W-7 HYDROCHLORIDE

Description

Calmodulin is a calcium-dependent protein that regulates the activity of a diverse array of enzymes, ion channels, and other proteins and thus has diverse roles in cell function. W-7 is a cell-permeable antagonist of calmodulin (K_i = 11 μM). Two molecules of W-7 bind to calcium-binding domains in each calmodulin molecule, blocking its interaction with target proteins. W-7 also associates, at lower affinities, with calcium-binding domains of other proteins, including troponin C and myosin light chain kinase (K_i = 70 and 300 μM, respectively).

Chemical Properties

White Crystalline Solid

Uses

N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide hydrochloride has been used to study its effect of on coated pit staining.

Uses

W7 is a vascular relaxing agent which affects vascular smooth muscle actomyosin. W7, an inhibitor of actomyosin superprecipitation, produces relaxation of isolated rabbit arterial strips and antagonizes the contraction of the strips induced by various contractile agonists. W7 is also a calmodulin antagonist that binds to calmodulin and inhibits Ca2+/calmodulin-regulated enzyme activities.

General Description

A cell-permeable and reversible calmodulin antagonist that inhibits myosin light chain kinase (IC₅₀ = 51 μM) and Ca²⁺-calmodulin-dependent phosphodiesterase (IC₅₀ = 28 μM).

Biological Activity

Calmodulin antagonist. Inhibits Ca 2+ -calmodulin-dependent phosphodiesterase (IC 50 = 28 μ M) and myosin light chain kinase (IC 50 = 51 μ M).

Biochem/physiol Actions

Cell permeable: yes

storage

Store at RT