A selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II); poorly inhibits CaMKII

(S)-Glycyl-H-1152 (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
913844-45-8
Storage:
-20
UN-No:
De Minimis - 1230 / 3|6.1

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal.{17734}{17735}{17322} Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II).{17736} It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each).{17736} The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).{17736,17737}  

 

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Description

A selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II); poorly inhibits CaMKII, protein kinase G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each)

Formal name: 2-amino-1-[(3S)-hexahydro-3-methyl-4-[(4-methyl-5-isoquinolinyl)sulfonyl]-1H-1,4-diazepin-1-yl]-ethanone, dihydrochloride

Synonyms:  Rho Kinase Inhibitor IV

Molecular weight: 449.4

CAS: 913844-45-8

Purity: ≥98%

Formulation: A solution in methanol

Product Type|Biochemicals|Kinase Inhibitors|ROCK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area

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