KMH-233 |
رقم الكتالوجGC61845 |
KMH-233 ، مثبط 1 (LAT1) قوي وقابل للعكس وانتقائي لنقل الأحماض الأمينية ، يمنع امتصاص LAT1 الركيزة ، l-leucin (IC50 = 18 ميكرومتر) وكذلك نمو الخلايايعمل KMH-233 على تقوية فعالية Bestatin و Cisplatin بشكل كبير حتى بتركيزات منخفضة (25 ميكرومتر)
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Cas No.: 1941174-13-5
Sample solution is provided at 25 µL, 10mM.
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].
References:
[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.
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