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.

IC50: larger than 500 μM (GABA transaminase)^[1]

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^[1]. 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^[2]. 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^[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Treatment with L-DABA hydrobromide results in 43.4% reduction of tumor growth^[1]. L-DABA hydrobromide is a more effective inhibitor of GABA transaminase in vivo than in vitro^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

199.05

C₄H₁₁BrN₂O₂

73143-97-2

固体

White to off-white

• Ketones, Aldehydes, Acids

• 内源性代谢物

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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.  [Content Brief]

  [2]. Beart PM, et al. l-2,4-Diaminobutyric acid and the GABA system. Neurosci Lett. 1977 Jul;5(3-4):193-8.  [Content Brief]

  [3]. Panasci L, et al. The cytolytic effect of L-2,4 diaminobutyric acid with malignant glioma cells and fibroblasts. Cancer Chemother Pharmacol. 1988;21(2):143-4.  [Content Brief]