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JPH203 CAS: 1037592-40-7

Category: Inhibitors
Product Name: JPH203
Cat No: I000222
CAS No: 1037592-40-7
Molecular Formula: C23H19Cl2N3O4
Molecular Weight: 472.32
Solubility: Slightly soluble in DMSO
CAS 1037592-40-7,JPH203
  • Description

JPH203 is a potent and selective L-type amino acid transporter 1 inhibitor (LAT1), used for cancer research.
IC50﹠Target:
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].

  • References


[1]. Oda K, et al. L-type amino acid transporter 1 inhibitors inhibit tumor cell growth. Cancer Sci. 2010 Jan;101(1):173-9.
[2]. Yann?Cormerais, et al. 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. ?
[3]. Yun DW, et al. JPH203, an L-type amino acid transporter 1-selective compound, induces apoptosis of YD-38 human oral cancer cells. J Pharmacol Sci. 2014;124(2):208-17.
[4]. Toyoshima J, et al. Investigation of the role of transporters on the hepatic elimination of an LAT1 selective inhibitor JPH203. J Pharm Sci. 2013 Sep;102(9):3228-38.
[5]. Wempe MF, et al. Metabolism and pharmacokinetic studies of JPH203, an L-amino acid transporter 1 (LAT1) selective compound. Drug Metab Pharmacokinet. 2012;27(1):155-61.


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