| Identification | Back Directory | [Name]
(S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE | [CAS]
451462-58-1 | [Synonyms]
H1152
H1152P
H-1152;H 1152;H1152
(S)-H-1152 (hydrochloride)
(S)-H-1152 dihydrochloride
(S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE
4-methyl-5-[(2-methyl-1,4-diazepan-1-yl)sulfonyl]isoquinoline,dihydrochloride
Isoquinoline, 5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]-4-methyl-
(S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]-hexahydro-1H-1,4-diazepinedihydrochloride | [Molecular Formula]
C16H21N3O2S | [MDL Number]
MFCD07357272 | [MOL File]
451462-58-1.mol | [Molecular Weight]
319.42 |
| Chemical Properties | Back Directory | [Boiling point ]
519.6±60.0 °C(Predicted) | [density ]
1.218±0.06 g/cm3(Predicted) | [storage temp. ]
Desiccate at +4°C | [solubility ]
25℃: DMSO | [form ]
Powder | [pka]
9.76±0.40(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Description]
Rho-associated kinase (ROCK), activated by GTP-linked Rho, phosphorylates targets that are involved in cytoskeletal remodeling, smooth muscle contraction, and neuronal development. H-1152 is a potent, specific, ATP-competitive, and cell permeable inhibitor of ROCK (Ki = 1.6 nM). It is a more potent inhibitor of ROCK than either Y-27632 (Ki = 140 nM) or HA-1077 (Ki = 330 nM). H-1152 poorly inhibits PKA, PKC, and myosin light chain kinase (Ki = 0.63, 9.27, and 10.1 μM, respectively). It has been used to examine the role of ROCK in such diverse processes as stress fiber assembly, vasoconstriction, as well as spontaneously tonic smooth muscle and neurite extension. | [Uses]
H-1152 is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2. | [Definition]
ChEBI: (S)-2-methyl-1-(4-methylisoquinoline-5-sulfonyl)-1,4-diazepane is a member of the class of isoquinolines that is the sulfonamide formed by the formal condensation of the sulfo group of 4-methylisoquinoline-5-sulfonic acid with the 1-amino group of (S)-2-methyl-1,4-diazepane. It has a role as an EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor. It is a member of isoquinolines and a N-sulfonyldiazepane. It is a conjugate base of a (S)-2-methyl-1-(4-methylisoquinoline-5-sulfonyl)-1,4-diazepane(2+). | [Biological Activity]
Rho-kinase (ROCK) inhibitor that displays high selectivity over other protein kinases (IC 50 values are 0.012, 0.180, 0.360, 0.745, 3.03, 5.68 and 28.3 μ M for ROCKII, CAMKII, PKG, Aurora A, PKA, PKC and MLCK respectively). Inhibits sulprostone-induced contractions in guinea pig aorta (IC 50 = 190 nM) and displays proerectile effects in rats. | [IC 50]
ROCKII: 12 nM (IC50); CaMKII: 0.18 μM (IC50); PKG: 0.36 μM (IC50); AuroraA: 0.745 μM (IC50); PKA: 3.03 μM (IC50); Src: 3.06 μM (IC50); PKC: 5.68 μM (IC50); Abl: 7.77 μM (IC50); MKK4: 16.9 μM (IC50); MLCK: 28.3 μM (IC50); EGFR: 50 μM (IC50); GSK3α: 60.7 μM (IC50); AMPK: 100 μM (IC50); P38α: 100 μM (IC50) | [storage]
Store at -20°C | [References]
[1] Tamura M, et al. Development of specific Rho-kinase inhibitors and their clinical application. Biochim Biophys Acta. 2005 Dec 30;1754(1-2):245-52. Epub 2005 Sep 12. DOI:10.1016/j.bbapap.2005.06.015
[2] Ikenoya M, et al. Inhibition of rho-kinase-induced myristoylated alanine-rich C kinase substrate (MARCKS) phosphorylation in human neuronal cells by H-1152, a novel and specific Rho-kinase inhibitor. J Neurochem. 2002 Apr;81(1):9-16. DOI:10.1046/j.1471-4159.2002.00801.x
[3] Lie M, et al. Accelerated neurite growth from spiral ganglion neurons exposed to the Rho kinase inhibitor H-1152. Neuroscience. 2010 Aug 25;169(2):855-62. DOI:10.1016/j.neuroscience.2010.05.020 |
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