Art. -Nr.: HY-145597

KL-11743

Name: KL-11743
Brand: MedChemExpress
SKU: HY-145597
Price: 142.00 USD
Availability: InStock
Rating: 5 (8 reviews)

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

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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Reinheit : 99.40%
CAS. Nr.: 1369452-53-8
Formel: C₃₀H₃₀N₆O₃
Molecular Weight:522.60

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

KL-11743 Chemical Structure

CAS. Nr.: 1369452-53-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[3]

GLUT1

115 nM (IC₅₀)

GLUT2

137 nM (IC₅₀)

GLUT3

90 nM (IC₅₀)

GLUT4

68 nM (IC₅₀)

Alle GLUT Isoform-spezifische Produkte anzeigen :

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.

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.

Related Protocols :

Chemical Information

CAS. Nr. 1369452-53-8
Appearance Solid
Molecular Weight 522.60
Formel C₃₀H₃₀N₆O₃
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (8)

All Cell Proliferation/Viability AssayIF

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Journal Impact Factor

Adv Sci (Weinh)

Glucose Deprivation-Induced Disulfidptosis via the SLC7A11-INF2 Axis: Pan-Cancer Prognostic Exploration and Therapeutic Validation. [Abstract]

2025 Jul 25:e08556. PMID: 40709550

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.
Acta Biomater

A tumor microenvironment-responsive nanocomposite for enhanced copper retention and hypoxia reversal to promote cuproptosis in tumor treatment. [Abstract]

2025 Aug:202:463-475. PMID: 40618974
Bioorg Chem

A mitochondria-targeting glutathione fluorescent probe reveals distinct mitochondria-endoplasmic reticulum contact between disulfidptosis and ferroptosis. [Abstract]

2026 Feb:169:109437. PMID: 41453306

KL-11743 purchased from MedChemExpress. Usage Cited in: Bioorg Chem. 2026 Feb: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).
Sci Rep

2026 Jul 28;16(1):24140. PMID: 42557295
Viruses

Identification of Oncolytic Avian Reovirus Receptors in B16-F10 Cells and the Signaling-Mediated Pathways Involved in Viral Entry. [Abstract]

2026 Mar 12;18(3):350. PMID: 41902258
Vita

2026 Aug 25.
bioRxiv

Citrate Compartmentalization Controls Calcium-Dependent Cytokine Production in Effector T Cells. [Abstract]

2026 Jun 12:2026.06.11.731694. PMID: 42327233
Biomed Pharmacother

PIEZO1 as a new target for hyperglycemic stress-induced neuropathic injury: The potential therapeutic role of bezafibrate. [Abstract]

2024 Jul:176:116837. PMID: 38815290

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.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9135 mL

9.5675 mL

19.1351 mL

5 mM

0.3827 mL

1.9135 mL

3.8270 mL

10 mM

0.1914 mL

0.9568 mL

1.9135 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

Working Solution

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Liu KG, et, al. Discovery and Optimization of Glucose Uptake Inhibitors. J Med Chem. 2020 May 28;63(10):5201-5211. [Content Brief]

[2]. Liu X, et, al. Cystine transporter regulation of pentose phosphate pathway dependency and disulfide stress exposes a targetable metabolic vulnerability in cancer. Nat Cell Biol. 2020 Apr;22(4):476-486. [Content Brief]

[3]. Olszewski K, et, al. Inhibition of glucose transport synergizes with chemical or genetic disruption of mitochondrial metabolism and suppresses TCA cycle-deficient tumors. Cell Chem Biol. 2021 Oct 22;S2451-9456(21)00441-4. [Content Brief]

[4]. Koppula P, et, al. KEAP1 deficiency drives glucose dependency and sensitizes lung cancer cells and tumors to GLUT inhibition. iScience. 2021 May 25;24(6):102649. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

KL-11743

8 Cited Publications

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KL-11743

Publications Citing Use of MedChemExpress (MCE) KL-11743

Alle GLUT Isoform-spezifische Produkte anzeigen