1. Membrane Transporter/Ion Channel
    Antibody-drug Conjugate/ADC Related
    Apoptosis
  2. GLUT
    ADC Cytotoxin
    Apoptosis
  3. Glucopiericidin A

Glucopiericidin A 

目录号: HY-133541
产品使用指南

Glucopiericidin A 是一种天然的哌啶菌素化合物,从海洋衍生的链霉菌菌株获得。Glucopiericidin A 充当葡萄糖转运蛋白 (GLUT) 的化学探针,可以抑制糖酵解。Glucopiericidin A 与 Piericidin A (PA; HY-114936) 协同可以抑制 ATP 依赖性丝状伪足突起,而单独使用没有作用。Glucopiericidin A 通过增加 PRDX1 降低活性氧 (ROS) 水平来诱导细胞凋亡,同时在 ACHN 小鼠异种移植物中也表现出有效的抗肿瘤功效。

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Glucopiericidin A Chemical Structure

Glucopiericidin A Chemical Structure

CAS No. : 108073-65-0

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Description

Glucopiericidin A is a natural piericidin compound obtained from a marine-derived Streptomyces strain. Glucopiericidin A serves as a glucose transporter (GLUT) chemical probe and suppresses glycolysis. Glucopiericidin A inhibits ATP-dependent filopodia protrusion with Piericidin A (PA; HY-114936) and has no effect alone. Glucopiericidin A induces cell apoptosis through reducing the reactive oxygen species (ROS) level by increasing PRDX1 and exhibits potent antitumor efficacy in ACHN mice xenografts[1][2].

In Vitro

Glucopiericidin A has cytotoxicities against three renal carcinoma cell lines, ACHN (IC50=0.21 μM), OS-RC-2 (IC50>100 μM), and 786-O (IC50>100 μM), as well as a normal renal cell line, HK-2 (IC50>100 μM)[2].
Glucopiericidin A (25, 50 nM; 24 h) causes the upregulation of PRDX1 in ACHN cells[2].
Glucopiericidin A (25, 50 nM; 24 h) not only raises the expression of mRNA and protein of PRDX1 but also forces it into the nucleus[2].
Glucopiericidin A (25, 50 nM; 24 h) reduces ROS in normal ACHN cells[2].
Neither Glucopiericidin A (GPA) nor Piericidin A (PA) alone, at concentrations up to 500 nM and 2.3 mM, respectively, shows inhibitory activity. When combined, much lower concentrations of GPA (17 nM) and PA (0.68 nM) produces inhibition of filopodia protrusion[1].

Western Blot Analysis[2]

Cell Line: ACHN cells
Concentration: 25 and 50 nM
Incubation Time: 24 hours
Result: Caused the upregulation of PRDX1 in ACHN cells.

RT-PCR[2]

Cell Line: ACHN cells
Concentration: 25 and 50 nM
Incubation Time: 24 hours
Result: Not only raised the expression of mRNA and protein of PRDX1 but also forced it into the nucleus
In Vivo

Glucopiericidin A (0.8 mg/kg/day; IP; for three weeks) significantly reduces the final tumor weight of the mice[2].

Animal Model: Nude mice bearing ACHN tumor xenografts[2]
Dosage: 0.8 mg/kg
Administration: IP; daily; for three weeks
Result: Significantly reduced the final tumor weight of the mice.
Increased the mRNA and protein expression of PRDX1 in tumor tissues.
Molecular Weight

577.71

Formula

C₃₁H₄₇NO₉

CAS No.

108073-65-0

SMILES

O[C@H]([C@H]([C@@H]([C@@H](CO)O1)O)O)[C@@H]1O[C@@H](/C(C)=C/C)[C@H](C)/C=C(C)/C=C/C/C(C)=C/CC2=NC(OC)=C(OC)C(O)=C2C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
  • 摩尔计算器

  • 稀释计算器

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Keywords:

Glucopiericidin AGLUTADC CytotoxinApoptosisGlucose transporter glucosetransporterglycolysisfilopodiaprotrusionPiericidin AreactiveoxygenspeciesPRDX1ACHNOS-RC-2786-OHK-2Inhibitorinhibitorinhibit

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产品名称:
Glucopiericidin A
目录号:
HY-133541
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