| Description | JPH203 dihydrochloride (KYT-0353 dihydrochloride) is a tyrosine analog, acts as a selective inhibitor of L-type amino acid transporter 1 (LAT1), and is used in cancer research. |
| In vitro | JPH203（30 mM）在Saos2人类骨肉瘤细胞中诱导线粒体依赖性凋亡。JPH203（0.001-100 μM）对FOB细胞的14C-亮氨酸（1.0 μM）吸收有轻微抑制作用，IC50值为92.12 ± 10.71 μM，但在Saos2细胞中显著表现此效应，IC50值为1.31 ± 0.27 μM。JPH203（0.01至30 mM, 1-4 d）显著抑制Saos2细胞增殖，呈剂量和时间依赖性，IC50值为4.09-0.09 mM，但对FOB细胞增殖仅轻微抑制，IC50值为24.1-2.8 mM。JPH203 Dihydrochloride是LAT1的选择性抑制剂。JPH203抑制S2-hLAT1和HT-29细胞的14C-亮氨酸摄取，IC50分别为0.14 μM和0.06 μM。JPH203（3-1000 μM）对S2-hLAT1细胞增长表现出浓度依赖性的抑制效应，IC50为16.4 μM。JPH203还抑制HT-29细胞增长，IC50值为4.1 μM。JPH203（0.001-100 μM）通过YD-38细胞对14C-亮氨酸（1.0 μM）的吸收抑制作用呈浓度依赖性，IC50值为0.79 ± 0.06 μM。JPH203在正常人类口腔角质形成细胞（NHOKs）中略显此效应。JPH203（0.01-30 mM, 1-4 d）完全抑制YD-38细胞增殖，具有剂量和时间依赖性。然而，JPH203对NHOKs增殖仅轻微抑制。JPH203（30 mM）诱导YD-38细胞凋亡。JPH203（3 mM）同时增加caspases级联激活中的cleaved PARP水平。 |
| In vivo | JPH203在裸鼠HT-29中以浓度依赖的方式抑制肿瘤生长。 |
| Synonyms | KYT-0353 dihydrochloride |
| molecular weight | 545.24 |
| Molecular formula | C23H21Cl4N3O4 |
| CAS | 1597402-27-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (91.7 mM), Sonication is recommended. H2O: 10 mg/mL (18.34 mM) |
| 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. |