Heptelidic acid
Modify Date: 2024-01-13 12:33:14
Heptelidic acid structure
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Common Name | Heptelidic acid | ||
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| CAS Number | 57710-57-3 | Molecular Weight | 280.31600 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C15H20O5 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Heptelidic acidHeptelidic acid (Koningic acid) is a sesquiterpene antibiotic[1]. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases[2]. Koningic acid (KA) is a specific GAPDH inhibitor with an IC50of 90 μM[3]. |
| Name | heptelidic acid |
|---|---|
| Synonym | More Synonyms |
| Description | Heptelidic acid (Koningic acid) is a sesquiterpene antibiotic[1]. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases[2]. Koningic acid (KA) is a specific GAPDH inhibitor with an IC50of 90 μM[3]. |
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| Related Catalog | |
| Target |
Caspase-3 |
| In Vitro | Heptelidic acid is a sesquiterpene antibiotic, found in the culture filtrate of three different strains of fungi isolated from soil samples. Heptelidic acid produces organisms, fermentation, isolation and characterization[1]. Heptelidic acid inhibits Etoposide-induced apoptosis in human leukemia U937 cells[2].Heptelidic acid inhibits caspase- 3 induction in U937 cells with an IC50 value of 40 μM after 8 h of Etoposide treatment[2]. Heptelidic acid (Koningic acid; KA), a natural product obtained from the Trichoderma fungus, can directly bind to the active site of human GAPDH. The expression of T. koningii KAr-GAPDH successfully rescued cell viability in human cells treated with Heptelidic acid. HEK293T cells expressing T. koningii KAr-GAPDH exhibited complete cell viability after treatment with 0-200 μM Heptelidic acid with the IC50=5 μM[3]. Cell Viability Assay[3] Cell Line: HEK293T cells expressing KAr-GAPDH or EV (top left) Concentration: 0.1, 1, 10, 100, 1000 μM Incubation Time: 24 hours Result: IC50=5 μM. |
| In Vivo | Heptelidic acid (Koningic acid; KA) is bioavailable and induces dynamic changes to glycolysis in vivo[3]. Animal Model: 6-week old female Foxn1nu mice bearing BT-474 tumor[3] Dosage: 1, 2.5, 5, and 10 mg/kg Administration: Daily intraperitoneal (IP) injections, 24 hours Result: 1 mg/kg was determined to be the maximum tolerated dose (MTD) based upon behavioral monitoring and adverse events at higher doses (hemolysis, hematuria, and anemia). |
| References |
| Molecular Formula | C15H20O5 |
|---|---|
| Molecular Weight | 280.31600 |
| Exact Mass | 280.13100 |
| PSA | 76.13000 |
| LogP | 1.62160 |
| (+)-heptelidic acid |
| 1,5a,6,7,8,9a-hexahydro-6-(1-methyl-ethyl)-1-oxo-spiro<2-benzoxepin-9(3H),2'oxirane>-4-carboxylic acid (heptelidic acid) |
| koningic acid |
| 1,5a,6,7,8,9a-hexahydro-6-(1-methyl-ethyl)-1-oxo-spiro[2-benzoxepin-9(3H),2'oxirane]-4-carboxylic acid (heptelidic acid) |