ALEXIS Biochemicals: H-1152 . dihydrochloride

ALX-270-423

Revised 11-Oct-06

H-1152 . dihydrochloride
SYNONYMS	H-1152P . 2HCl (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine . 2HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Rho-associated Protein Kinases [ROCK] / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-423-M001		1 mg	95.00 USD
ALX-270-423-M005		5 mg	380.00 USD
ALX-270-423-M025		25 mg	1'100.00 USD

Product Specification

FORMULA:	C₁₆H₂₁N₃O₂S . 2HCl
MW:	319.4 . 73.0
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Hygroscopic. Protect from light.
HAZARD:	HARMFUL.
IDENTITY:	Identity determined by ¹H-NMR and ¹³C-NMR.

Product Description

A cell permeable, highly specific, potent and ATP-competitive inhibitor of Rho kinase (ROCK) (K_i=1.6nM). Exhibits a much weaker affinity for other serine/threonine kinases (K_i=630nM for PKA, 9.27mM for PKC and 10.1mM for MLCK). More potent and selective than Y-27632 (Prod. No. ALX-270-333). Inhibits the phosphorylation of MARCKS in cells stimulated by lysophosphatidic acid. Inhibits EP3-stimulated NO formation. Prevents fragmentation of apoptotic cells. Relieves neuropathic pain.

Product Specific Literature References

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: M. Ikenoya, et al.; J. Neurochem. 81, 9 (2002) Abstract
The novel and specific Rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinoline)sulfonyl]-homopiperazine as a probing molecule for Rho-kinase-involved pathway: Y. Sasaki, et al.; Pharmacol. Ther. 93, 225 (2002) Abstract
New aspects of neurotransmitter release and exocytosis: Rho-kinase-dependent myristoylated alanine-rich C-kinase substrate phosphorylation and regulation of neurofilament structure in neuronal cells: Y. Sasaki; J. Pharmacol. Sci. 93, 35 (2003) Abstract
Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity: C. Breitenlechner, et al.; Structure 11, 1595 (2003) Abstract
Involvement of Rho-kinase in inflammatory and neuropathic pain through phosphorylation of myristoylated alanine-rich C-kinase substrate (MARCKS): S. Tatsumi, et al.; Neuroscience 131, 491 (2005) Abstract
Rho-kinase mediates spinal nitric oxide formation by prostaglandin E2 via EP3 subtype: S. Matsumura, et al.; BBRC 338, 550 (2005) Abstract
Rho kinase regulates fragmentation and phagocytosis of apoptotic cells: K.A. Orlando, et al.; Exp. Cell Res. 312, 5 (2006) Abstract
Direct Rho-associated kinase inhibiton induces cofilin dephosphorylation and neurite outgrowth in PC-12 cells: Z. Zhang, et al.; Cell. Mol. Biol. Lett. 11, 12 (2006) Abstract
Regulation of the crossbridge cycle in vascular smooth muscle by cAMP signalling: G. Pfitzer, et al.; J. Muscle Res. Cell. Motil. 27, 445 (2006) Abstract
Involvement of ROCK-mediated endothelial tension development in neutrophil-stimulated microvascular leakage: J.W. Breslin, et al.; Am. J. Physiol. Heart Circ. Physiol. 290, H741 (2006) Abstract