产品
编 号:F440848
分子式:C4H11BrN2O2
分子量:199.05
产品类型
结构图
CAS No: 73143-97-2
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产品详情
生物活性:
L-DABA (L-2,4-Diaminobutyric acid) hydrobromide is a week GABA transaminase inhibitor with an IC50 of larger than 500 μM; exhibits antitumor activity in vivo and in vitro.
体内研究:
Treatment with L-DABA hydrobromide results in 43.4% reduction of tumor growth. L-DABA hydrobromide is a more effective inhibitor of GABA transaminase in vivo than in vitro.
体外研究:
The tumor cells are irreversibly and totally damaged by incubation with 10 mM L-2,4-Diaminobutyric acid for 24 h at 37°C. The cell-destructive effect by L-DABA hydrobromide is probably due to an osmotic lysis induced by the non-saturated intracellular accumulation of L-DABA hydrobromide. The harmful effect of L-DABA hydrobromide could be abolished by concomitant incubation with L-alanine and L-methionine. Kinetic studies indicates that L-DABA hydrobromide is a non-linear, non-competitive inhibitor of GABA transaminase activity. The L-DABA hydrobromide-induced elevation of GABA levels parallels the inhibition of GABA transaminase activity. L-2,4-Diaminobutyric acid, an amino acid analogue, produceS a cytolytic effect with a human glioma cell line, SKMG-1, and normal human fibroblasts. The concentrations of L-DABA hydrobromide necessary to reduce the cell count to 50% of control following a 24-h incubation at 37°C are 12.5 mM for the human fibroblasts and 20 mM for the glioma cell line.