产品
编 号:F395189
分子式:C15H20O5
分子量:280.32
产品类型
结构图
CAS No: 57710-57-3
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产品详情
生物活性:
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 IC50of 90 μM.
体内研究:
Heptelidic acid (Koningic acid; KA) is bioavailable and induces dynamic changes to glycolysis in vivo.Animal Model:6-week old female Foxn1nu mice bearing BT-474 tumor
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).
体外研究:
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.Heptelidic acid inhibits Etoposide-induced apoptosis in human leukemia U937 cells.Heptelidic acid inhibits caspase- 3 induction in U937 cells with an IC50 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 IC50=5 μM.