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[1][2][3][4].

Product Specifications

CAS Number

[1369452-53-8]

UNSPSC

12352005

Target

Disulfidptosis; GLUT

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Cancer; Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/kl-11743.html

Purity

99.40

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

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

Molecular Formula

C30H30N6O3

Molecular Weight

522.60

References & Citations

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