Chemical Name: (3S)-N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-3,4-dihydro-6-methoxy-2H-1-benzopyran-3-carboxamide dihydrochloride
Biological ActivityChroman 1 is a highly potent and selective ROCK2 (Rho-kinase) inhibitor (IC50 values are 1 and 52 pM at ROCK2 and ROCK1, respectively). Chroman 1 exhibits >2000-fold selectivity for ROCK2 over a range of related kinases including MRCK, PKA, and AKT1 (IC50 values are 150, >20000, and >20000 nM, respectively). Chroman 1 promotes survival of pluripotent stem cells (PSCs) in culture when used in combination with Emricasan (Cat. No. 7310), Polyamine Supplement x1000 (lyophilized) (Cat. No. 7739), and trans-ISRIB (Cat. No. 5284), a combination known as CEPT. When used as part of the CEPT cocktail, Chroman 1 also improves survival of differentiated cells following cryopreservation with cardiomyocyte cell survival increasing by 36% and motor neuron survival improving by 63% compared with DMSO controls.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Asymmetric synthesis of potent chroman-based Rho kinase (ROCK-II) inhibitors.
Chen et al.
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