An irreversible inhibitor of GAPDH (Ki = 1.6 µM); selectively induces apoptosis in high-glycolytic cancer cells by inhibiting the generation of ATP in the glycolytic pathway; also inhibits mammalian DNA polymerases β and λ as well as terminal deoxynucleotidyl transferase in family X of DNA polymerases (Kis range from 5.2-9.5 µM)

Heptelidic Acid – 1 mg

Brand:
Cayman
CAS:
57710-57-3
Storage:
-20
UN-No:
Non-Hazardous - /

Glyceraldehyde 3-phosphate dehydrogenase (GAPDH), a key enzyme in carbohydrate metabolism, reversibly catalyzes the conversion of GAP to 1,3-bisphosphoglycerate and NAD+. Heptelidic acid is a sesquiterpene lactone produced by the fungus T. koningii that was shown to have antibiotic activity against anaerobic bacteria such as Bacteroides.{30738} It acts as an irreversible inhibitor of GAPDH that binds to the cysteine-149 residue at the active site of the enzyme (Ki = 1.6 µM).{30740} It can selectively induce apoptosis in high-glycolytic cancer cells by inhibiting the generation of ATP in the glycolytic pathway.{30739} Heptelidic acid is also a selective and competitive inhibitor of mammalian DNA polymerases β and λ as well as terminal deoxynucleotidyl transferase in family X of DNA polymerases (Kis range from 5.2-9.5 µM).{30741}  

 

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Description

An irreversible inhibitor of GAPDH (Ki = 1.6 µM); selectively induces apoptosis in high-glycolytic cancer cells by inhibiting the generation of ATP in the glycolytic pathway; also inhibits mammalian DNA polymerases β and λ as well as terminal deoxynucleotidyl transferase in family X of DNA polymerases (Kis range from 5.2-9.5 µM)

Formal name: (2’S,5aS,6R,9aS)-1,5a,6,7,8,9a-hexahydro-6-(1-methylethyl)-1-oxo-spiro[2-benzoxepin-9(3H),2′-oxirane]-4-carboxylic acid

Synonyms:  Avocettin|BRN 5091359|FO-4443|Koningic Acid

Molecular weight: 280.3

CAS: 57710-57-3

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Antibiotics||Product Type|Biochemicals|Natural Products|Microbial Metabolites||Product Type|Biochemicals|Small Molecule Inhibitors|Nucleic Acid Turnover/Signaling||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Metabolism||Research Area|Endocrinology & Metabolism|Carbohydrate Metabolism

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