Heptelidic acid (Koningic acid, Avocettin, FO-4443, BRN 5091359)

Antibiotic. \nPotent selective glyceraldehyde 3-phosphate dehydrogenase (GAPDH) inhibitor. Binds to the essential Cys149 residue in the catalytic site of GADPH. \nAnticancer compound. Selectively kills high-glycolytic cancer cells through glucose-dependent active ATP deprivation. \nAntimalarial. \nApoptosis inhibitor. DNA fragmentation and caspase-3 activation inhibitor. \nSelective and competitive inhibitor of mammalian DNA polymerases beta, lambda and terminal deoxynucleotidyl transferase (TdT) in family X of pols. \n\n\nStorage and Stability:\nShort-term Storage: +4 degrees C\nLong-term Storage: -20 degrees C\nStable for at least 3 years after receipt when stored at -20 degrees C.

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SPECIFICATIONS

Catalog Number

044883

Size

250ug

Purity

>95% (HPLC)

References

Product Reference: \n?A new sesquiterpene antibiotic, heptelidic acid producing organisms, fermentation, isolation and characterization: Y. Itoh, et al.; J. Antibiot. (Tokyo) 33, 468 (1980)\n?Structure of heptelidic acid, a new sesquiterpene antibiotic from fungi: Y. Itoh, et al.; J. Antibiot. (Tokyo) 33, 525 (1980)\n?Specific inhibition of glyceraldehyde-3-phosphate dehydrogenase by koningic acid (heptelidic acid): A. Endo, et al.; J. Antibiot. (Tokyo) 38, 920 (1985)\n?Inactivation of rabbit muscle glyceraldehyde-3-phosphate dehydrogenase by koningic acid: K. Sakai, et al.; Biochim. Biophys. Acta 952, 297 (1988)\n?Identification of koningic acid (heptelidic acid)-modified site in rabbit muscle glyceraldehyde-3-phosphate dehydrogenase: K. Sakai, et al.; Biochim. Biophys. Acta 1077, 192 (1991)\n?Koningic acid (heptelidic acid) inhibition of glyceraldehyde-3-phosphate dehydrogenases from various sources: M. Kato, et al.; Biochim. Biophys. Acta 1120, 113 (1992)\n?Glyceraldehyde-3-phosphate dehydrogenase is required for the transport of nitric oxide in platelets: B. McDonald, et al.; PNAS 90, 11122 (1993)\n?Antitumor activity of heptelidic acid chlorohydrin: J. Kawashima, et al.; J. Antibiot. (Tokyo) 47, 1562 (1994)\n?Antimalarial activity of radicicol, heptelidic acid and other fungal metabolites: Y. Tanaka, et al.; J. Antibiot. (Tokyo) 51, 153 (1998)\n?Glyceraldehyde-3-phosphate dehydrogenase activity as an independent modifier of methylglyoxal levels in diabetes: P.J. Beisswenger, et al.; Biochim. Biophys. Acta 1637, 98 (2003)\n?D-Glyceraldehyde causes production of intracellular peroxide in pancreatic islets, oxidative stress, and defective beta cell function via non-mitochondrial pathways: H. Takahashi, et al.; J. Biol. Chem. 279, 37316 (2004)\n?Glucose-dependent active ATP depletion by koningic acid kills high-glycolytic cells: S. Kumagai, et al.; BBRC 365, 362 (2008)\n?Heptelidic acid, a sesquiterpene lactone, inhibits Etoposide-induced apoptosis in human leukemia U937 cells: J.H. Kim & C.H. Lee; J. Microbiol. Biotechnol. 19, 787 (2009)\n?Novel terpenoids, trichoderonic acids A and B isolated from Trichoderma virens, are selective inhibitors of family X DNA polymerases: Y. Yamaguchi, et al.; Biosci. Biotechnol. Biochem. 74, 793 (2010)\n?

Alternative Names

Koningic acid, Avocettin, FO-4443, BRN 5091359