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L-DABA hydrobromide

CAS No. : 73143-97-2

MCE 站：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。

研究领域：Metabolic Enzyme/Protease  |  Neuronal Signaling  |  Membrane Transporter/Ion Channel

作用靶点：Endogenous Metabolite  |  GABA Receptor

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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