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Submit ReviewChroman 1
Description: Highly potent and selective ROCK 2 inhibitor; improves cell survival after cryogeneisis
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
Purity: ≥98% (HPLC)
Biological Activity for Chroman 1
Chroman 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, Polyamines, and Trans-ISRIB (Cat. No. 5284), a combination known as CEPT. The compound also improves survival of differentiated cells following cryopreservation when used as as part of the CEPT cocktail, with cardiomyocyte cell survival increasing by 36% and motor neuron survival improving by 63% compared with DMSO controls.
Compound Libraries for Chroman 1
Chroman 1 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for Chroman 1
| M. Wt | 509.43 |
| Formula | C24H28N4O4.2HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| InChI Key | ROFMCPHQNWGXGE-SFHVURJKSA-N |
| Smiles | COC1=CC=C2OC[C@@H](C(NC3=C(C=C(C4=CNN=C4)C=C3)OCCN(C)C)=O)CC2=C1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Chroman 1
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 50.94 | 100 | |
| water | 2.55 | 5 |
Preparing Stock Solutions for Chroman 1
The following data is based on the product molecular weight 509.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.96 mL | 9.81 mL | 19.63 mL |
| 5 mM | 0.39 mL | 1.96 mL | 3.93 mL |
| 10 mM | 0.2 mL | 0.98 mL | 1.96 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
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Product Datasheets for Chroman 1
References for Chroman 1
References are publications that support the biological activity of the product.
Chen et al (2011) Asymmetric synthesis of potent chroman-based Rho kinase (ROCK-II) inhibitors. Med.Chem.Commun. 2 73
Chen et al (2021) A versatile polypharmacology platform promotes cytoprotection and viability of human pluripotent and differentiated cells. Nat.Methods 18 528 PMID: 33941937
If you know of a relevant reference for Chroman 1, please let us know.
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Citations for Chroman 1
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