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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 Chemical Structure
PDM2, CAS 688348-25-6
Pack Size Availability Price/USD Quantity
10 mg In stock $ 42.00
25 mg In stock $ 79.00
50 mg In stock $ 127.00
100 mg In stock $ 229.00
1 mL * 10 mM (in DMSO) In stock $ 46.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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 1 year

Solubility Information

DMSO: 50 mg/mL (176.32 mM), sonification is recommended.

TargetMolReferences 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:
Bioactive Compounds Library Max Immunology/Inflammation Compound Library Anti-Metabolism Disease Compound Library Kinase Inhibitor Library Transcription Factor-Targeted Compound Library Bioactive Compound Library Inhibitor Library Nuclear Receptor Compound Library Nonsteroidal Anti-Inflammatory Compound Library NO PAINS Compound Library

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Keywords

PDM2 688348-25-6 Immunology/Inflammation Metabolism AhR Aryl Hydrocarbon Receptor inhibit Inhibitor PDM 2 PDM-2 inhibitor

 

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