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PDM2

Catalog No. T4608 CAS 688348-25-6

PDM 2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.

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PDM2, CAS 688348-25-6

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Purity: 98%

Biological Description

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Description	PDM 2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.
Targets&IC50	AhR:1.2±0.4 nM(Ki)
In vitro	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].

Molecular Weight	283.58
Formula	C14H9Cl3
CAS No.	688348-25-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 50 mg/mL (176.32 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. de Medina, P. ,Casper, R.,Savouret, J.F., et al. Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators. Journal of Medicinal Chemistry 48, 287-291 (2005).

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Immunology/Inflammation Compound Library Anti-Metabolism Disease Compound Library Nonsteroidal Anti-Inflammatory Compound Library Bioactive Compound Library

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Keywords

PDM2 688348-25-6 代谢免疫与炎症 AhR Aryl Hydrocarbon Receptor inhibit PDM-2 PDM 2 Inhibitor inhibitor

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