JPH203

JPH203 is an inhibitor of L-type amino acid transporter 1 (LAT1, IC50 = 0.14 µM for 14C-leucine uptake in S2 cells expressing the human transporter). It is selective for LAT1 over LAT2 (IC50 = >10 µM). JPH203 inhibits 14C-leucine uptake by, and growth of, HT-29 cells (IC50s = 0.06 and 4.1 µM, respectively). It induces apoptosis and increases levels of cleaved caspase-3, caspase-7, caspase-9, and poly(ADP-ribose) polymerase (PARP) in YD-38 oral cancer cells when used at a concentration of 3 mM. JPH203 (6.3, 12.5, and 25 mg/kg) reduces tumor growth in an HT-29 mouse xenograft model.Formal Name: O-[(5-amino-2-phenyl-7-benzoxazolyl)methyl]-3,5-dichloro-L-tyrosine. CAS Number: 1037592-40-7. Synonyms: KYT-0353. Molecular Formula: C23H19Cl2N3O4. Formula Weight: 472.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml. lambdamax: 277 nm. SMILES: NC1=CC(COC2=C(Cl)C=C(C[C@H](N)C(O)=O)C=C2Cl)=C3C(N=C(C4=CC=CC=C4)O3)=C1. InChi Code: InChI=1S/C23H19Cl2N3O4/c24-16-6-12(8-18(27)23(29)30)7-17(25)21(16)31-11-14-9-15(26)10-19-20(14)32-22(28-19)13-4-2-1-3-5-13/h1-7,9-10,18H,8,11,26-27H2,(H,29,30)/t18-/m0/s1. InChi Key: XNRZJPQTMQZBCE-SFHVURJKSA-N.