Teleocidin A1 | Non-phorbol ester PKC activator

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Teleocidin A1 (70497-14-2) is a selective protein kinase C activator1 (EC50 = 40 ng/ml) representing a new class of non-phorbol ester tumor promotor2. Teleocidin A1 mimics the effect of diacylglycerol (DAG), activating PKC, but unlike DAG causes persistent activation.3 It enhances actin redistribution, vacuole formation and c-fos expression in PLC/PRF/5 hepatoma cells.4 Occurs in toxic cyanobacterial blooms.5

References/Citations:

  1. Fujiki et al. (1984), Activation of calcium-activated, phospholipid-dependent protein kinase (protein-kinase C) by new classes of tumor promoters: teleocidin and debromoaplysiatoxin; Biochem. Biophys. Res. Commun. 120 339
  2. Fujiki et al. (1987), New Classes of Tumor Promoters: Teleocidin, Aplysiatoxin, and Palytoxin; Adv. Cancer Res. 49 223
  3. Kozikowski et al. (1991), Synthesis of structural analogues of lyngbyatoxin A and their evaluation as activators of protein kinase C; J. Med. Chem. 34 2420
  4. Tsukamoto et al. (1993), Thapsigargin, an inhibitor of endoplasmic reticulum Ca(2+)-ATPase, enhances c-fos expression but antagonizes vacuole formation of human hepatoma cells induced by teleocidin; Biochim. Biophys. Acta 1177 31
  5. Esposito et al. (2019), A Fast Detection Strategy for Cyanobacterial blooms and associated cyanotoxins (FDSCC) reveals the occurrence of lyngbyatoxin A in campania (South Italy); Chemosphere 225 342
70497-14-2, Lyngbyatoxin A, non-phorbol ester PKC activator, PKC activator, protein kinase C activator, Teleocidin, Teleocidin A1, Teleocidin A1 Supplier
Alternate Name:
Lyngbyatoxin A

Safety Data Sheet:

N/A

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Teleocidin A1 (70497-14-2) is a selective protein kinase C activator1 (EC50 = 40 ng/ml) representing a new class of non-phorbol ester tumor promotor2. Teleocidin A1 mimics the effect of diacylglycerol (DAG), activating PKC, but unlike DAG causes persistent activation.3 It enhances actin redistribution, vacuole formation and c-fos expression in PLC/PRF/5 hepatoma cells.4 Occurs in toxic cyanobacterial blooms.5

References/Citations:

  1. Fujiki et al. (1984), Activation of calcium-activated, phospholipid-dependent protein kinase (protein-kinase C) by new classes of tumor promoters: teleocidin and debromoaplysiatoxin; Biochem. Biophys. Res. Commun. 120 339
  2. Fujiki et al. (1987), New Classes of Tumor Promoters: Teleocidin, Aplysiatoxin, and Palytoxin; Adv. Cancer Res. 49 223
  3. Kozikowski et al. (1991), Synthesis of structural analogues of lyngbyatoxin A and their evaluation as activators of protein kinase C; J. Med. Chem. 34 2420
  4. Tsukamoto et al. (1993), Thapsigargin, an inhibitor of endoplasmic reticulum Ca(2+)-ATPase, enhances c-fos expression but antagonizes vacuole formation of human hepatoma cells induced by teleocidin; Biochim. Biophys. Acta 1177 31
  5. Esposito et al. (2019), A Fast Detection Strategy for Cyanobacterial blooms and associated cyanotoxins (FDSCC) reveals the occurrence of lyngbyatoxin A in campania (South Italy); Chemosphere 225 342