Description
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).
Product information
CAS Number: 1941174-13-5
Molecular Weight: 587.58
Formula: C32H25N7O5
Chemical Name: (2S)-2-amino-3-{3-[(10,12-dicyano-11-{4-[(methylcarbamoyl)methoxy]phenyl}-1,8-diazatricyclo[7.4.0.0²,⁷]trideca-2,4,6,8,10,12-hexaen-13-yl)carbamoyl]phenyl}propanoic acid
Smiles: CNC(=O)COC1C=CC(=CC=1)C1=C(C#N)C2=NC3=CC=CC=C3N2C(NC(=O)C2=CC(C[C@H](N)C(O)=O)=CC=C2)=C1C#N
InChiKey: MLNOOVGSMCJSCE-DEOSSOPVSA-N
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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (170.19 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
KMH-233 is able to inhibit binding and transport of essential neutral amino acids and thus, inhibit the cell growth of cancer cells. KMH-233 shows a significant reduction of cell growth with an IC50 of 124 µM. 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.
Products are for research use only. Not for human use.
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