2,5-Dihydroxycinnamic acid phenethyl ester is an inhibitor of 5-lipoxygenase (5-LO) with an IC value of 0.33 µM for inhibition of 5-LO product synthesis in polymorphonuclear leukocytes (PMNLs) stimulated with the sarcoendoplasmic reticulum calcium ATPase (SERCA) inhibitor thapsigargin . It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals (IC = 16.41 µM) in a cell-free assay. 2,5-Dihydroxycinnamic acid phenethyl ester selectively decreases viability of RCC4 and 786-O cells lacking the Von Hippel-Lindau (VHL) tumor suppressor gene (ICs = 8 and 34.8 µM, respectively) over cells homozygously expressing VHL (ICs = 99.6 and >100 µM, respectively). However, it also decreases viability of RCC10 VHL and RCC10 VHL cells (ICs = 5.04 and 0.96 µM, respectively). It increases the levels of pro-caspase-3a, LC3B-I, and LC3B-II in RCC4 VHL cells in a concentration-dependent manner.
2,5-Dihydroxycinnamic Acid phenethyl ester , an inhibitor of 5-lipoxygenase (5-LOX) with an IC50 of 0.33 μM, inhibits 5-LOX in a dose-dependent manner . 2,5-Dihydroxycinnamic Acid phenethyl ester, reduces the cell viability of renal cancer cells and induces apoptosis, can be used for cancer research.
IC50&Target
5-LOX
0.33 μM (IC50)
体外研究
2,5-dihydroxycinnamic Acid phenyl ester (0-100 μM; 4 days) can reduce the viability of renal cancer cells and is more selective towards RCC4 and 786.0 cells lacking the Von Hippel Lindau (VHL) tumor suppressor gene.
2,5-dihydroxycinnamic Acid phenyl ester (0-10 μM; 24 hours) can increase the expression of LC3B and p62, block autophagy flux in RCC4 cells, and induce apoptosis mediated cell death by activating the caspase-3 pathway.
Cell Viability Assay
Cell Line:
RCC4, RCC10, 786.0 cells
Concentration:
0-100 μM
Incubation Time:
4 days
Result:
Reduced the cell viability of renal cancer cells and was more selective toward RCC4 and 786.0 cells which are deficient for the Von Hippel-Lindau (VHL) tumor suppressor gene.
Western Blot Analysis
Cell Line:
RCC4, RCC10, 786.0 cells
Concentration:
0-10 μM
Incubation Time:
24 hours
Result:
Increased in LC3B and p62 expression, blocked of the autophagic flux in RCC4 cells.
Stimulated in a dose ependent manner the cleavage of pro-caspase-3 only in the RCC4 cells which lack the VHL tumor suppressor.
分子式
C17H16O4
分子量
284.31
CAS号
179691-97-5
运输条件
Room temperature in continental US; may vary elsewhere.