For research use only. Not for therapeutic Use.
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].
| Catalog Number | I030109 |
| CAS Number | 1941174-13-5 |
| Synonyms | (2S)-2-amino-3-[3-[[2,4-dicyano-3-[4-[2-(methylamino)-2-oxoethoxy]phenyl]pyrido[1,2-a]benzimidazol-1-yl]carbamoyl]phenyl]propanoic acid |
| Molecular Formula | C32H25N7O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C32H25N7O5/c1-36-27(40)17-44-21-11-9-19(10-12-21)28-22(15-33)29-37-25-7-2-3-8-26(25)39(29)30(23(28)16-34)38-31(41)20-6-4-5-18(13-20)14-24(35)32(42)43/h2-13,24H,14,17,35H2,1H3,(H,36,40)(H,38,41)(H,42,43)/t24-/m0/s1 |
| InChIKey | MLNOOVGSMCJSCE-DEOSSOPVSA-N |
| SMILES | CNC(=O)COC1=CC=C(C=C1)C2=C(C3=NC4=CC=CC=C4N3C(=C2C#N)NC(=O)C5=CC=CC(=C5)CC(C(=O)O)N)C#N |
| Reference | [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. |
