|(E)-1-(6-甲氧基萘-2-基)-3-(吡啶-3-基)丙-2-烯-1-酮|CsnPharm

CAS No.: 1821143-80-9

(E)-1-(6-Methoxynaphthalen-2-yl)-3-(pyridin-3-yl)prop-2-en-1-one Catalog No. CSN22890

Synonyms: DMU2139

DMU2139 is a selective inhibitor of CYP1B1 with IC50 of 9 nM.

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技术信息

生物活性

描述The cytochrome P450 (CYP) enzyme superfamily plays a key role in the phase 1 oxidative metabolism and detoxification of both endogenous and xenobiotic substances. CYP1B1, belonging to the CYP1 subfamily, has been identified as a key enzyme in the carcinogenic action of 17-β-estradiol (E₂) and participates by catalysing hydroxylation at C-4 in E₂ to generate 4-hydroxyestradiol (4-OHE₂). MU2139 is a potent and specific inhibitor of CYP1B1 with IC₅₀ of 9 nM. MU2139 shows 88 and 133-fold selectivity over CYP1A1 and CYP1A2. IC₅₀ for MU2139 in live yeast cells was determined to be 65 nM. This result indicates MU2139 can enter live yeast cells to inhibit the endoplasmic reticular membrane-bound CYP1B1. IC₅₀ value for MU2139 was found to be in the range of 4-53 nM in live human HEK293 cells. This result indicates that MU2139 potently inhibits the human CYP1B1 enzyme that resides on the endoplasmic reticular membranes within human cells. In the presence of DMU2139, the EC₅₀ is reversed back to 8.3 μM from 61 μM indicating that DMU2139 overcomes cisplatin resistance in adherent HEK293 cells that overexpress CYP1B1^[1].
作用机制The driving force for the binding of DMU2139 seems to be the additional hydrophobic interactions of the A ring with the hydrophobic Phe123 residue of the binding cavity^[1].
参考文献

[1] Horley NJ, Beresford KJ, Chawla T, et al. Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines. Eur J Med Chem. 2017;129:159‐174

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4563 mL
- 17.2814 mL
- 34.5629 mL
- 5 mM
- 0.6913 mL
- 3.4563 mL
- 6.9126 mL
- 10 mM
- 0.3456 mL
- 1.7281 mL
- 3.4563 mL

技术信息

CAS号

1821143-80-9

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H15NO2

运输

蓝冰

分子量

289.33

别名

DMU2139

溶解度

DMSO	30.0 mg/mL (103.7 mM) warming
Water	insoluble

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(E)-1-(6-Methoxynaphthalen-2-yl)-3-(pyridin-3-yl)prop-2-en-1-one Catalog No. CSN22890

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