L-DABA (L-2,4-Diaminobutyric acid) is a week GABA transaminase inhibitor with an IC 50 of larger than 500 μM; exhibits antitumor activity in vivo and in vitro.
性状
Solid
IC50 & Target[1][2]
Human Endogenous Metabolite
体外研究(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 is probably due to an osmotic lysis induced by the non-saturated intracellular accumulation of L-DABA. The harmful effect of L-DABA could be abolished by concomitant incubation with L-alanine and L-methionine. Kinetic studies indicates that L-DABA is a non-linear, non-competitive inhibitor of GABA transaminase activity. The L-DABA-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 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
体内研究(In Vivo)
Treatment with L-DABA results in 43.4% reduction of tumor growth. L-DABA is a more effective inhibitor of GABA transaminase in vivo than in vitro. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
结构分类
Ketones, Aldehydes, Acids
参考文献
[1]. Ronquist G, et al. Antitumor activity of L-2,4 diaminobuturic acid against mouse fibrosarcoma cells in vitro and in vivo. J Cancer Res Clin Oncol. 1980;96(3):259-68.[2]. Beart PM, et al. l-2,4-Diaminobutyric acid and the GABA system. Neurosci Lett. 1977 Jul;5(3-4):193-8.[3]. Panasci L, et al. The cytolytic ef
溶解度数据
In Vitro: H2O : 1 mg/mL (8.47 mM; Need ultrasonic)配制储备液
[1]. Ronquist G, et al. Antitumor activity of L-2,4 diaminobuturic acid against mouse fibrosarcoma cells in vitro and in vivo. J Cancer Res Clin Oncol. 1980;96(3):259-68.[2]. Beart PM, et al. l-2,4-Diaminobutyric acid and the GABA system. Neurosci Lett. 1977 Jul;5(3-4):193-8.[3]. Panasci L, et al. The cytolytic ef