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

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.

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
SMILES

COC1=NC(C/C=C(C)/C/C=C/C(C)=C/[C@@H](C)[C@H](/C(C)=C/C)O[C@@H]2O[C@@H]([C@H]([C@@H]([C@H]2O)O)O)CO)=C(C)C(O)=C1OC

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

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Glucopiericidin A
Cat. No.:
HY-133541
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