LAT1-IN-1 是 L 型氨基酸转运蛋白 1 的选择性竞争性抑制剂,显着抑制细胞对氨基酸的摄取和 mTOR 磷酸化,从而诱导抑制癌症生长和细胞凋亡。
产品描述
LAT1-IN-1 (BCH) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis. is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1).
体外活性
LAT1-IN-1 (30 mM; 0-24 hours; KYSE30 and KYSE150 cells) treatment decreases phosphorylation of 4E-BP1 and p70S6K at 30 minutes and the decrease is continued for 24 hours. The amount of mTOR, 4E-BP1, and p70S6K proteins is slightly decreased.LAT1-IN-1 (1-100 mM;?3 days;?KYSE30 and KYSE150 esophageal cancer cells) treatment suppresses cell proliferation in a dose-dependent manner.?LAT1-IN-1 (30 mM;?24 and 48 hours;?KYSE30 and KYSE150 cells) treatment significantly increases cell population in the G0/G1 phase in both KYSE30 and KYSE150 cells, indicating that LAT1-IN-1 induces cell cycle arrest at G1 phase.
体内活性
LAT1-IN-1 (200 mg/kg;?intravenous injection;?daily;?for 14 days;?male BALB/c nude mice) treatment significantly delays tumor growth and decreases glucose metabolism, indicating that LAT1 inhibition potentially suppresses esophageal cancer growth in vivo.
Cas No.
20448-79-7
分子式
C8H13NO2
分子量
155.19
别名
2-氨基-2-去甲菠烷羧酸;BCH;LAT1-IN-1
储存和溶解度
H2O:12.5 mg/mL (80.55 mM),Need ultrasonic
DMSO:< 1 mg/mL,insoluble or slightly soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years