CAY10746

DESCRIPTION

A ROCK1 and ROCK2 inhibitor (IC50s = 14 and 3 nM, respectively); selective for ROCK1 and ROCK2 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 LIMK2, Aurora A, Aurora B, PKG1α, and PKG1β (IC50s = 46, 1,072, 1,239, 517, and 660 nM, respectively); inhibits phosphorylation of MYPT1 in SH-SY5Y cells at 0.1-10 µM; inhibits HUVEC migration at 1 µM; protects isolated mouse retinal neurons from apoptosis and oxidative stress induced by high glucose in an in vitro model of diabetic retinopathy; promotes high glucose-induced vessel regression in mouse retinal explants

DETAILS

Inchi: InChI=1S/C26H23N3O5/c1-29(2)20-8-6-17(7-9-20)26(32)28-19-5-3-4-18(14-19)27-25(31)16-34-21-10-11-22-23(30)12-13-33-24(22)15-21/h3-15H,16H2,1-2H3,(H,27,31)(H,28,32)
Purity: ≥95%
Raptas: Product Type|Biochemicals|Antioxidants||Product Type|Biochemicals|Kinase Inhibitors|LIMKs||Product Type|Biochemicals|Kinase Inhibitors|ROCK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cardiovascular System|Vasculature|Endothelium||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Neuroscience|Ophthalmology||Research Area|Oxidative Stress & Reactive Species|Antioxidant Activity
Smiles: CN(C)C1=CC=C(C(NC2=CC=CC(NC(COC3=CC(OC=CC4=O)=C4C=C3)=O)=C2)=O)C=C1
Inchikey: WVGDUQVQWLHVEA-UHFFFAOYSA-N
Cas Number: 2247240-76-0
Formulation: A crystalline solid
Storage Temp: -20
Shipping Temp: -20
Formula Markup: C26H23N3O5
Formula Weight: 457.5
Shelf Life Days: 730