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^[1][2].

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].

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

577.71

C₃₁H₄₇NO₉

108073-65-0

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

Room temperature in continental US; may vary elsewhere.

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• [1]. Mitsuhiro Kitagawa, et al. Metabolomic identification of the target of the filopodia protrusion inhibitor glucopiericidin A. Chem Biol. 2010 Sep 24;17(9):989-98.

  [2]. Xuefeng Zhou, et al. Exploring the Natural Piericidins as Anti-Renal Cell Carcinoma Agents Targeting Peroxiredoxin 1. J Med Chem. 2019 Aug 8;62(15):7058-7069.