KMH-233 是一种有效，可逆的且选择性的 l 型氨基酸转运蛋白 1 (LAT1) 抑制剂，可抑制LAT1底物，l-leucin 的摄取 (IC50=18 µM) 以及细胞生长。即使在低浓度 (25 µM) 下，KMH-233 仍可显着增强 Bestatin 和顺铂的疗效。
货号:ajcx32566
CAS:1941174-13-5
分子式:C32H25N7O5
分子量：587.58
溶解度:DMSO : 100 mg/mL (170.19 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 µM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 µM)[1].

KMH-233 is able to inhibit binding and transport of essential neutral amino acids and thus, inhibit the cell growth of cancer cells[1].KMH-233 shows a significant reduction of cell growth with an IC50 of 124 µM[1].KMH-233 is effective and able to potentiate the anti-proliferative efficacy of Bestatin (100 µM) and Cisplatin (100 µM) at a lower concentration of 25 µM, inhibiting cell growth 53% and 50%, respectively[1].

参考文献:
[1]. Huttunen KM, et al. A Selective and Slowly Reversible Inhibitor of l-Type Amino Acid Transporter 1 (LAT1) Potentiates Antiproliferative Drug Efficacy in Cancer Cells. J Med Chem. 2016;59(12):5740-5751.