IF 16
PMID: 41087351 ↗JPH203 Dihydrochloride
Catalog No.: GC19400Purity:>98.00%Synonyms: KYT-0353
JPH203 Dihydrochloride is a tyrosine analog, acts as a selective inhibitor of L-type amino acid transporter 1 (LAT1), and is used in cancer research.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1597402-27-1
2mgIn Stock
$50.00
1
5mgIn Stock
$78.00
1
10mgIn Stock
$125.00
1
25mgIn Stock
$206.00
1
50mgIn Stock
$366.00
1
100mgIn Stock
$571.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 2mg | $50.00 | In Stock | 1 | |
| 5mg | $78.00 | In Stock | 1 | |
| 10mg | $125.00 | In Stock | 1 | |
| 25mg | $206.00 | In Stock | 1 | |
| 50mg | $366.00 | In Stock | 1 | |
| 100mg | $571.00 | In Stock | 1 |
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Citations
2 publicationsPublications from researchers using this productDescription
JPH203 Dihydrochloride is a tyrosine analog, acts as a selective inhibitor of L-type amino acid transporter 1 (LAT1), and is used in cancer research.
JPH203 Dihydrochloride is a selective inhibitor of LAT1. JPH203 (KYT-0353) inhibits 14C-leucine uptake in S2-hLAT1 and HT-29 cells, with IC50s of 0.14 uM and 0.06 uM. JPH203 (3-1000 uM) exhibits concentration-dependent inhibitory effects on S2-hLAT1 cell growth with an IC50 of 16.4 uM. JPH203 also displays inhibitory activities against HT-29 cell growth, with an IC50 value of 4.1 uM[1]. JPH203 (0.001-100 uM) inhibits the 14C-leucine (1.0 uM) uptake in a concentration dependent way by the YD-38 cells with an IC50 value of 0.79 ± 0.06 uM. JPH203 slightly shows such effects in normal human oral keratinocytes (NHOKs). JPH203 (0.01-30 mM, 1-4 d) completely inhibits the proliferation of YD-38 cells in a dose- and time-dependent manner. However, JPH203 slightly inhibits the proliferation of NHOKs. JPH203 (30 mM) induces apoptosis of YD-38 cells. JPH203 (3 mM) also increases the level of cleaved PARP in activation of the caspases cascade[2]. JPH203 (30 mM) induces mitochondria-dependent apoptosis in Saos2 human osteosarcoma cells. JPH203 (0.001-100 uM) inhibits 14C-leucine (1.0 uM) uptake slightly in FOB cells with an IC50 value of 92.12 ± 10.71 uM, but potently exihibts such effects in Saos2 cells with an IC50 value of 1.31 ± 0.27 uM. JPH203 (0.01 to 30 mM, 1-4 d) potently inhibits cell proliferation in Saos2 cells in a dose- and time-dependent manner, with an IC50 of 4.09-0.09 mM, but slightly inhibits that of FOB cells, with an IC50 of 24.1-2.8 mM[3].
JPH203 (6.3, 12.5, and 25.0 mg/kg, i.v. for 14 days) exhibits dose-dependent inhibition on HT-29 tumor growth in nude mice[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]. 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. Epub 2014 Feb 4.
[3]. Choi DW, et al. JPH203, a selective L-type amino acid transporter 1 inhibitor,Choi DW, et al. JPH203, a selective L-type amino acid transporter 1 inhibitor, induces mitochondria-dependent apoptosis in Saos2 human osteosarcoma cells. Korean J Physiol Pharmacol. 2017 Nov;21(6):599-607.
Protocol
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Cell experiment: |
Growth inhibition is evaluated by the MTT assay method. Namely, cell suspensions (1 × 104 cells/mL) in a volume of 135 μL are placed into the wells of a flat-bottom 96-well microtiter plate, and incubated in the atmosphere of 5% CO2 at 37°C (24 h). Drug solutions (15 μL) at various concentrations are added and incubated (96 h) under the same conditions. Next, MTT (15 μL; 5 mg/mL) dissolved in PBS is added and incubated (4.0 h). The incubation medium containing MTT is aspirated off. Cells are mixed (5 min) with DMSO (200 μL) and optical density read (540 nm) using a microtiter plate reader Emax; subsequently, IC50 values are determined[1]. |
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Animal experiment: |
Human-derived nude mouse HT-29 tumor growth inhibition is evaluated. HT-29 tumor blocks are injected subcutaneously to the right flank of male nude mice. After tumor volumes reach 100 to 300 mm3, the mice are divided into groups (n = 6). On the day of grouping (day 0), test compounds (JPH203) are administered intravenously daily for 14 days at three different doses (6.3, 12.5, and 25.0 mg/kg). Tumor volumes and body weights are measured two or three times a week for 42 days. Tumor volumes are expressed relative to initial tumor volume (day 0). Growth inhibition ratios for each treatment group is obtained from the mean tumor volume of the treated group compared to that of the control group[1]. |
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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. |
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Product Documents
Purity:>98.00%Appearance:A solid
Chemical Properties
CAS No.
1597402-27-1
Synonyms
KYT-0353
SMILES
N[C@@H](CC1=CC(Cl)=C(C(Cl)=C1)OCC2=C(OC(C3=CC=CC=C3)=N4)C4=CC(N)=C2)C(O)=O.[H]Cl.[H]Cl
Molecular Formula
C23H21Cl4N3O4
Molecular Weight
545.24
Solubility
DMSO : ≥ 105.5 mg/mL (193.49 mM; use within 2 hours); Do not use water to dissolve.
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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