Table 8. Anthracene and Phenanthrene Derivatives as LRRK2 Inhibitors.
IC50 |
|||||||
---|---|---|---|---|---|---|---|
no. | name | wild-type LRRK2 | LRRK2-G2019S | substrate | substrate selectivitya | in vivo | lit. |
15 | SP600125 | 3100 nMb | 5000 nMb | MBPc | 2 | (58) | |
16 | Damnacanthal | 7810 nMb | 9450 nMb | MBPc | 2 | (58) | |
17 | LDN-73794 | 3500 nMd | PLK-peptide | 2 | (68) | ||
18 | LDN-22684e | 6900 nMf | 6100 nMf | PLK-peptide | (69) |
Number of all kinases, including LRRK2.
GST-LRRK2 (wt/G2019S).
Myelin basic protein (MBP).
Purified from BAC-transgenic mouse brain.
Non-ATP competitive.
Human LRRK2 (970-2527; wt/G2019S).