JPH203

Catalog No.S8667 Synonyms: KYT-0353

JPH203 Chemical Structure

Molecular Weight(MW): 472.32

JPH203, a selective L-type amino acid transporter 1 inhibitor, shows a dramatic inhibition of leucine uptake (IC50=0.06 µM) and cell growth (IC50=4.1 µM) in human colon cancer cells (HT-29), human oral cancer cells (YD-38) and leukemic cells.

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Biological Activity

Description JPH203, a selective L-type amino acid transporter 1 inhibitor, shows a dramatic inhibition of leucine uptake (IC50=0.06 µM) and cell growth (IC50=4.1 µM) in human colon cancer cells (HT-29), human oral cancer cells (YD-38) and leukemic cells.
Targets
LAT1 [1]
(Cell-free assay)
In vitro

JPH203 completely and slightly inhibited the L-Leucine uptake in YD-38 cells (IC50 value: 0.79 μM) and NHOKs (IC50 value: >100 μM), respectively. JPH203 inhibited HT-29 cell growth, generating an apparent IC50 of 4.1 μM, but the JPH203 IC50 concentration (0.06 μM) needed to inhibit the L-Leucine uptake did not inhibit HT-29 cell growth, which represents a 68-fold difference in susceptibility[1]. JPH203 activated the mitochondria-dependent apoptotic signaling pathway by upregulating pro-apoptotic factors, such as Bad, Bax, and Bak, and the active form of caspase-9, and downregulating anti-apoptotic factors, such as Bcl-2 and Bcl-xL in Saos2 human osteosarcoma cells. JPH203 can distinguish relative abundance between LAT1 and LAT2. It has high selectivity for LAT1[2]. JPH203 was metabolically stable in mouse, rat, dog, monkey and human liver microsomal incubations[3]. JPH203 induces both G2/M and G0/G1 cell cycle arrest, as well as reduced the S phase accompanied by altered expression of the proteins in cell cycle progression: cyclin D1, CDK4, and CDK6[4].

Assay
Methods Test Index PMID
Western blot
p53 / Bad / Bcl-2 / Bcl-xl / Bax / Bak / Cleaved caspase / Cleaved PARP ; 

PubMed: 29200902     


Saos2 cells were treated with 3 mM JPH203 for 24 h. Cell lysate was prepared and analyzed by immunoblotting as described in METHODS.

p70S6K / p-P70S6k / p-S6 / S6 / p-ERK / ERK / p-AKT / AKT'; 

PubMed: 30241549     


P-p70 S6 kinase, p-ERK and p-AKT levels were assayed in PTC cell lines. Cells were plated in triplicates using normal growth medium, after overnight incubation cells were washed and 0.125X EAA was added. Cells were treated with 10 μM JPH203 or DMSO as control and lysed after 24 h.

p-GCN2 / GCN2 / p-EIF2α / EIF2α / ATF4 ; 

PubMed: 30784173     


Activity of the two AA sensing pathways GCN2 and mTORC1 were analysed by immunoblot in the absence or presence of either 20 or 30 µmol/L of JPH203. ERK1/2 served as a loading control (the experiment presented here is representative of at least three independent experiments)

29200902 30241549 30784173
Growth inhibition assay
Cell viability; 

PubMed: 29200902     


Saos2 and FOB cells were treated with various concentrations of JPH203 (A, Saos2 cells; B, FOB cells) for 1-4 days. The cell viabilities were determined by MTT assays. The percentage cell viability was calculated as a ratio of the optical density at 570 nm of JPH203 treated cells and untreated control cells. The control cells were measured in the absence of JPH203 treatment. Each data point represents the mean±S.E.M. of four experiments. *p<0.05 vs. control, **p<0.01 vs. control and ***p<0.001 vs. control.

29200902
In vivo Daily intravenous administration of JPH203 (12.5 and 25 mg/kg) significantly inhibited tumor growth in KKU-213 cholangiocarcinoma cell xenografts in the nude mice model in a dose-dependent manner with no statistically significant change in the animal’s body weight and with no differences in the histology and appearance of the internal organs compared with the control group. Thus, JPH203 shows anti-tumor efficacy in nude mice bearing human cholangiocarcinom (CCA) cell xenografts without general toxicity[4].

Protocol

Cell Research:

[2]
+ Expand
  • Cell lines: Saos2 human osteosarcoma cells
  • Concentrations: 100 µM
  • Incubation Time: 72 h
  • Method:

    Colony formation assays are performed by seeding 300 cells/well into 6 well plates. After 24 h of growth, the cells are treated with 100 µM JPH203 for 72 h. The JPH203 treatment is removed and fresh medium is added. The cells are incubated for 10 days. Thereafter, medium is removed and the cells are washed with phosphate buffered saline (PBS) and fixed with 4% paraformaldehyde for 10 min at 4℃. Sequentially, the colonies are stained with 2% crystal violet for 10 min. Finally, colonies stained by crystal violet are washed with PBS and dried at room temperature, before imaged by a digital camera.


    (Only for Reference)
Animal Research:

[3]
+ Expand
  • Animal Models: Sprague-Dawley rats
  • Formulation: dissolved in DMSO and diluted in water
  • Dosages: 0.9-1.0 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 0.01 mg/mL (0.02 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 472.32
Formula

C23H19Cl2N3O4
CAS No. 1037592-40-7
Storage powder
in solvent
Synonyms KYT-0353

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID