| Identification | Back Directory | [Name]
Benzamide, 4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]- | [CAS]
2247240-76-0 | [Synonyms]
CAY10746
Benzamide, 4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]- | [Molecular Formula]
C26H23N3O5 | [MOL File]
2247240-76-0.mol | [Molecular Weight]
457.48 |
| Chemical Properties | Back Directory | [Boiling point ]
664.2±55.0 °C(Predicted) | [density ]
1.363±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble | [form ]
A crystalline solid | [pka]
12.72±0.70(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Biological Activity]
CAY10746 is an inhibitor of Rho-associated kinase I (ROCK-I) and ROCK-II (IC50s = 14 and 3 nM, respectively).1 It is selective for ROCK-I and ROCK-II over PKA (IC50 = >10,000 nM) and over 387 recombinant human protein kinases in a panel of 394 kinases (IC50s = >10,000 nM for all) but does inhibit LIM kinase 2 (LIMK2), Aurora A, Aurora B, cGMP-dependent protein kinase 1α (PKG1α), and PKG1β (IC50s = 46, 1,072, 1,239, 517, and 660 nM, respectively). CAY10746 (0.1-10 μM) inhibits phosphorylation of the ROCK target protein MYPT1 in SH-SY5Y cells. It also inhibits migration of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 1 μM. CAY10746 (1 μM) protects isolated mouse retinal neurons from apoptosis and oxidative stress induced by high glucose in an in vitro model of diabetic retinopathy. It also promotes high glucose-induced vessel regression in mouse retinal explants. | [References]
1.Zhao, L., Li, Y., Wang, Y., et al.Discovery of 4H-chromen-4-one derivatives as a new class of selective Rho kinase (ROCK) inhibitors, which showed potent activity in ex vivo diabetic retinopathy modelsJ. Med. Chem.62(23)10691-10710(2019)
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