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 |
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| Formula: | C16H21N3O2S . 2HCl |
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| MW: | 319.4 . 73.0 |
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| CAS: | 451462-58-1 |
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| Purity: | ≥98% (TLC) |
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| Identity: | Identity determined by 1H-NMR and 13C-NMR. |
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| Appearance: | White to off-white solid. |
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| Solubility: | Soluble in water. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Handling: | Protect from light. Hygroscopic. |
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| 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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