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Key Documents

688001

Sigma-Aldrich

Y-27632

≥95% (HPLC), liquid, Rho kinase inhibitor, Calbiochem®

Sinónimos:

InSolution Y-27632, Rho Kinase Inhibitor VI

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About This Item

Fórmula empírica (notación de Hill):
C14H21N3O · 2HCl · xH2O
Peso molecular:
320.26 (anhydrous basis)
UNSPSC Code:
12352200
NACRES:
NA.77

product name

Y-27632, InSolution, ≥95%, reversible, inhibitor of Rho kinases

Quality Level

assay

≥95% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

shipped in

wet ice

storage temp.

−20°C

General description

A 5 mM (500 µg/296 µl) aqueous solution of Y-27632 (Cat. No. 688000). A highly potent, cell-permeable, selective inhibitor of Rho-associated protein kinase (Ki = 140 nM for p160ROCK (ROCK-I). Also inhibits ROCK-II with almost equal potency. Inhibition is achieved by competing with ATP for binding to the catalytic site. Exhibits 10- to 50-fold lower affinity for PKCε than p160ROCK. Does not affect the activity of p21-activated protein kinase (PAK) even at high concentrations (~100 mM). Also acts as a potent inhibitor of agonist-induced Ca2+ sensitization of myosin phosphorylation and smooth muscle contractions (IC50 = 700 nM for phenylephrine-induced contractions in aortic strips).
A highly potent, cell-permeable, selective inhibitor of Rho-associated protein kinase (Ki = 140 nM for p160ROCK (ROCK-I). Also inhibits ROCK-II with almost equal potency. Inhibition is achieved by competing with ATP for binding to the catalytic site. Exhibits 10- to 50-fold lower affinity for PKCε than p160ROCK. Does not affect the activity of p21-activated protein kinase (PAK) even at high concentrations (~100 mM). Also acts as a potent inhibitor of agonist-induced Ca2+ sensitization of myosin phosphorylation and smooth muscle contractions (IC50 = 700 nM for phenylephrine-induced contractions in aortic strips).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
p160ROCK
Product competes with ATP.
Reversible: no
Target IC50: 700 nM against phenylephrine-induced contractions in aortic strips
Target Ki: 140 nM for p160ROCK (ROCK-I)

Packaging

Packaged under inert gas

Warning

Toxicity: Harmful (C)

Physical form

A 5 mM (500 µg/296 µl) solution of Y-27632 (Cat. No. 688000) in H₂O.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C).

Other Notes

Chitaley, K., et al. 2001. Nat. Med.7, 119.
Davies, S.P., et al. 2000. Biochem. J. 351, 95.
Narumiya, S., et al. 2000. Methods Enzymol.325, 273.
Hirose, M., et al. 1999. J. Cell Biol.141, 1625.
Maekawa, M., et al. 1999. Science285, 895.
Uehata, M., et al. 1997. Nature389, 990.

Legal Information

Sold under license of PCT Application W098/06,433A1 and under license from Mitsubishi Pharma Tanabe Corporation.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

12 - Non Combustible Liquids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


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