Heptelidic acid(Synonyms: 萜烯七脂酸; Koningic acid)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Heptelidic acid (Synonyms: 萜烯七脂酸; Koningic acid)

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。

Heptelidic acid(Synonyms: 萜烯七脂酸; Koningic acid)

Heptelidic acid Chemical Structure

CAS No. : 57710-57-3

规格 是否有货
1 mg 询价

* Please select Quantity before adding items.

生物活性

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].

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 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 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[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

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

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Y Itoh, et al. A new sesquiterpene antibiotic, heptelidic acid producing organisms, fermentation, isolation and characterization. J Antibiot (Tokyo). 1980 May;33(5):468-73.

    [2]. Jin Hee Kim, et al. Heptelidic acid, a sesquiterpene lactone, inhibits Etoposide-induced apoptosis in human leukemia U937 cells. J Microbiol Biotechnol. 2009 Aug;19(8):787-91.

    [3]. Maria V Liberti, et al. A Predictive Model for Selective Targeting of the Warburg Effect through GAPDH Inhibition with a Natural Product. Cell Metab. 2017 Oct 3;26(4):648-659.e8.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务