CAS No. : 1037592-40-7

(Synonyms: KYT-0353)

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Cat. No. : HY-100868
M.Wt: 472.32
Formula: C23H19Cl2N3O4
Purity: >98 %
Storage: at -20℃ 3 years
Solubility: 10 mM in DMSO
Introduction of 1037592-40-7 :

JPH203 is a potent and selective L-type amino acid transporter 1 inhibitor (LAT1), used for cancer research. In Vitro: JPH203 inhibits 14C-leucine uptake and cell growth in human colon cancer-derived HT-29 cells; IC50s are 0.06 μM and 4.1 μM, respectively. JPH203 also inhibits 14C-leucine uptake in mouse renal proximal tubule cells expressing l-type amino acid transporter 1, and inhibits cell growth; IC50s are 0.14 μM and 16.4 μM, respectively[1]. Growth dose response demonstrates an extreme sensitivity of CD98KO cells to JPH203 with an IC50 of 1.0 μM, whereas the IC50 for WT cells is 35-fold higher. Furthermore, 5.0 μM of JPH203 completely abolishes the growth of CD98KO cells. JPH203 treatment increases the GCN2 pathway, reduces mTORC1 activity, and inhibits proliferation in all of the cell lines tested[2]. JPH203 (0.001-100 μM) inhibits the [14C]L-leucine (1.0 mM) uptake slightly in the NHOKs. JPH203 (0.01-30 mM) completely inhibits the proliferation of YD-38 cells in a dose- and time-dependent manner[3]. In Vivo: JPH203 (12.5 mg/kg and 25.0 mg/kg, i.v.) shows statistically significant growth inhibition against HT-29 tumors transplanted to nude mice with maximal inhibition ratios of 65.9% and 77.2%, respectively[1].

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