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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: Ficha de dados de segurança do material (FDSM) ou ficha de segurança do material (FSM), certificado de análise (CA) e certificado de qualidade (CQ), dossiês e outros documentos disponíveis.

Sinônimos: 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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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
      Número de catálogo GTIN
      555550-1MG 04055977268393

      Documentation

      Rho Kinase Inhibitor - Calbiochem MSDS

      Título

      Ficha de Segurança de Produtos (MSDS) 

      Rho Kinase Inhibitor - Calbiochem Certificados de análise

      TítuloNúmero do lote
      555550

      Referências

      Visão geral de referência
      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.

      Brochura

      Título
      Bulk Product Guide
      Ficha de dados

      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.