E-Cadherin Upregulator, ResEcad-Calbiochem

C₁₇H₁₇N₃O₃

311.34

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).

Toxicity: Regulatory Review (Z)

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

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

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥95% (HPLC)

powder

Calbiochem^®

OK to freeze
protect from light

off-white

DMSO: 50 mg/mL

ambient

2-8℃

10 mg in Glass bottle
Packaged under inert gas

11 - Combustible Solids

WGK 3