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2,5-Dihydroxycinnamic Acid phenethyl ester Sale

目录号 : GC46057

An inhibitor of 5-LO

2,5-Dihydroxycinnamic Acid phenethyl ester Chemical Structure

Cas No.:179691-97-5

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1mg
¥599.00
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5mg
¥2,399.00
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10mg
¥4,196.00
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25mg
¥9,747.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

2,5-Dihydroxycinnamic acid phenethyl ester is an inhibitor of 5-lipoxygenase (5-LO) with an IC50 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 .1 It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals (IC50 = 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 (IC50s = 8 and 34.8 μM, respectively) over cells homozygously expressing VHL (IC50s = 99.6 and >100 μM, respectively). However, it also decreases viability of RCC10 VHL-/- and RCC10 VHL+/+ cells (IC50s = 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.

|1. Selka, A., Doiron, J.A., Lyons, P.A., et al. Discovery of a novel 2,5-dihydroxycinnamic acid-based 5-lipoxygenase inhibitor that induces apoptosis and may impair autophagic flux in RCC4 renal cancer cells. Eur. J. Med. Chem. 179, 347-357 (2019).

Chemical Properties

Cas No. 179691-97-5 SDF
Canonical SMILES O=C(OCCC1=CC=CC=C1)/C=C/C2=CC(O)=CC=C2O
分子式 C17H16O4 分子量 284.3
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml 储存条件 Store at -20°C
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1 mM 3.5174 mL 17.5871 mL 35.1741 mL
5 mM 0.7035 mL 3.5174 mL 7.0348 mL
10 mM 0.3517 mL 1.7587 mL 3.5174 mL
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Research Update

Discovery of a novel 2,5-dihydroxycinnamic acid-based 5-lipoxygenase inhibitor that induces apoptosis and may impair autophagic flux in RCC4 renal cancer cells

Eur J Med Chem 2019 Oct 1;179:347-357.PMID:31260889DOI:10.1016/j.ejmech.2019.06.060.

The inhibition of 5-lipoxygenase (5-LO), the key enzyme for the biosynthesis of leukotrienes (LTs), has generated increasing enthusiasm as anti-inflammatory and antitumor strategies in recent years. Based on our previous studies, we synthesized a series of dihydroxycinnamic acid-based analogs that might be 5-LO inhibitors. LTs biosynthesis inhibition in HEK293 cells and polymorphonuclear leukocytes (PMNL) was measured and antitumor activities were investigated in Renal Cell Carcinoma (RCC). Results showed that the 2,5-Dihydroxycinnamic Acid phenethyl ester (10b) was the best 5-LO inhibitor and was 7-fold more potent than Zileuton (1), the only clinically approved 5-LO inhibitor. 2,5-Dihydroxy substitution was more favorable to 5-LO inhibition since compound 10b is twice as active as CAPE (2) which is a 3,4-dihydroxylcinnamic acid ester. Meanwhile, 10b 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. As to the underlying cell-death mechanisms, 10b induced apoptosis in VHL-deficient RCC4 cells. Also, increases in LC3B and p62 expression suggest a blockage of the autophagic flux in RCC in response to 10b.