Skip to main content
. 2012 Jan 18;3(3):151–160. doi: 10.1021/cn200117j

Table 5. Indolinone Dervivatives as LRRK2 Inhibitors.

graphic file with name cn-2011-00117j_0005.jpg

    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)
a

Number of all kinases, including LRRK2.

b

Goat GST-LRRK2.

c

GST-LRRK2 (wt/G2019S).

d

Myelin basic protein (MBP).

e

GST-LRRK2 (1326–2527; wt/G2019S).

f

GST-LRRK2 (970–2527; wt/G2019S).

g

Herpes simplex virus.