H1152, dihydrochloride

Chemical properties

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The Uses of H1152, dihydrochloride

ROCK Inhibitor. A cell-permeable isoquinolinesulfonamide compoud that acts as a highly specific, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK: Ki=1.6nM). Exhibits a much weaker affinity for other serine/threonine

The Uses of H1152, dihydrochloride

ROCK Inhibitor. A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK: Ki=1.6nM). Exhibits a much weaker affinity for other serine/threonine kinases (Ki=630nM for PKA 9.27 mMfor PKC, and 10.1mM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate MARCKS (IC50=2.5nM) in NT-2 cells.

Definition

ChEBI: (S)-2-methyl-1-(4-methylisoquinoline-5-sulfonyl)-1,4-diazepane dihydrochloride is a hydrochloride salt resulting from the reaction of (S)-2-methyl-1-(4-methylisoquinoline-5-sulfonyl)-1,4-diazepane with 2 mol eq. of hydrogen chloride. An ATP-competitive inhibitor of Rho kinase (ROCK). It has a role as an EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor. It contains a (S)-2-methyl-1-(4-methylisoquinoline-5-sulfonyl)-1,4-diazepane(2+).

General Description

A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, reversible, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK; K_i = 1.6 nM). Exhibits a much weaker affinity for other serine/threonine kinases (K_i = 630 nM for PKA, 9.27 μM for PKC, and 10.1 μM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate MARCKS (IC₅₀ = 2.5 μM) in NT-2 cells. Reported to be more potent and selective than Y-27632 (Cat. Nos. 688000 and 688001). Mainly targets Aurora Kinase A, and induces polyploidization of acute megakaryocytic leukemia cells (AMKL). At 10 mM (500 μg/128 μl) solution of Rho Kinase Inhibitor (Cat. No. 555552) in H₂O is also available.

Biochem/physiol Actions

Primary TargetROCK

Storage

Desiccate at +4°C