耗材描述
L-DABA hydrobromide
产品活性:L-DABA (L-2,4-Diaminobutyric acid) hydrobromide 是 GABA 转氨酶的弱抑制剂,IC50 值大于500 μM。在体内和体外具有抗肿瘤活性。
产品来源: https://www.medchemexpress.cn/l-daba-hydrobromide.html
研究领域:Metabolic Enzyme/Protease | Neuronal Signaling | Membrane Transporter/Ion Channel
作用靶点:Endogenous Metabolite | GABA Receptor
结构分类:酮、醛、酸 | 结构分类
In Vitro: 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.
In Vivo: 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.
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