KL-11743

• 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].

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  GLUT1; GLUT2; GLUT3; GLUT4

• CAS Number:

  [1369452-53-8]