Table 5. Indolinone Dervivatives as LRRK2 Inhibitors.
IC50 |
|||||||
---|---|---|---|---|---|---|---|
no. | name | wild-type LRRK2 | LRRK2-G2019S | substrate | selectivitya | in vivo | lit. |
9 | Raf-1 kinase inhibitor I (GW5074) | ∼500 nM;b3150 nMc | 880 nMc | LRRKtide; MBPd | 2 | HSVg amplicon-based mouse model | (58, 61) |
10 | Indirubin-3′-monooxime | 4830 nMc | 1310 nMc | MBPd | 2 | HSVg amplicon-based mouse model | (58) |
11 | Sunitinib | 79 nM;e 15 nMf | 19 nM;e 26 nMf | Nictide; LRRKtide | 85 | (60, 63, 65) |
Number of all kinases, including LRRK2.
Goat GST-LRRK2.
GST-LRRK2 (wt/G2019S).
Myelin basic protein (MBP).
GST-LRRK2 (1326–2527; wt/G2019S).
GST-LRRK2 (970–2527; wt/G2019S).
Herpes simplex virus.