Heptelidic acid

Heptelidic acid (Koningic acid) is a sesquiterpene antibiotic. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases . Koningic acid (KA) is a specific GAPDH inhibitor with an IC 50 of 90 μM .In VitroHeptelidic 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. Heptelidic acid inhibits Etoposide-induced apoptosis in human leukemia U937 cells.Heptelidic acid inhibits caspase- 3 induction in U937 cells with an IC 50 value of 40 μM after 8 h of Etoposide treatment. 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 IC 50 =5 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HEK293T cells expressing KAr-GAPDH or EV (top left) Concentration: 0.1, 1, 10, 100, 1000 μM Incubation Time: 24 hours Result: IC 50 =5 μM.In VivoHeptelidic acid (Koningic acid; KA) is bioavailable and induces dynamic changes to glycolysis in vivo. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-week old female Foxn1 nu mice bearing BT-474 tumorDosage: 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).Form:Solid. Molecular Formula: C15H20O5 Molecular Weight: 280.32 PubChem CID: 10945834 Isomeric SMILES: CC(C)[C@H]1CC[C@@]2(CO2)[C@@H]3[C@@H]1C=C(COC3=O)C(=O)O