Comparative Evaluation and Profiling of Chemical Tools for the Nuclear Hormone Receptor Family 2.

Validation studies in a cellular reporter gene assay indicated TLX activation with EC 50 values of 9.2 μM ( 14 ), 1.0 μM ( 15 ), and 250 nM ( 16 ) and 15 showed a trend toward SIRT and SLC1a1 but not p21 induction in human glioblastoma cells (T98G) in qRT-PCR experiments. 146 Importantly, TLX expression was not affected by 15 . 106 A small selectivity panel suggested a preference of 14 – 16 for TLX over ERβ, LXRβ (DSF), PNR, RXRα, and COUP-TF2 (reporter gene assays). 146 Low toxicity in a WST-1 assay in HEK293T cells further supported the suitability of 15 as an early chemical tool to study TLX modulation despite low stability against microsomal degradation ( t 1/2 < 15 min).

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