N-Alkylated aziridines are easily-prepared, potent, specific and cell-permeable covalent inhibitors of human β-glucocerebrosidaseElectronic supplementary information (ESI) available: Copies of the proton (1H) and carbon (13C) NMR spectra for all novel compounds synthesized, all enzyme kinetic data (Fig. S1-S4) and the figures for inactivation rates inside live cells (Fig. S5). See DOI: 10.1039/c5cc03828f

β-Glucocerebrosidase deficiency leads to Gaucher disease and is a potential marker of Parkinson's disease. We have identified N -octyl conduritol aziridine as a potent and specific covalent inactivator of GBA1 in living cells. This compound is a promising lead towards a positron emission tomography probe intended to image GBA1 activity. N -Octyl conduritol aziridine is a potent and specific covalent inactivator of β-glucocerebrosidase (GBA1) inside live human cells.