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

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.

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DRB18 Chemical Structure

DRB18 Chemical Structure

CAS No. : 2863686-81-9

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Solid + Solvent
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

DRB18 Related Antibodies

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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].

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

DRB18 Related Antibodies

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].

MedChemExpress (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
CAS No.
Appearance

Solid

Color

White to yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (130.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6118 mL 13.0589 mL 26.1178 mL
5 mM 0.5224 mL 2.6118 mL 5.2236 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.81%

COA (251 KB) HNMR (257 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6118 mL 13.0589 mL 26.1178 mL 65.2946 mL
5 mM 0.5224 mL 2.6118 mL 5.2236 mL 13.0589 mL
10 mM 0.2612 mL 1.3059 mL 2.6118 mL 6.5295 mL
15 mM 0.1741 mL 0.8706 mL 1.7412 mL 4.3530 mL
20 mM 0.1306 mL 0.6529 mL 1.3059 mL 3.2647 mL
25 mM 0.1045 mL 0.5224 mL 1.0447 mL 2.6118 mL
30 mM 0.0871 mL 0.4353 mL 0.8706 mL 2.1765 mL
40 mM 0.0653 mL 0.3265 mL 0.6529 mL 1.6324 mL
50 mM 0.0522 mL 0.2612 mL 0.5224 mL 1.3059 mL
60 mM 0.0435 mL 0.2176 mL 0.4353 mL 1.0882 mL
80 mM 0.0326 mL 0.1632 mL 0.3265 mL 0.8162 mL
100 mM 0.0261 mL 0.1306 mL 0.2612 mL 0.6529 mL
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DRB18 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

DRB182863686-81-9DRB 18DRB-18GLUTGlucose transporterGlucose-based metabolismAnticancerOxidative stressNecrotic cell deathA549 cellsInhibitorinhibitorinhibit

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