Basic information Safety Supplier Related

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

Basic information Safety Supplier Related

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

Product Name:
(S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE
Synonyms:
  • (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-
CAS:
451462-58-1
MF:
C16H21N3O2S
MW:
319.42
Product Categories:
  • Angiogenesis and Metastasis
  • Intracellular signaling
  • SiChem
Mol File:
451462-58-1.mol
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(S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE Chemical Properties

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

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.

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.

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

Shanghai Boyle Chemical Co., Ltd.
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(S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE(451462-58-1)Related Product Information