1. Membrane Transporter/Ion Channel
  2. GLUT
  3. DRB18

DRB18 

Cat. No.: HY-145963
Handling Instructions

DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor activity.

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

DRB18 Chemical Structure

DRB18 Chemical Structure

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Description

DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor activity[1].

IC50 & Target

GLUT[1]

In Vitro

DRB18 (0-10 μM; 30 min) reduces glucose uptake in GLUT1-4-expressed HEK293 cell lines in a dose-dependent manner with IC50s varying from ~ 900 nM to ~ 9 μM[1].
DRB18 (5 and 10 μM; 72 hours) causes cell cycle arrest in the G1/S phase transition[1].
DRB18 (5 and 10 μM; 72 hours) increases ROS levels in A549 cells[1].
DRB18 (5 and 10 μM; 72 hours) reduces expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner[1].

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

Cell Proliferation Assay

Cell Line: GLUT1-4-expressed HEK293 cell lines[1]
Concentration: 0-10 μM
Incubation Time: 30 min
Result: Reduced glucose uptake in these cell lines in a dose-dependent manner with IC50s varying from ~ 900 nM to ~ 9 μM.

Cell Cycle Analysis

Cell Line: A549[1]
Concentration: 5 and 10 μM
Incubation Time: 72 hours
Result: Caused cell cycle arrest in the G1/S phase transition.

Western Blot Analysis

Cell Line: A549[1]
Concentration: 5 and 10 μM
Incubation Time: 72 hours
Result: Reduced expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner.

Western Blot Analysis

Cell Line: A549[1]
Concentration: 5 and 10 μM
Incubation Time: 72 hours
Result: Reduced expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner.
In Vivo

DRB18 (10 mg/kg; IP; thrice a week for 5 weeks) inhibits tumors volume by 44% and tumors weight by 43%[1].

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

Animal Model: Male NU/J nude mice (3-4 weeks; tumor cell-injected)[1]
Dosage: 10 mg/kg
Administration: IP; thrice a week for 5 weeks
Result: The tumors were 44% smaller by volume and 43% smaller by weight, also showed DRB18 decreased expression of GLUT1-4 (Fig. 5f) and reduced proliferative capacity within the xenografted tumor.
Molecular Weight

382.88

Formula

C22H23ClN2O2

SMILES

ClC1=CC(NCC2=CC(O)=C(C)C=C2)=C(NCC3=CC=C(C)C(O)=C3)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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DRB18
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HY-145963
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