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Heptelidic Acid
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Heptelidic Acid图片
CAS NO:57710-57-3
包装:1mg
市场价:10400元

产品名称
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 sesquiterpeneantibiotic[1]. Heptelidic acid inhibits Etoposide-inducedapoptosisvia downregulation ofcaspases[2]. Koningic acid (KA) is a specificGAPDHinhibitor with anIC50of 90 μM[3].

IC50& Target[2]

Caspase-3

 

体外研究
(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 IC50value of 40 μM after 8 h of Etoposide treatment[2].
Heptelidic acid (Koningic acid; KA), a natural product obtained from theTrichodermafungus, can directly bind to the active site of human GAPDH. The expression ofT. koningiiKAr-GAPDH successfully rescued cell viability in human cells treated with Heptelidic acid. HEK293T cells expressingT. koningiiKAr-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.
体内研究
(In Vivo)

Heptelidic acid (Koningic acid; KA) is bioavailable and induces dynamic changes to glycolysis in vivo[3].

Animal Model:6-week old femaleFoxn1numice 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).
分子量

280.32

性状

Solid

Formula

C15H20O5

CAS 号

57710-57-3

中文名称

萜烯七脂酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month