E-Cadherin Upregulator, ResEcad

Toxicity: Regulatory Review (Z)

A cell-permeable isoxazolocarboxamide compound that enhances the E-cadherin protein level in lung squamous cell carcinoma H520 and colorectal adenocarcinoma SW620 cells (6.3- and 10-fold, respectively; 10 µM for 24 h) in a dose-dependent manner (EC₅₀ = 1.25 and 2.13 µM, respectively), resulting in an effective culture invasiveness reduction (by ~50% in SW620 invasion assays). The observed cellular E-cadherin protein upregulation correlates well with an increase in both cellular E-cadherin gene CHD1 transcription (10.2-fold increase in SW620 by RNA-Seq analysis;10 µM for 24 h) and histone H4 Lys9 acetylation (19- and 57-fold enhancement in H529 and SW620 cells, respectively; 10 µM for 24 h), although evidence indicates no direct inhibition of HDACs 1-11 activity by the compound and other cellular factors involved in histone acetylation regulation are the likely candidates as the direct drug target(s).

Stoops, S.L., et al. 2011. ACS Chem. Biol.6, 452.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

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