Heptelidic acid 萜烯七脂酸; Koningic acid

产品编号:Bellancom-120838| CAS NO:57710-57-3| 分子式:C15H20O5| 分子量:280.32

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Bellancom-120838
10400.00 杭州 北京(现货)

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Heptelidic acid 萜烯七脂酸; Koningic acid

产品介绍 Heptelidic acid (Koningic acid) 是一种倍半萜类抗生素 (antibiotic)。Heptelidic acid 通过下调 caspase 从而抑制 Etoposide 诱导的细胞凋亡。Koningic acid (KA) 是一种特异性 GAPDH 抑制剂,IC50 为 90 μM。
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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.
体内研究
(In Vivo)

Heptelidic acid (Koningic acid; KA) is bioavailable and induces dynamic changes to glycolysis in vivo.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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).
体内研究

Heptelidic acid (Koningic acid; KA) is bioavailable and induces dynamic changes to glycolysis in vivo.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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).
体内研究

Heptelidic acid (Koningic acid; KA) is bioavailable and induces dynamic changes to glycolysis in vivo.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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).
性状Solid
溶解性数据
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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