2-APB - CAS 524-95-8 - Calbiochem

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