KYT 0353

Biological Activity

KYT 0353 is a potent and selective inhibitor of L-type amino acid transporter 1 (LAT1) (IC₅₀ = 60 nM for ¹⁴C-leucine uptake in H-29 cells). Also suppreses ¹⁴C-leucine uptake in renal proximal tubule cells expressing LAT1 (IC₅₀ = 140 nM). Displays ~500-fold selectivity for LAT1 over LAT2. Reduces cell viability and induces apoptosis in YD-38 oral cancer cells. Arrests growth in several tumor cell lines. Exhibits growth inhibitory effects on HT-29 cells in vivo.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Investigation of the role of transporters on the hepatic elimination of an LAT1 selective inhibitor JPH203.
   Toyoshima et al.
   J.Pharm.Sci., 2013;102:3228
2. Genetic disruption of the multifunctional CD98/LAT1 complex demonstrates the key role of essential amino acid transport in the control of mTORC1 and tumor growth.
   Cormerais et al.
   Cancer Res., 2016;2016:4481
3. Prostate cancer cells in different androgen receptor status employ different leucine transporters.
   Otsuki et al.
   Prostate, 2017;77:222
4. L-type amino acid transporter 1 inhibitors inhibit tumor cell growth.
   Oda et al.
   Cancer Sci., 2010;101:173

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