FSL0431

Structure

• InChI=1S/C10H12O4/c1-9-5-3-4-6(13-5)10(9,2)8(12)14-7(9)11/h5-6H,3-4H2,1-2H3/t5?,6?,9-,10+
• InChIKey=DHZBEENLJMYSHQ-OBDNUKKESA-N

Synonyms

• 56-25-7
• Cantharidin

Origin

Epicauta
Lytta vesicatoria

Biological activities

Inhibition of protein phosphatase 2A

Therapeutic

Anticancer

Target

Protein phosphatase 2A (PP2A)

Assay information

IC₅₀ of phosphorylase a phosphatase activity of PP2A AC form (EC 3.1.3.16) by cantharidin and okadaic acid treatment are 50 nM and 12 nM, respectively
Inhibition of purified catalitic subunits of PP2A (IC₅₀=0.16 μM by cantharidin and 0.04 nM by okadaic acid) and PP1 (IC₅₀=1.7 μM by cantharidin)
Growth inhibition (IC₅₀) of human pancreatic cancer cells (PANC-1 and CFPAC-1) at 72 h after cantharidin treatment are 9.42 and 7.25 μM, respectively. In comparison, the IC₅₀ of normal human pancreatic dust cells is

References

• Li W, Xie L, Chen Z, Zhu Y, Sun Y, Miao Y, Xu Z, Han X
  Cantharidin, a potent and selective PP2A inhibitor, induces an oxidative stress-independent growth inhibition of pancreatic cancer cells through G2/M cell-cycle arrest and apoptosis.
  Cancer Sci, 101(5): 1226-1233 (2010)  20331621  doi: 10.1111/j.1349-7006.2010.01523.x
• Honkanen RE
  Cantharidin, another natural toxin that inhibits the activity of serine/threonine protein phosphatases types 1 and 2A.
  FEBS Lett, 330(3): 283-286 (1993)  8397101
• Li YM, Casida JE
  Cantharidin-binding protein: identification as protein phosphatase 2A.
  Proc Natl Acad Sci U S A, 89(24): 11867-11870 (1992)  1334551
• J. Org. Chem., 50: 2576-2578 (1985)
• J. Am. Chem. Soc., 75: 384-392 (1953)
• Ann. Chim., 76: 302-307 (1810)