CAY10746 |
Catalog No.GC47053 |
A ROCK1 and ROCK2 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2247240-76-0
Sample solution is provided at 25 µL, 10mM.
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.
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)
Average Rating: 5
(Based on Reviews and 7 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *