BIO-2007817 is a small-molecule positive allosteric modulator of Parkin E3 ligase with EC50 of 0.17 uM (TR-FRET).
BIO-2007817 stimulated Parkin autoubiquitination as measured by Western blots in a concentration-dependent manner, was also able to induce the appearance of monoubiquitinated forms of Miro1.
BIO-2007817 induced the appearance of slower-migrating Parkin species in a concentration-dependent manner with maximal efficacy at 20 uM in Parkin autoubiquitination assay.
BIO-2007817 does not affect the rate of Parkin translocation to mitochondria nor the number of mitochondria within lysosomes.
