Cantharidic acid, an analog of cantharidin (CA), is a potent and selective inhibitor of PP2 (protein phosphatase (PP2A) and PP1 (protein phosphatase 1). PP2A regulates phosphorylation-dephosphorylation events and is found in plants and mammalian tissues. Studies show that it can cause biochemical changes in the mouse liver. Both okadaic acid (sc-3513), also a PP2A inhibitor, and cantharidic acid have been demonstrated to elevate levels of microtubule-bound phospho-53 in the breast cancer cell line, MCF7. Cantharidic acid does not inhibit PP2B or PP2C.
1. Graziano, M.J. and Casida, J.E. 1987. Toxicol. Lett. 37: 143-148. PMID: 2955551 2. Li, Y.M. and Casida, J.E. 1992. Proc. Natl. Acad. Sci. U.S.A. 89: 11867-11870. PMID: 1334551 3. Li, Y.M., et al. 1993. Biochem. Pharmacol. 46: 1435-1443. PMID: 8240393 4. Béghin, A., et al. 2008. Cell Cycle. 7: 3074-3082. PMID: 18818514
Soluble in DMSO (25 mg/ml), and ethanol (10 mg/ml warm). Partly miscible in water.
Store at room temperature
~407.8° C at 760 mmHg (Predicted)
~1.4 g/cm3 (Predicted)
PP2A: IC50 = 53 nM; PP1: IC50 = 0.56 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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Beghin et alBeghin et al. (PubMed ID 18818514) showed that cantharidic acid-mediated inhibition of PPA2 increased mirotubule-bound phospho-p53 and reduced sensitivity to chemotherapy in breast cancer cells. -SCBT Publication Review
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