cytotoxicity assay
72 h
Cytotoxicity against human DU145 cells after 72 hrs by MTS assay, EC50=22.7 μM
21788134
JJN-3 cells
Cytotoxicity assay
72 h
Cytotoxicity against human JJN-3 cells after 72 hrs by MTS assay, EC50=16.7 μM
21788134
BP-1-102 动物研究
Animal study
BP-1-102 is orally bioavailable and accumulates in tumor tissues at concentrations that are adequate to impede the functions of abnormally active Stat3 and to inhibit tumor growth[1]. Mice treated with BP-1-102, which is orally bioavailable and targets the activation and interaction of STAT3/NF-kB, show a decrease in colon tumor development and a lower expression of cytokines that activate STAT3/NF-kB in tumor tissues[2].
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