GSK429286A is a cell-permeable, selective Rho-associated kinase (ROCK) inhibitor with an IC50 of 14 nM. GSK429286A also possessed exciting selectivity (30-fold) against a panel of 33 kinases, including RSK1 (IC50 = 3.1 μM) and p70S6K (Ic50 = 2.85μM). ROCKs are serine/threonine specific protein kinases which play a crucial role in organization of the actin cytoskeleton. ROCK inhibitors have been found to prevent apoptosis, as well as to enhance the survival and cloning efficiency of dissociated human embryonic stem (ES) cells without affecting their self-renewal properties or pluripotency.
|Animal models||Male spontaneously hypertensive rats (SHRs)|
|Formulation||Formulated in 6% Hydroxypropyl-β-Cyclodextrin (pH4.0) and 5% DMSO solution|
|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.
|Solubility||DMSO 85 mg/mL|
|Related ROCK Products|
ZINC00881524 is a potent and selective ROCK inhibitor.
|HA 1100 hydrochloride
HA 1100 hydrochloride is a cell-permeable, selective Rho-kinase inhibitor.
|Ripasudil (K-115) dihydrate
Ripasudil (K-115) hydrochloride dihydrate is potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.
SR-3677 is a new potent and selective ROCK-II inhibitor with an IC50 of ~3 nM in enzyme and cell based assays; IC50 for ROCK-I is 56 ± 12 nM.
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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