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Beschreibung

A cell-permeable butenediamide compound that acts as a potent, active site cysteine reactive irreversible inhibitor of CRM1/exportin 1. Shown to selectively repress agonist-mediated nuclear export of HDAC4/5, Rev and NFAT proteins in neonatal rat ventricular myocytes (NRVMs, EC50 = 2.2 and 3.5 nM for GFP-HDAC5 and GFP-HIV Rev) and suppress hypertrophic growth of NRVMs (EC50 = 52 nM for ANF expression inhibition) with negligible effect either on the phosphorylation of HDAC5 or on the kinase activities of PKD and CaMKII at 1 µ,M.