| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
JPH203 (KYT-0353), a selective L-type amino acid transporter 1 inhibitor, significantly inhibited leucine uptake and cell growth in HT-29 YD-38 and leukemia cells, with IC50 values of 0.06 μM and 4.1 μM, respectively.
Cell lines | Saos2 cells |
Preparation Method | Colony formation assays were performed by seeding 300 cells/well into 6-well plates for 24 h after growth, cells were treated with 100 M JPH203 (KYT-0353) for 72 h to remove the JPH203 (KYT-0353) treatment and cultured for 10 days with fresh medium. |
Reaction Conditions | Treatment with 100 μM JPH203 (KYT-0353) for 72 hours |
Applications | JPH203 (KYT-0353) inhibited colony formation in Saos2 cells. |
Animal models | Six-week-old male athymic BALB/c nude mice |
Preparation Method | Mice in treatment group were injected with JPH203 (KYT-0353) intravenously every day for 20 days. |
Dosage form | 6.3 mg/kg; 12.5 mg/kg; 25 mg/kg JPH203 (KYT-0353) for 20 days |
Applications | JPH203 (KYT-0353) (KYT-0353) was administered intravenously daily for 20 days at three different doses starting at day 3 after the injection of cancer cells. On the days 18 and 21, JPH203 (KYT-0353) showed dose-dependent inhibition on tumor growth with significantly inhibited tumor growth in the groups of JPH203 (KYT-0353) at 12.5 mg/kg and 25 mg/kg . |
| 产品描述 | JPH203 (KYT-0353), a selective L-type amino acid transporter 1 inhibitor, significantly inhibited leucine uptake and cell growth in HT-29 YD-38 and leukemia cells, with IC50 values of 0.06 μM and 4.1 μM, respectively[1,5]. JPH203 (KYT-0353) can up-regulate the activated forms of pro-apoptotic factors such as Bad, Bax, Bak and caspase-9 and down-regulate anti-apoptotic factors such as Bcl-2,Bcl-xl, activation of mitochondria dependent apoptotic signaling pathway JPH203 (KYT-0353), can distinguish the relative abundance of LAT1 and LAT2, and it has high selectivity for LAT1[2]. JPH203 (KYT-0353) is metabolically stable in liver microsomes of mice, rats, dogs, monkeys and humans[3]. JPH203 (KYT-0353) induced 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]. Study on leukemia reported that JPH203 (KYT-0353) induced type ?? cell death, autophagy, followed by caspase-3-dependent apoptosis at 48 h after treatment[6].LAT1 inhibition by JPH203 (KYT-0353) sensitizes cancer cells to radiation by enhancing cellular senescence via mTOR downregulation[7]. In vivo model, using intravenously administered JPH203 (KYT-0353) (12.5 and 25.0 mg/kg), a statistically significant inhibition of growth of HT-29 tumors transplanted to nude mice with only a slight decrease in body weight[4]. References: |
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