An inhibitor of LAT1
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Alternative(s)
29715JPH203
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JPH203 (hydrochloride)

Item No. 36053

Technical Information
Formal Name
O-[(5-amino-2-phenyl-7-benzoxazolyl)methyl]-3,5-dichloro-L-tyrosine, dihydrochloride
CAS Number
1597402-27-1
Synonyms
  • KYT-0353
Molecular Formula
C23H19Cl2N3O4 • 2HCl
Formula Weight
Purity
≥98%
Formulation
A solid
DMF: Slightly solubleDMSO: Slightly solubleEthanol: Slightly soluble
SMILES
ClC(C=C(C=C1Cl)C[C@H](N)C(O)=O)=C1OCC2=C3C(N=C(C4=CC=CC=C4)O3)=CC(N)=C2.Cl.Cl
InChi Code
InChI=1S/C23H19Cl2N3O4.2ClH/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);2*1H/t18-;;/m0../s1
InChi Key
MJSAOPNUSNNYQL-NTEVMMBTSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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).1 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.2 JPH203 (6.3, 12.5, and 25 mg/kg) reduces tumor growth in an HT-29 mouse xenograft model.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Oda, K., Hosoda, N., Endo, H., et alL-type amino acid transporter 1 inhibitors inhibit tumor cell growth. Cancer Sci. 101(1), 173-179 (2010).

    2. Yun, D.-W., Lee, S.A., Park, M.-G., et alJPH203, an L-type amino acid transporter 1–selective compound, induces apoptosis of YD-38 human oral cancer cells. J. Pharmacol. Sci. 124(2), 208-217 (2014).