| Description |
Chroman 1 is a highly potent ROCK2 inhibitor, with an IC50 of 1 nM.
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| Related Catalog |
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| Target |
ROCK2:1 nM (IC50)
MRCK:150 nM (IC50)
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| In Vitro |
Chroman 1 is a highly potent ROCK2 inhibitor, with an IC50 of < 1 nM. Chroman 1 also shows inhibitory activities against MRCK, with an IC50 of 150 nM, but has no effect on PKA (IC50, > 20000 nM) or AKT1 (IC50, > 20000 nM)[1].
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| Kinase Assay |
Assays are performed using the HTRF KinEASE STK S2 kit. A 5 μL mixture of 1 μM STK2 substrate and 20 μM ATP in STK-buffer is added to the wells. Inhibitor (including Chroman 1, 20 nL) at various concentrations is then dispensed. Reaction is started by addition of 0.5 nM ROCK-II in STK-buffer (5 μL). After 4 h at room temperture (rt), the reaction is stopped by addition of 10 μL mixture of 1× STK antibody-Cryptate in detection buffer and 62.5 nM Sa-XL in detection buffer. After 1 h at rt, the plates are read on the Viewlux in HTRF mode[1].
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| References |
[1]. Yen Ting Chen, et al. Asymmetric synthesis of potent chroman-based Rho kinase (ROCK-II) inhibitors. Med.Chem.Commun., 2011, 2, 73-75.
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