Identification | Back Directory | [Name]
H1152, DIHYDROCHLORIDE | [CAS]
871543-07-6 | [Synonyms]
H1152, DIHYDROCHLORIDE 5-[[(2S)-Hexahydro-2-Methyl-1H-1,4-diazepin-1-yl]sulfonyl]-4-Methylisoquinoline H1152P2HCl,(S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolynyl)sulfonyl]homopiperazineDihydrochloride H1152P Dihydrochloride, (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolynyl)sulfonyl]homopiperazine Dihydrochloride | [Molecular Formula]
C16H21N3O2S | [MDL Number]
MFCD06411451 | [MOL File]
871543-07-6.mol | [Molecular Weight]
319.422 |
Chemical Properties | Back Directory | [Appearance]
White to Off-White Solid | [Melting point ]
182-184°C | [storage temp. ]
Hygroscopic, -20°C Freezer, Under Inert Atmosphere | [solubility ]
Methanol, Water | [form ]
Solid | [color ]
White to Off-White | [Stability:]
Hygroscopic |
Hazard Information | Back Directory | [Chemical Properties]
White to Off-White Solid | [Uses]
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 | [Uses]
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; Ki = 1.6 nM). Exhibits a much weaker affinity for other serine/threonine kinases (Ki = 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 |
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SPIRO PHARMA
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Lynnchem
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Novachemistry
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Musechem
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