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

Glucopiericidin A 

Cat. No.: HY-133541
Handling Instructions

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.

For research use only. We do not sell to patients.

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

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Keywords:

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

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