SR-3677 is an effective and specific inhibitor of ROCK2 (IC50: 3 nM).

ROCK2:3 nM, ROCK1:56 nM

SR-3677在酶和细胞实验中的IC50约为3 nM，其对353种激酶的非靶点作用率为1.4%，且只抑制了70种非激酶酶和受体中的3种。SR-3677对ROCK-I的IC50值为56 nM。

SR-3677在离体条件下增加猪眼的房水流出，并抑制肌球蛋白轻链的磷酸化。持续暴露于25 μM SR-3677可使流出功能在1小时灌注时增加60%，在2至5小时的时间点增加至70-80%。

5 μL mixture of a 1 μM STK2 substrate and ATP (ROCK-I: 4 μM; ROCK-II: 20 μM) in STK-buffer is added to the wells. 20 nL of test compounds (SR-3677) is dispensed. The reaction is started by addition of 5 μL of 2.5 nM. ROCK-I or 0.5 nM ROCK-II in STK-buffer. After 4 h at RT, the reaction is stopped by the addition of 10 μL of 1x antibody and 62.5 nM Sa-XL in the detection buffer.