1309371-03-6 Usage
Uses
Different sources of media describe the Uses of 1309371-03-6 differently. You can refer to the following data:
1. 2-Trifluoromethyl-2'-methoxychalcone is a novel chalcone derivative as potent Nrf2 activators in mice and human lung epithelial cells.
2-Trifluoromethyl-2'-methoxychalcone is a potent activator of Nrf2, both, in vitro and in mice. 4 Human bronchial epithelial cells treated with 10 μM 2-trifluoromethyl-2'-methoxychalcone showed a marked increase in the expression of the Nrf2-regulated antioxidant genes, GCLM and NQO1.
2. Nrf2 activation is central to cytoprotective gene expression against oxidative and/or electrophilic stress. Unless activated by inflammatory, environmental, or oxidative stressors, Nrf2 is sequestered in the cytoplasm by its repressor, Keap1. Because of its protective capabilities, small molecules that activate Nrf2 signaling are being examined as potential anti-cancer or anti-inflammatory agents. 2-Trifluoromethyl-2'-methoxychalcone is a potent activator of Nrf2, both in vitro and in mice. Human bronchial epithelial cells treated with 10 μM 2-trifluoromethyl-2'-methoxychalcone showed a marked increase in the expression of the Nrf2-regulated antioxidant genes, GCLM and NQO1. Furthermore, treatment of mice mice with 50 mg/kg 2-trifluoromethyl-2’-methoxychalcone leads to a 4.5- and 4.6-fold increase in the expression of GCLM and NQO1, respectively, in the small intestine compared to controls.[Cayman Chemical]
3. 2-Trifluoromethyl-2''-methoxychalcone is a novel chalcone derivative as potent Nrf2 activators in mice and human lung epithelial cells. 2-Trifluoromethyl-2''-methoxychalcone is a potent activator of Nrf2, both, in vitro and in mice. 4 Human bronchial epithelial cells treated with 10 μM 2-trifluoromethyl-2''-methoxychalcone showed a marked increase in the expression of the Nrf2-regulated antioxidant genes, GCLM and NQO1.
Biological Activity
2-trifluoromethyl-2'-methoxychalcone is a nrf2 activator.nrf2-mediated activation of antioxidant response element is a key process of molecular mechanisms regulating the protective function of phase ii detoxification and antioxidant enzymes against oxidative stress, carcinogenesis, and inflammation.
in vitro
the expression of luciferase gene under the control of nqo1-are sequence was measured using stably transfected beas-2b cells treated with 2-trifluoromethyl-2'-methoxychalcone. results showed that the exposure to 2-trifluoromethyl-2'-methoxychalcone led to a significant concentration-dependent increase in luciferase activity. moreover, beas-2b cells were coincubated with 2-trifluoromethyl-2'-methoxychalcone and with or without n-acetylcysteine, and it was found that 2-trifluoromethyl-2'-methoxychalcone could potentially increase the expression of nr2-regulated antioxidant genes in the presence of n-acetylcysteine [1].
in vivo
c57bl/6 mice were treated with a single dose of vehicle or 2-trifluoromethyl-2'-methoxychalcone or sulforaphane as the positive control, and small intestines were harvested 24 h later. results showed that the expression of gclm and nqo1 in the small intestine of mice treated with 2-trifluoromethyl-2'-methoxychalcone was 6-fold and 10-fold higher compared to vehicle, respectively. in addition, the expression of gclm and nqo1 in the small intestine treated with 2-trifluoromethyl-2'-methoxychalcone was 3-fold and 5-fold higher compared to sulforaphane, respectively [1].
references
[1] v. kumar, s. kumar, m. hassan, et al. novel chalcone derivatives as potent nrf2 activators in mice and human lung epithelial cells. journal of medicinal chemistry 54(12), 4147-4159 (2011).
Check Digit Verification of cas no
The CAS Registry Mumber 1309371-03-6 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,0,9,3,7 and 1 respectively; the second part has 2 digits, 0 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 1309371-03:
(9*1)+(8*3)+(7*0)+(6*9)+(5*3)+(4*7)+(3*1)+(2*0)+(1*3)=136
136 % 10 = 6
So 1309371-03-6 is a valid CAS Registry Number.
1309371-03-6Relevant articles and documents
Synthesis of a series of unsaturated ketone derivatives as selective and reversible monoamine oxidase inhibitors
Choi, Ji Won,Jang, Bo Ko,Cho, Nam-Chul,Park, Jong-Hyun,Yeon, Seul Ki,Ju, Eun Ji,Lee, Yong Sup,Han, Gyoonhee,Pae, Ae Nim,Kim, Dong Jin,Park, Ki Duk
, p. 6486 - 6496 (2015/10/05)
We have synthesized three categories of α,β-unsaturated carbonyl derivatives and evaluated their MAO-A and MAO-B inhibitory activities. Among them, compound 10b including α,β-unsaturated ketone group showed the most potent and selective MAO-B inhibitory activity (IC50 human MAO-B 16 nM, >6000-fold selective vs MAO-A) and compound 10b exhibited good reversibility compared with selegiline, a well-known irreversible MAO-B inhibitor. However, both α,β-unsaturated amide and ester derivatives exhibited weaker MAO-B inhibition potencies. The docking studies provided insights into the possible binding modes and the key interaction sites of the synthesized MAO-B inhibitors.
NUCLEAR RECEPTOR MODULATORS AND THEIR USE FOR THE TREATMENT AND PREVENTION OF CANCER
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Page/Page column 45, (2013/02/28)
Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein R1 to R5 and X1 to X5 are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed.
