Y-39983 Hcl is a selective ROCK inhibitor derived from Y-27632, inhibited ROCK more potently than Y-27632.
|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|
|Solubility||10 mM in DMSO
10 mM in H2O
|Related ROCK Products|
|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.
GSK269962A is a potent ROCK inhibitor with IC50 values of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2, respectively.
Fasudil (HA-1077) is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively.
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