(S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE

Product Name: (S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE
CAS No.: 451462-58-1
Chemical Name: (S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE
Synonyms: H1152;H1152P;H-1152;H 1152;H1152;(S)-H-1152 dihydrochloride;(S)-H-1152 (hydrochloride);(s)-4-methyl-5-((2-methyl-1,4-diazepan-1-yl)sulfonyl)isoquinoline;(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
CBNumber: CB2377081
Molecular Formula: C16H21N3O2S
Formula Weight: 319.42
MOL File: 451462-58-1.mol

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(S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H318Causes serious eye damage

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 10007653
Product name: (S)-H-1152 (hydrochloride)
Purity: ≥95%
Packaging: 500μg
Price: $36
Updated: 2024/03/01

Cayman Chemical

Product number: 10007653
Product name: (S)-H-1152 (hydrochloride)
Purity: ≥95%
Packaging: 1mg
Price: $66
Updated: 2024/03/01

Cayman Chemical

Product number: 10007653
Product name: (S)-H-1152 (hydrochloride)
Purity: ≥95%
Packaging: 5mg
Price: $274
Updated: 2024/03/01

Cayman Chemical

Product number: 10007653
Product name: (S)-H-1152 (hydrochloride)
Purity: ≥95%
Packaging: 10mg
Price: $477
Updated: 2024/03/01

AK Scientific

Product number: 3714AH
Product name: (S)-4-Methyl-5-((2-methyl-1,4-diazepan-1-yl)sulfonyl)isoquinoline
Packaging: 5mg
Price: $402
Updated: 2021/12/16

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(S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE Chemical Properties,Usage,Production

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 (K_i = 1.6 nM). It is a more potent inhibitor of ROCK than either Y-27632 (K_i = 140 nM) or HA-1077 (K_i = 330 nM). H-1152 poorly inhibits PKA, PKC, and myosin light chain kinase (K_i = 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)

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

(S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE Preparation Products And Raw materials

Raw materials

Preparation Products

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(S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE Suppliers

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451462-58-1, (S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINERelated Search:

H-9 DIHYDROCHLORIDE (S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE H-8 DIHYDROCHLORIDE H-1152Glycyl, Dihydrochloride FASUDIL

(S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]-hexahydro-1H-1,4-diazepinedihydrochloride

H1152

H1152P

(S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE

(S)-H-1152 (hydrochloride)

(S)-H-1152 dihydrochloride

H-1152;H 1152;H1152

Isoquinoline, 5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]-4-methyl-

4-methyl-5-[(2-methyl-1,4-diazepan-1-yl)sulfonyl]isoquinoline,dihydrochloride

(s)-4-methyl-5-((2-methyl-1,4-diazepan-1-yl)sulfonyl)isoquinoline

451462-58-1

C16H21N3O2S2HCl

Angiogenesis and Metastasis

Intracellular signaling

SiChem