PDM2 是一种有效的选择性芳烃受体 (AhR) 拮抗剂,Ki为 1.2±0.4 nM。
产品描述
PDM 2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.
体外活性
In a previous screening study, it was found that the replacement of resveratrol hydroxyls by the same substituent produced compounds with the following order of affinity: OH (resveratrol) , OMe< F< CF3< Cl (PDM 2). PDM 2 exhibited a Ki of 1.25 for AhR and no affinity for ER, indicating that replacement of hydroxyl with chloride could abolish binding on ER and dramatically increase the affinity for AhR. Moreover, among its analogs PDM 2 was the most potent AhR antagonists in this series, being 10-fold more efficient than resveratrol. PDM 2, devoid of measurable affinity for ER, did not display any effect on ER-driven transcription. Therefore, PDM 2 was considered as a selective AhR modulator with regard to ER. In addition, its trimethoxylated derivatives and 3,5-methoxy derivatives were able to induce cytotoxicity at doses lower than 100 nM, which was consistent with previous data. 3,5-Methoxy derivatives, however, only showed cytotoxicity at concentrations higher than 10 μM [1].
Cas No.
688348-25-6
分子式
C14H9Cl3
分子量
283.58
储存和溶解度
DMSO:50 mg/mL (176.32 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years