PDM2

SKU: orb1302714

Description

PDM 2 is a highly selective small molecule antagonist of the aryl hydrocarbon receptor (AhR). It is a valuable research tool for investigating AhR signaling in both cellular and animal models, with applications in immunology, toxicology, and cancer research.

Research Area

Immunology & Inflammation, Metabolism Research

Key Properties

• CAS Number: 688348-25-6
• MW: 283.58
• Purity: 99.57% (May vary between batches)
• Formula: C₁₄H₉Cl₃
• SMILES: Clc1ccc(\C=C\c2cc(Cl)cc(Cl)c2)cc1
• Target: Aryl Hydrocarbon Receptor,AhR
• Solubility: DMSO:50 mg/mL (176.32 mM);10% DMSO+90% Corn Oil:2.5 mg/mL (8.82 mM)

Bioactivity

• Target 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 (PDM2). PDM2 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 PDM2 was the most potent AhR antagonists in this series, being 10-fold more efficient than resveratrol. PDM2, devoid of measurable affinity for ER, did not display any effect on ER-driven transcription. Therefore, PDM2 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 .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Aryl Hydrocarbon Receptor, ArylHydrocarbonReceptor, AhR, PDM 2, PDM2, PDM-2, inhibit, Inhibitor

Compound Identifiers

PubChem CID

9838722