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Rho Pathway Inhibitor I - Rho kinase (ROCK) inhibitor Y-27632

Manufacturer: Cytoskeleton Inc
Shipping: Standard

NOTE : THIS PRODUCT IS NO LONGER AVAILABLE AND HAS BEEN REPLACED BY PRODUCT CODES CT04-A AND CT04-B

TYPE IN PRODUCT CODE CT04-A OR CT04-B IN THE SEARCH BOX 

Product Uses Include :

  • Specific inhibitor of ROCK.
  • Rho pathway studies in cultured cells.
  • Study effects of altered Rho pathway signaling on other connected pathways.

The G-switch™  line of small G-protein tools has been developed with an emphasis on creating highly potent reagents that target endogenous Rho family proteins and pathways.  In contrast to methods that rely on over-expression or knockdown of target proteins (e.g., DNA transfection of dominant negative or constitutively active Rho mutants, RNAi knockdown) , the G-switchTM reagents act rapidly on the endogenous target protein (in minutes to hours, depending on product), thereby optimizing the chance of generating a more physiologically relevant response.  The G-switch™ product line includes reagents that directly and indirectly modulate Rho family signal transduction, thereby offering a wide range of mechanistic tools to study these critical cellular functions.  See Cytoskeleton’s web site for the latest G-switch™ information.

Rho Pathway Inhibitor CN06 acts by directly and potently inhibiting the Rho-associated coiled-coil forming protein serine/threonine kinase (ROCK) family of proteins, with a Ki of 220 nM for ROCK I and 300 nM for ROCK II (1,2).  The affinities for other Rho effector kinases; such as citron and PKN are at least 10X lower (1). Effector kinases in the Rho family pathway such as the Rac/Cdc42 effector, p21-activated kinase (PAK), are not affected (3).  The uptake of cell permeable CN06 is time and temperature dependent.  Uptake has been shown to reach a plateau at 30 minutes at 37°C and is negligible at 4°C (4).  ROCK proteins are ubiquitously expressed, making this inhibitor applicable to the study of almost all cell lines and tissues (4 and Table 1).

References :

  1. Ishizaki T. et al. 2000. Pharmacological properties of Y-27632, a specific inhibitor of Rho-associated kinases. Mol. Pharmacol. 57, 976-983.
  2. Sold under license of PCT Application W098/06,433A1.
  3. Suzuki-Inoue K. et al. 2001. Rac, a small guanosine triphosphate-binding protein, and p21-activated kinase are activated during platelet spreading on collagen-coated surfaces: roles of integrin alpha(2)beta(1). Blood. 98, 3708-3716.
  4. Narumiya S. et al. 2000. Use and properties of ROCK-specific inhibitor Y-27632. Meth. Enzymol. 325, 273-284.
  5. Hirose M. et al. 1998. Molecular dissection of the Rho-associated protein kinase (p160ROCK)-regulated neurite remodeling in neuroblastoma N1E-115 cells. J. Cell Biol. 141,1625-1636.
  6. Essler M. et al. 1999. Mildly oxidized low density lipoprotein induces contraction of human endothelial cells through activation of Rho/Rho kinase and inhibition of myosin light chain phosphatase. J. Biol. Chem. 274, 30361-30364.

 

SizeCatalogue noPrice 
5x10 units size CN06-A £115.00/€161.00
Qty:
20 x 10 units size CN06-B £295.00/€413.00
Qty:

All prices shown are exlusive of VAT.