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555550 Rho Kinase Inhibitor - Calbiochem

Overview

Replacement Information

Key Spec Table

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

Products

Catalogue NumberPackaging Qty/Pack
555550-1MG Plastic ampoule 1 mg
555550-5MG Glass bottle 5 mg
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 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.

Brochure

Title
Bulk Product Guide
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.