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H-1152 . dihydrochloride

ROCK inhibitor
ALX-270-423-M001 1 mg 87.00 USD
ALX-270-423-M005 5 mg 349.00 USD
ALX-270-423-M025 25 mg 998.00 USD
Do you need bulk/larger quantities?
A cell permeable, highly specific, potent and ATP-competitive inhibitor of Rho kinase (ROCK) (Ki=1.6nM). Exhibits a much weaker affinity for other serine/threonine kinases (Ki=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 Details

Alternative Name:H-1152P . 2HCl, (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine . 2HCl
Formula:C16H21N3O2S . 2HCl
MW:319.4 . 73.0
Purity:≥98% (TLC)
Identity:Identity determined by 1H-NMR and 13C-NMR.
Appearance:White to off-white solid.
Solubility:Soluble in water.
Shipping:Ambient Temperature
Long Term Storage:-20°C
Handling:Protect from light. Hygroscopic.
Regulatory Status:RUO - Research Use Only
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Product Literature References

LFA-1 and Kindlin-3 enable the collaborative transport of SLP-76 microclusters by myosin and dynein motors: K.P. Eidell, et al.; J. Cell Sci. 36, 258602 (2021), Abstract;
Dysregulation in Actin Cytoskeletal Organization Drives Increased Stiffness and Migratory Persistence in Polyploidal Giant Cancer Cells: B. Xuan, et al.; Sci. Rep. 8, 11935 (2018), Abstract;
Sema3d controls collective endothelial cell migration by distinct mechanisms via Nrp1 and PlxnD1: M.J. Hamm, et al.; J. Cell Biol. 215, 415 (2016), Abstract; Full Text
A self-organized biomechanical network drives shape changes during tissue morphogenesis: A. Munjal, et al.; Nature 524, 351 (2015), Application(s): Cell culture , Abstract;
Actin-Mediated Gene Expression Depends on RhoA and Rac1 Signaling in Proximal Tubular Epithelial Cells: K. Giehl, et al.; PLoS One 10, e0121589 (2015), Application(s): Cell Culture, Abstract; Full Text
Local and tissue-scale forces drive oriented junction growth during tissue extension: C. Collinet, et al.; Nat. Cell Biol. 17, 1247 (2015), Application(s): Cell Culture, 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;
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;
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;
Rho kinase regulates fragmentation and phagocytosis of apoptotic cells: K.A. Orlando, et al.; Exp. Cell Res. 312, 5 (2006), 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;
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;
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;

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ROCK inhibitor
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ALX-270-333-M001 1 mg 153.00 USD
ALX-270-333-M005 5 mg 243.00 USD
ALX-270-333-M025 25 mg 742.00 USD
Do you need bulk/larger quantities?