1273579-40-0

1273579-40-0 structure

Name: Chroman 1
Chemical Name: (3S)-N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-6-methoxy-3,4-dihydro-2H-chromene-3-carboxamide
CAS Number: 1273579-40-0
Molecular Formula: C₂₄H₂₈N₄O₄
Molecular Weight: 436.50400
Catalog: Signaling Pathways Cell Cycle/DNA Damage ROCK
Create Date: 2016-12-15 19:23:03
Modify Date: 2024-01-10 18:32:41
Chroman 1 is a highly potent ROCK2 inhibitor, with an IC50 of 1 nM.

Name	(3S)-N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-6-methoxy-3,4-dihydro-2H-chromene-3-carboxamide
Synonyms	CS-0775 ROCK-II inhibitor Chroman 1

Description	Chroman 1 is a highly potent ROCK2 inhibitor, with an IC50 of 1 nM.
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK Signaling Pathways >> Stem Cell/Wnt >> ROCK Signaling Pathways >> TGF-beta/Smad >> ROCK Research Areas >> Cardiovascular Disease
Target	ROCK2:1 nM (IC50) MRCK:150 nM (IC50)
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].
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].
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.