A ROCK-I and ROCK-II inhibitor (IC50s = 14 and 3 nM

CAY10746 – 5 mg

Brand:
Cayman
CAS:
2247240-76-0
Storage:
-20
UN-No:
Non-Hazardous - /

CAY10746 is an inhibitor of Rho-associated kinase I (ROCK-I) and ROCK-II (IC50s = 14 and 3 nM, respectively).{50804} 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.  

 

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SKU: 29814 - 5 mg Category:

Description

A ROCK-I and ROCK-II inhibitor (IC50s = 14 and 3 nM, respectively); 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 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

Formal name: 4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]-benzamide

Synonyms: 

Molecular weight: 457.5

CAS: 2247240-76-0

Purity: ≥95%

Formulation: A crystalline solid

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