1. Membrane Transporter/Ion Channel Cell Cycle/DNA Damage
  2. GLUT Disulfidptosis
  3. 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.

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

CAS No. : 1369452-53-8

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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    KL-11743 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 25:e08556.  [Abstract]

    The cell viability of SKOV3 cells was evaluated following culture in the specified medium and treatment with DMSO, KL‐11743 (5 µm), or BAY‐876 (5 µm), in the presence or absence of varying concentrations of Irofulven for a duration of 24 h.

    KL-11743 purchased from MedChemExpress. Usage Cited in: Bioorg Chem. 2025 Dec 24:169:109437.  [Abstract]

    Fluorescence images of A549 cells cultured for 12 hours under the following conditions: untreated (control); glucose-free medium (-glucose); 20.0 μM BAY-876 (BAY-876); 2.0 μM KL-11743 (KL-11743); 20.0 μM BAY-876 and 200.0 μM DTT (BAY-876 + DTT); 2.0 μM KL-11743 and 200.0 μM DTT (KL-11743 + DTT).

    KL-11743 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Jul:176:116837.  [Abstract]

    Pretreatment with 0.5 μM KL-11743 for 2 hours, followed by incubation with Glu for 24 hours, yielded representative immunofluorescence images of GLUT3 and PIEZO1.

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    • 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
    33 1
    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]
    HT-1080 IC50
    150 1
    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
    150 1
    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 1
    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
    150 1
    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
    33 1
    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]
    HT-1080 IC50
    268 1
    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
    268 1
    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 1
    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.

    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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    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
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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

    Purity: 99.40%

    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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      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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    Product Name:
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