1. Membrane Transporter/Ion Channel Apoptosis
  2. GLUT Apoptosis
  3. Glutor

Glutor is a selective GLUT 1/2/3 inhibitor that can suppress glucose uptake. Glutor can inhibit glycolysis and has anti-tumor activity, inducing cell apoptosis.

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Glutor Chemical Structure

Glutor Chemical Structure

CAS No. : 2561471-22-3

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Description

Glutor is a selective GLUT 1/2/3 inhibitor that can suppress glucose uptake. Glutor can inhibit glycolysis and has anti-tumor activity, inducing cell apoptosis[1][2].

In Vitro

Glutor reduced the uptake of 2-DG with similar efficacy in different cancer cell lines, such as HCT116 (IC50 = 10.8 nM), UM-UC-3 (IC50 = 8.3 nM), UO-31 (IC50 = 3.6 nM), and MIA PaCa-2 (IC50 = 1.1 nM)[1].
Glutor effectively decreases glycolysis in HCT116 cells, thereby preventing the reduction of oxidative phosphorylation rates after glucose addition[1].
Glutor inhibits the proliferation of malignant cell lines without harming the growth of non-malignant peripheral blood mononuclear cells (PBMCs) and IMR-90 embryonic lung cells[1].
Glutor (0.5μM, 24-48h) suppresses the glucose uptake-induced upregulation of GLUT-1 and GLUT-3 expression[1].
Glutor (0.0001-1μM, 24h) inhibits the number of DL cells in a time- and dose-dependent manner, with an Glutor reduced the uptake of 2-DG with similar efficacy in different cancer cell lines, such as HCT116 (IC50 = 10.8 nM), UM-UC-3 (IC50 = 8.3 nM), UO-31 (IC50 = 3.6 nM), and MIA PaCa-2 (IC50 = 1.1 nM)[1].
Glutor effectively decreases glycolysis in HCT116 cells, thereby preventing the reduction of oxidative phosphorylation rates after glucose addition[1].
Glutor inhibits the proliferation of malignant cell lines without harming the growth of non-malignant peripheral blood mononuclear cells (PBMCs) and IMR-90 embryonic lung cells[1].
Glutor (0.5 μM, 24-48 h) suppresses the glucose uptake-induced upregulation of GLUT-1 and GLUT-3 expression[1].
Glutor (0.0001-1 μM, 24 h) inhibits the number of DL cells in a time- and dose-dependent manner, with an IC50 of 0.01 μM, showing no cytotoxicity to thymocytes[2].
Glutor (0.01-1 μM, 24 h) induces apoptosis in DL cells[2].
Glutor (0.01-1 μM, 24 h) links tumor inhibition to the regulation of cell survival and metabolic regulatory molecules[2].
Glutor (0.01-1 μM, 2 h) increases the expression of reactive oxygen species (ROS) in DL cells[2].
Glutor (0.01-1 μM, 24 h) triggers depolarization of the mitochondrial membrane, disrupting the pH homeostasis of DL cells and altering their chemical sensitivity[2].
of 0.01 μM, showing no cytotoxicity to thymocytes[2].
Glutor (0.01-1 μM, 24 h) induces apoptosis in DL cells[2].
Glutor (0.01-1 μM, 24 h) links tumor inhibition to the regulation of cell survival and metabolic regulatory molecules[2].
Glutor (0.01-1 μM, 2 h) increases the expression of reactive oxygen species (ROS) in DL cells[2].
Glutor (0.01-1 μM, 24 h) triggers depolarization of the mitochondrial membrane, disrupting the pH homeostasis of DL cells and altering their chemical sensitivity[2].

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

Real Time qPCR[1]

Cell Line: DLD-1
Concentration: 0.5 μM
Incubation Time: 24, 48 h
Result: Showed under low blood sugar conditions, the levels of GLUT1 and GLUT3 increase.

Western Blot Analysis[1]

Cell Line: DLD-1
Concentration: 0.5 μM
Incubation Time: 24, 48 h
Result: Showed under low blood sugar conditions, the levels of GLUT1 and GLUT3 increase.

Cell Viability Assay[2]

Cell Line: DL
Concentration: 0.0001, 0.001, 0.01, 0.1, 1μM
Incubation Time: 24 h
Result: Showed the number of cells decreases in a dose- and time-dependent manner.

Apoptosis Analysis[2]

Cell Line: DL
Concentration: 0.01 μM
Incubation Time: 24 h
Result: Increased the number of cells with typical apoptotic morphological characteristics.

Western Blot Analysis[2]

Cell Line: DL
Concentration: 0.01 μM
Incubation Time: 24 h
Result: Suppressed the expression of hypoxia-inducible factor 1-alpha (HIF-1a), hexokinase 2 (HK-2), and lactate dehydrogenase A (LDH-A), regulating the expression of cell survival molecules B-cell lymphoma 2 (Bcl-2), Bcl-2-associated X (BAX), and p53. The expression of Bcl-2, transforming growth factor-beta (TGF-b), Cmyc, and heat shock protein 70 (Hsp70) decreased, while the expression of BAX and p53 increased.
Molecular Weight

536.62

Formula

C31H32N6O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@]1(C)N(C(C2=CC(C3=CC=CC=C3)=NN2C1)=O)CC(C=C4)=CC=C4N5CCOCC5)NCC6=CC=CN=C6

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 : 34 mg/mL (63.36 mM; Need ultrasonic and warming; 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 1.8635 mL 9.3176 mL 18.6352 mL
5 mM 0.3727 mL 1.8635 mL 3.7270 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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Purity & Documentation

Purity: ≥99.0%

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 1.8635 mL 9.3176 mL 18.6352 mL 46.5879 mL
5 mM 0.3727 mL 1.8635 mL 3.7270 mL 9.3176 mL
10 mM 0.1864 mL 0.9318 mL 1.8635 mL 4.6588 mL
15 mM 0.1242 mL 0.6212 mL 1.2423 mL 3.1059 mL
20 mM 0.0932 mL 0.4659 mL 0.9318 mL 2.3294 mL
25 mM 0.0745 mL 0.3727 mL 0.7454 mL 1.8635 mL
30 mM 0.0621 mL 0.3106 mL 0.6212 mL 1.5529 mL
40 mM 0.0466 mL 0.2329 mL 0.4659 mL 1.1647 mL
50 mM 0.0373 mL 0.1864 mL 0.3727 mL 0.9318 mL
60 mM 0.0311 mL 0.1553 mL 0.3106 mL 0.7765 mL
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  • 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.

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