2. Membrane Transporter/Ion Channel
  3. GLUT
  4. KL-11743

KL-11743 is a potent, orally active, and glucose-competitive inhibitor of the class I glucose transporters, with IC50s of 115, 137, 90, and 68 nM for GLUT1, GLUT2, GLUT3, and GLUT4, respectively. KL-11743 specifically blocks glucose metabolism. KL-11743 can synergize with electron transport inhibitors to induce cell death. In addition, KL-11743 can induce the formation of disulfide bonds in actin cytoskeletal proteins, leading to the occurrence of cellular disulfidptosis.

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KL-11743 Chemical Structure

KL-11743 Chemical Structure

CAS No. : 1369452-53-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 345 In-stock
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10 mM * 1 mL in DMSO USD 345 In-stock
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1 mg USD 142 In-stock
5 mg USD 300 In-stock
10 mg USD 480 In-stock
25 mg USD 795 In-stock
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100 mg USD 1540 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

KL-11743 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE KL-11743

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View All Isoforms
GLUT1 GLUT2 GLUT3 GLUT4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

KL-11743 is a potent, orally active, and glucose-competitive inhibitor of the class I glucose transporters, with IC50s of 115, 137, 90, and 68 nM for GLUT1, GLUT2, GLUT3, and GLUT4, respectively. KL-11743 specifically blocks glucose metabolism. KL-11743 can synergize with electron transport inhibitors to induce cell death. In addition, KL-11743 can induce the formation of disulfide bonds in actin cytoskeletal proteins, leading to the occurrence of cellular disulfidptosis[1][2][3][4].

IC50 & Target[3]

GLUT1

115 nM (IC50)

GLUT2

137 nM (IC50)

GLUT3

90 nM (IC50)

GLUT4

68 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HT-1080 IC50
150 nM
Compound: 8
Inhibition of oligomycin-treated GLUT in human HT1080 cells assessed as reduction in ATP level measured after 90 mins by Celltiter-glo luminescent assay
Inhibition of oligomycin-treated GLUT in human HT1080 cells assessed as reduction in ATP level measured after 90 mins by Celltiter-glo luminescent assay
[PMID: 32282207]
HT-1080 IC50
268 nM
Compound: 8
Inhibition of GLUT in oligomycin-treated human HT1080 cells assessed as reduction in ATP level measured after 90 mins in presence of 10 mM glucose by Celltiter-glo luminescent assay
Inhibition of GLUT in oligomycin-treated human HT1080 cells assessed as reduction in ATP level measured after 90 mins in presence of 10 mM glucose by Celltiter-glo luminescent assay
[PMID: 32282207]
HT-1080 IC50
33 nM
Compound: 8
Inhibition of GLUT in oligomycin-treated human HT1080 cells assessed as reduction in ATP level measured after 90 mins in presence of 0.37 mM glucose by Celltiter-glo luminescent assay
Inhibition of GLUT in oligomycin-treated human HT1080 cells assessed as reduction in ATP level measured after 90 mins in presence of 0.37 mM glucose by Celltiter-glo luminescent assay
[PMID: 32282207]
In Vitro

KL-11743 (compound 8) competes with glucose for binding to GLUT1, with IC50s of 33 nM and 268 nM at 0.37 mM and 10 mM glucose, respectively[1].
KL-11743 (39-10000 nM; 24-72 h) dose-dependently inhibits the growth of HT-1080 cells, with an IC50 of 677 nM[3].
KL-11743 inhibits the growth of KEAP1-mutant lung cancer cells with more potency compared to KEAP1-WT lung cancer cells[4].
KL-11743 (0.001-10 μM) induces a rapid increase in the phosphorylation of AMPK and acetyl-coenzyme A carboxylase in HT-1080 cells [3].
KL-11743 (2 μM) inhibits glucose uptake in 786-O cells. KL-11743 increases NADP+/NADPH in NCl-H226 cells. KL-11743 induces cell death in SLC7A11-high cancer cell lines (NCl-H226 and UMRC6 cells)[2].
KL-11743 (0.001-10 μM) inhibits both glucose consumption, lactate secretion, and 2DG transport in HT-1080 fibrosarcoma cells, with IC50s of 228, 234, and 87 nM, respectively, and fully inhibited glycolytic ATP production in oligomycin-treated cells with an IC50 of 127 nM[3].

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

KL-11743 Related Antibodies

Cell Viability Assay[3]

Cell Line: HT-1080 cells
Concentration: 39, 78, 156, 312, 625, 1250, 2500, 5000, 10000 nM
Incubation Time: 24, 48, 72 hours
Result: Inhibited the growth of HT-1080 cells in a dose-dependent manner.
In Vivo

KL-11743 (100 mg/kg; i.p. every two days for 5 weeks) decreases the growth of SLC7A11-high NCI-H226 xenograft tumors and was well-tolerated in vivo[2].
KL-11743 (30-100 mg/kg; a single p.o.) significantly elevates blood glucose levels and delays glucose clearance in mice challenged with 5 g/kg glucose[3].
KL-11743 significantly suppresses the growth of KEAP1 KO tumors[4].
Plasma levels of KL-11743 (100 mg/kg; i.p.) are maintained at inhibitory levels for most of the 24-hour dosing period[2].
KL-11743 (p.o) exhibits moderate oral between 30% and 15%, and favorable and dose-linear plasma exposure profile reaching concentrations of approximately 20 μM in mice (10-100 mg/kg) and rats (10-300 mg/kg)[3].
KL-11743 exhibits comparable half-lives ranging between 2.04 and 5.38 h in rats (10 mg/kg for i.v.; 10-300 mg/kg for p.o.), and 1.45-4.75 h in mice (10 mg/kg for i.v. and i.p.; 10-100 mg/kg for p.o.)[3].

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

Animal Model: 4 to 6-week-old athymic nude mice (Foxn1nu/Foxn1nu) were injected with NCI-H226 cells 100 mg/kg[2]
Dosage: 100 mg/kg
Administration: I.p. every two days for 5 weeks
Result: Inhibited the growth of tumors.
Exhibited extensive necrotic cell death.
Decreased PPP intermediate 6-phosphogluconate levels and increased NADP+/NADPH ratio.
Molecular Weight

522.60

Formula

C30H30N6O3
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C(COC1=CC=CC(C2=NC(NC3=CC=C(C4=CNN=C4)C=C3)=C5C=C(OCC)C=CC5=N2)=C1)NC(C)C
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 : 25 mg/mL (47.84 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 1.9135 mL 9.5675 mL 19.1351 mL
5 mM 0.3827 mL 1.9135 mL 3.8270 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.98 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  0.5% Methylcellulose/0.25% Tween-80 in Water

    Solubility: 9.98 mg/mL (19.10 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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 1.9135 mL 9.5675 mL 19.1351 mL 47.8377 mL
5 mM 0.3827 mL 1.9135 mL 3.8270 mL 9.5675 mL
10 mM 0.1914 mL 0.9568 mL 1.9135 mL 4.7838 mL
15 mM 0.1276 mL 0.6378 mL 1.2757 mL 3.1892 mL
20 mM 0.0957 mL 0.4784 mL 0.9568 mL 2.3919 mL
25 mM 0.0765 mL 0.3827 mL 0.7654 mL 1.9135 mL
30 mM 0.0638 mL 0.3189 mL 0.6378 mL 1.5946 mL
40 mM 0.0478 mL 0.2392 mL 0.4784 mL 1.1959 mL
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KL-11743 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:

KL-117431369452-53-8KL11743KL 11743GLUTGlucose transporterglucosetransporterGLUT1GLUT2GLUT3GLUT4Inhibitorinhibitorinhibit

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