General description
A cell-permeable modulator of Ins(1,4,5)P3-induced Ca2+ release. Inhibits Ins(1,4,5)P3-induced Ca2+ release from rat cerebellar microsomal preparations (IC50 = 42 µM) without affecting [3H]-Ins(1,4,5)P3 binding to its receptor. Does not affect Ca2+ release from the ryanodine-sensitive Ca2+ store in rat leg skeletal muscle and heart. Inhibits spontaneous as well as the phasic contractions induced by uterotonic agents. Also reported to inhibit angiotensin II-induced contractions in aortic muscles.
A cell-permeable modulator of Ins(1,4,5)P3-induced Ca2+ release. Inhibits Ins(1,4,5)P3-induced Ca2+ release from rat cerebellar microsomal preparations (IC50 = 42 µM) without affecting [3H]-Ins(1,4,5)P3 binding to its receptor. In liver cells, 2-APB inhibits store-operated Ca2+ channels through a mechanism which may involve its binding to either the channel protein or an associated regulatory protein. Has no effect on the Ca2+ release from the ryanodine-sensitive Ca2+ store prepared from rat leg skeletal muscle and heart.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Ins(1,4,5)P3-induced Ca2+ release
Product does not compete with ATP.
Reversible: no
Target IC50: 42 µM against Ins(1,4,5)P3-induced Ca2+ release from rat cerebellar microsomal preparations
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.
Other Notes
Brooke, R. T., et al. 2004. Lab. Invest.84, 29.
Gregory, R.B., et al. 2001. Biochem. J.354, 285.
Ma, H.T., et al. 2001. J. Biol. Chem.276, 18888.
Ascher-Landsberg, S., et al. 1999. Biochem. Biophys. Res. Commun.264, 979.
Maruyama, T., et al. 1997. J. Biochem.122, 498.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany