JPH203 | LAT1 inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $95.00 | ||
| 25 mg | $315.00 |
JPH203 (1597402-27-1) is a selective L-type amino acid transporter 1 inhibitor (LAT1 or SLC7A5; IC50 = 140 nM for 14C-leucine uptake in S2-hLAT1 cells, and 60 nM for HT29 human colon adenocarcinoma cells: growth inhibition IC50’s = 16.4 µM and 4.1 µM respectively for S2 and HT29 cells).1 Also active in HT-29 mouse xenograft models. JPH203 is active in a variety of cancer models and has progressed to clinical trials.2 It sensitized A549 and MIA Paca-2 cells to radiation by enhancing cellular senescence via mTOR downregulation3 and sensitized EGFR-expressing cancer cell lines to gefitinib therapy4. JPH203 treatment of non-small cell lung cancer cells led to downregulation of PD-L1 suggesting that LAT1 inhibition may help overcome the immune suppressive tumor microenvironment.5
References/Citations:
- Oda et al. (2010) L-type amino acid transporter 1 inhibitors inhibit tumor cell growth; Cancer Sci. 101 173
- Kanai (2022) Amino acid transporter LAT1 (SLC7A5) as a molecular target for cancer diagnosis and therapeutics; Pharmacol. Ther. 230 107964
- Bo et al. (2021) LAT1 inhibitor JPH203 sensitizes cancer cells to radiation by enhancing radiation-induced cellular senescence; Transl. Oncol. 14 101212
- Saito et al. (2018), Amino acid starvation culture condition sensitizes EGFR-expressing cancer cell lines to gefitinib-mediated cytotoxicity by inducing atypical necroptosis; Int. J. Oncol. 52 1165
- Liu et al. (2021), L-Type Amino Acid Transporter 1 Regulates Cancer Stemness and the Expression of Programmed Cell Death 1 Ligand 1 in Lung Cancer Cells; Int. J. Mol. Sci. 22 10955
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
JPH203 (1597402-27-1) is a selective L-type amino acid transporter 1 inhibitor (LAT1 or SLC7A5; IC50 = 140 nM for 14C-leucine uptake in S2-hLAT1 cells, and 60 nM for HT29 human colon adenocarcinoma cells: growth inhibition IC50’s = 16.4 µM and 4.1 µM respectively for S2 and HT29 cells).1 Also active in HT-29 mouse xenograft models. JPH203 is active in a variety of cancer models and has progressed to clinical trials.2 It sensitized A549 and MIA Paca-2 cells to radiation by enhancing cellular senescence via mTOR downregulation3 and sensitized EGFR-expressing cancer cell lines to gefitinib therapy4. JPH203 treatment of non-small cell lung cancer cells led to downregulation of PD-L1 suggesting that LAT1 inhibition may help overcome the immune suppressive tumor microenvironment.5
References/Citations:
- Oda et al. (2010) L-type amino acid transporter 1 inhibitors inhibit tumor cell growth; Cancer Sci. 101 173
- Kanai (2022) Amino acid transporter LAT1 (SLC7A5) as a molecular target for cancer diagnosis and therapeutics; Pharmacol. Ther. 230 107964
- Bo et al. (2021) LAT1 inhibitor JPH203 sensitizes cancer cells to radiation by enhancing radiation-induced cellular senescence; Transl. Oncol. 14 101212
- Saito et al. (2018), Amino acid starvation culture condition sensitizes EGFR-expressing cancer cell lines to gefitinib-mediated cytotoxicity by inducing atypical necroptosis; Int. J. Oncol. 52 1165
- Liu et al. (2021), L-Type Amino Acid Transporter 1 Regulates Cancer Stemness and the Expression of Programmed Cell Death 1 Ligand 1 in Lung Cancer Cells; Int. J. Mol. Sci. 22 10955
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