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555550 Rho Kinase Inhibitor - Calbiochem

The Rho kinase inhibitor, CAS 871543-07-6, is a cell-permeable, highly specific, reversible, potent, and ATP-competitive inhibitor of Rho-associated kinase (Ki = 1.6 nM).

Rho Kinase Inhibitor - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: H-1152, H-1152P, (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine, 2HCl, ROCK Inhibitor, Dimethylfasudil (diMF, H-1152P)

Primary Target: ROCK
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
871543-07-6C₁₆H₂₁N₃O₂S • 2HCl

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          Description
          OverviewA cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, reversible, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK; Ki = 1.6 nM). Exhibits a much weaker affinity for other serine/threonine kinases (Ki = 630 nM for PKA, 9.27 μM for PKC, and 10.1 μM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate MARCKS (IC50 = 2.5 μM) in NT-2 cells. Reported to be more potent and selective than Y-27632 (Cat. Nos. 688000 and 688001). Mainly targets Aurora Kinase A, and induces polyploidization of acute megakaryocytic leukemia cells (AMKL). At 10 mM (500 µg/128 µl) solution of Rho Kinase Inhibitor (Cat. No. 555552) in H2O is also available.
          Catalogue Number555550
          Brand Family Calbiochem®
          SynonymsH-1152, H-1152P, (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine, 2HCl, ROCK Inhibitor, Dimethylfasudil (diMF, H-1152P)
          References
          ReferencesWen, Qiang, et al. 2012. Cell 150, 575.
          Ikenoya, M., et al. 2002. J. Neurochem. 81, 9.
          Sasaki, Y., et al. 2002. Pharmacol. Ther. 93, 225.
          Product Information
          CAS number871543-07-6
          ATP CompetitiveY
          FormWhite solid
          Hill FormulaC₁₆H₂₁N₃O₂S • 2HCl
          Chemical formulaC₁₆H₂₁N₃O₂S • 2HCl
          Hygroscopic Hygroscopic
          ReversibleY
          Structure formula ImageStructure formula Image
          Quality LevelMQ100
          Applications
          ApplicationThe Rho kinase inhibitor, CAS 871543-07-6, is a cell-permeable, highly specific, reversible, potent, and ATP-competitive inhibitor of Rho-associated kinase (Ki = 1.6 nM).
          Biological Information
          Primary TargetROCK
          Primary Target K<sub>i</sub>1.6 nM against G-protein Rho-associated kinase
          Purity≥95% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Harmful
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications
          Global Trade Item Number
          Catalogue Number GTIN
          555550-1MG 04055977268393
          555550-5MG 04055977268409

          Documentation

          Rho Kinase Inhibitor - Calbiochem MSDS

          Title

          Safety Data Sheet (SDS) 

          Rho Kinase Inhibitor - Calbiochem Certificates of Analysis

          TitleLot Number
          555550

          References

          Reference overview
          Wen, Qiang, et al. 2012. Cell 150, 575.
          Ikenoya, M., et al. 2002. J. Neurochem. 81, 9.
          Sasaki, Y., et al. 2002. Pharmacol. Ther. 93, 225.
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision11-September-2012 JSW
          SynonymsH-1152, H-1152P, (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine, 2HCl, ROCK Inhibitor, Dimethylfasudil (diMF, H-1152P)
          DescriptionA cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, reversible, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK; Ki = 1.6 nM). Inhibits other serine/threonine kinases only at higher concentrations (Ki = 630 nM for PKA, 9.27 µM for PKC, and 10.1 µM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate (MARCKS) in NT-2 cells (IC50 = 2.5 µM). Reported to be a more potent and selective inhibitor than Y-27632 (Cat. No. 688000 & 688001). Mainly targets Aurora Kinase A, and induces polyploidization of acute megakaryocytic leukemia cells (AMKL).
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number871543-07-6
          Chemical formulaC₁₆H₂₁N₃O₂S • 2HCl
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityH₂O (5 mg/ml) or Methanol (5 mg/ml)
          Storage Protect from light
          +2°C to +8°C
          Hygroscopic
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Harmful
          ReferencesWen, Qiang, et al. 2012. Cell 150, 575.
          Ikenoya, M., et al. 2002. J. Neurochem. 81, 9.
          Sasaki, Y., et al. 2002. Pharmacol. Ther. 93, 225.