Biochem/physiol Actions

Primary Targetprotein phosphatase-2A & -1

Reversible: yes

Target IC₅₀: 0.5-1.0 and 2 nM for PP2A and PP1, respectively

Cell permeable: yes

General description

Cell-permeable protein phosphatase 2A (PP2A) inhibitor (IC₅₀ = 0.5-1.0 nM). Also inhibits protein phosphatase 1 (PP1; IC₅₀ = 2 nM). A non-phorbol ester type tumor promoter that induces oxidative DNA damage. Selectively increases the efficacy of AMPA receptor-mediated synaptic transmission at excitatory synapses. Recently, it has been used to study the regulation of Ca²⁺-activated K⁺ channels in smooth muscle and to correlate shape changes in fibroblasts with the degree of protein phosphorylation. Also known to prevent γ-radiation induced apoptosis in Burkitt′s lymphoma cell line BM13674.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Murakami, N., et al. 1994. Neurosci. Lett.176, 181.Takeuchi, T., et al. 1994. Biochem. Biophys. Res. Commun.205, 1803.Figurov, A., et al. 1993. Eur. J. Neurosci.5, 1083.Song, Q., and Lavin, M.F. 1993. Biochem. Biophys. Res. Commun.190, 47.Gopalakrishna, R., et al. 1992. Biochem. Biophys. Res. Commun.189, 950.Carl, A., et al. 1991. Am. J. Physiol.261, C387.Suganuma, M., et al. 1990. Cancer Res.50, 3521.Cohen, P. 1989. Annu. Rev. Biochem.58, 453.Cohen, P., et al. 1989. J. Biol. Chem.264, 21435.Ishihara, H., et al. 1989. Biochem. Biophys. Res. Commun.159, 871.Kato, Y., et al. 1988. J. Org. Chem.53, 3930.Kato, Y., et al. 1986. J. Am. Chem. Soc.108, 2780.

Packaging

Packaged under inert gas

5 µg in Glass bottle

Physical form

A 100 µM (5 µg/50 µL) sterile-filtered solution of Calyculin A, Discodermia calyx (Cat. No. 208851) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C. Use only fresh DMSO for further dilutions.

Warning

Toxicity: Standard Handling (A)