GSK269962A is a potent ROCK inhibitor with IC50 values of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2, respectively. GSK269962A displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases. GSK269962A induces vasorelaxation in preconstricted rat aorta (IC50 = 35 nM). GSK269962A induced a reduction in blood pressure of approximately 10, 20, and 50 mm Hg at doses of 1, 3, and 30 mg/kg. GSK269962A represents a novel class of ROCK inhibitors that have profound effects in the vasculature and may enable us to further evaluate the potential beneficial effects of ROCK inhibition in animal models of cardiovascular as well as other chronic diseases.
Clin Cancer Res. 2018 Jul 1;24(13):3149-3162.
Targeting bromodomain and extra-terminal (BET) family proteins in castration resistant prostate cancer (CRPC)
GSK269962A purchased from AbMole
|Source||Clin Cancer Res (2018). Figure 5. ROCK inhibitor (Abmole Bioscience)|
|Cell Lines||CP50 PDX-O|
|Incubation Time||30 to 45 minutes|
|Results||Nuclear BRD4 expression increased significantly (p=0.008) as patients progressed from HSPC|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Lipopolysaccharide promotes contraction of uterine myocytes via activation of Rho/ROCK signaling pathways.
Hutchinson JL, et al. FASEB J. 2014 Jan;28(1):94-105. PMID: 24076962.
Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.
Doe C, et al. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98. PMID: 17018693.
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GSK180736A, developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5.
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