The response of mammalian cells to hypoxia is mediated by a family of transcription factors known as HIF (hypoxia-inducible factors). The subunits of HIF, HIF-1α can be degraded rapidly under normoxia. KC7F2 is a HIF-1α inhibitor, which can inhibit the HIF-1α biological activity with IC50 value of 20μM (measured by HIF-1–responsive promoter) under hypoxia (1% O2). Accompanied with the inhibited activity of HIF-1α, treatment with KC7F2 40μM for 24h decreased the transcription of defined HIF-1α target genes, including carbonic anhydrase IX, MMP2, endothelin1 and enolase 1 in LN229 cells. KC7F2 has cytotoxicity in MCF7, LNZ308, A549, U251MG and LN229 with IC50 of approximately 15-25μM for 72h under normoxia, but is more severe under hypoxic conditions in other cell lines, such as D54MG. KC7F2 can also reduce the protein levels of HIF-1α in cancer cell lines of different tissue origin and genetic background, including U251MG, MCF7, PC3 and LNZ308 cells, on concentration of 40μM for 8 or 24 h under hypoxia, as well as in LN229 cells dose-dependently (20-80μM for 6h) [1].
作用机制
KC7F2 inhibits HIF-1α protein synthesis with no effect on neither the mRNA transcription nor the protein degradation rate of HIF-1α. The accurate mechanism of its action is unknown, but may involve in inhibition of the phosphorylation of 4EBP1 and S6K.[1]
KC7F2 实验方案
计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
1.75mL
0.35mL
0.18mL
8.77mL
1.75mL
0.88mL
17.53mL
3.51mL
1.75mL
KC7F2 技术信息
CAS号
927822-86-4
分子式
C16H16Cl4N2O4S4
分子量
570.381
别名
运输
蓝冰
存储条件
粉末Keep in dark place,Inert atmosphere,Room temperature
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