Calyculin A

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Calyculin A, a marine toxin isolated from Disodermia calyx, is a structurally distinct inhibitor of protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A-C). It has been shown that calyculin A displays inhibitory properties towards the endogenous phosphatase of smooth muscle myosin B and induces contraction in the muscle fibers. Contraction induced by calyculin A was accompanied by an increase in the cytosolic free Ca2+ concentration. Additionally, it has been reported that this compound can bind to protein phosphatases in mouse skin, which serve as okadaic acid receptors. Consequentially, calyculin A induces ornithine decarboxylase in the mouse skin and is believed to promote tumor growth.

Calyculin A is a more potent phosphatase inhibitor than Okadaic acid. As shown by Western blot, treatment of cells with 100 nM Calyculin A for 30 minutes induces threonine phosphorylation, detected by Phospho-Threonine-Polyclonal Antibody #9381. IC50 values for inhibitory activity against PP1 are approximately 2 nM. IC50 values for inhibitory activity against PP2A are approximately 0.5 -1.0 nM.
calyculin A increases the pacemaker current fully activated conductance in the SA node. The increase had a time constant of 466 sec, which is much greater than for changes associated with direct gating by cAMP (time constant of about 5 sec. These times are similar to those required for increases in the fully activated conductance in neurons by cAMP/PKA-mediated processes, suggesting that similar processes might mediate increases in fully activated conductance in SA node myocytes. Experiments have suggested the involvement of tyrosine kinases, along with cAMP/PKA, in the regulation of fully activated conductance. Inhibitors of these enzymes have been shown to reduce the maximal conductance of If in myocytes from the rabbit SA node. The reduction in maximal conductance produced by these inhibitors is augmented in the presence of CPTcAMP, a membrane-permeable analogue of cAMP, indicating a link between cAMP and tyrosine kinase pathways.

The toxicity and long-term health effects of recreational Calyculin A use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown.
Formula: C50H81N4O15P

CAS Number: 101932-71-2

Molecular Weight: 1009.17

Purity: 99.8% 

Appearance: Research Chemicals are available in solid

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