555550 Rho Kinase Inhibitor - Calbiochem

555550
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₆H₂₁N₃O₂S • 2HCl

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      555550-1MG
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          Plastic ampoule 1 mg
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          555550-5MG
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              Glass bottle 5 mg
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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
              ATP CompetitiveY
              FormWhite solid
              Hill FormulaC₁₆H₂₁N₃O₂S • 2HCl
              Chemical formulaC₁₆H₂₁N₃O₂S • 2HCl
              Hygroscopic Hygroscopic
              ReversibleY
              Structure formula ImageStructure formula Image
              Applications
              ApplicationThe Rho kinase inhibitor, CAS 872543-07-6, 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

              Documentation

              Rho Kinase Inhibitor - Calbiochem SDS

              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
              Chemical formulaC₁₆H₂₁N₃O₂S • 2HCl
              Structure formulaStructure formula
              Purity≥95% by HPLC
              SolubilityH₂O (5 mg/ml) or Methanol (5 mg/ml)
              Storage +2°C to +8°C
              Hygroscopic
              Protect from light
              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.