NR2E3 agonist 11a | NR2E3 agonist

NR2E3 agonist 11a chemical structure

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11a (911211-69-3) is an agonist of the photoreceptor-specific nuclear receptor (NR2E3; PNR; RNR), found in rod photoreceptor cells (EC50 = 141 nM ß-lactamase assay; 35 nM NCOR assay).1  An interesting tool for targeting age-related macular degeneration.  11a was able to increase p53 activation in uterine cancer tumors suggesting NR2E3 agonism as a new anti-cancer strategy.2 A previous study found that cytotoxicity of 11a was due to G1/S phase cell cycle arrest rather than NR2E3 agonism.3

References/Citations:

  1. Wolkenberg et al. (2006), Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand; Bioorg. Med. Chem. Lett., 16 5001
  2. Wang et al. (2025), Orphan nuclear receptor NR2E3 is a new molecular vulnerability in solid tumors by activating p53; Cell Death Dis., 16 15
  3. Zhao et al. (2013), Systematic Analyses of the Cytotoxic Effects of Compound 11a, a Putative Synthetic Agonist of Photoreceptor-Specific Nuclear Receptor (PNR), in Cancer Cell Lines; PLoS One, 8 e75198
911211-69-3, Compound 11a, NR2E3 agonist 11a, PNR agonist, RNR agonist

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11a (911211-69-3) is an agonist of the photoreceptor-specific nuclear receptor (NR2E3; PNR; RNR), found in rod photoreceptor cells (EC50 = 141 nM ß-lactamase assay; 35 nM NCOR assay).1  An interesting tool for targeting age-related macular degeneration.  11a was able to increase p53 activation in uterine cancer tumors suggesting NR2E3 agonism as a new anti-cancer strategy.2 A previous study found that cytotoxicity of 11a was due to G1/S phase cell cycle arrest rather than NR2E3 agonism.3

References/Citations:

  1. Wolkenberg et al. (2006), Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand; Bioorg. Med. Chem. Lett., 16 5001
  2. Wang et al. (2025), Orphan nuclear receptor NR2E3 is a new molecular vulnerability in solid tumors by activating p53; Cell Death Dis., 16 15
  3. Zhao et al. (2013), Systematic Analyses of the Cytotoxic Effects of Compound 11a, a Putative Synthetic Agonist of Photoreceptor-Specific Nuclear Receptor (PNR), in Cancer Cell Lines; PLoS One, 8 e75198