|tetramethyl Nordihydroguaiaretic Acid
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||24150-24-1||SDF||Download SDF|
|Solubility||≤0.2mg/ml in ethanol;2mg/ml in DMSO;2mg/ml in dimethyl formamide||Storage||Store at -20°C|
|Physical Appearance||A crystalline solid||Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
Tetramethyl Nordihydroguaiaretic acid (TMNDGA) is a synthetic derivative of NDGA (Nordihydroguaiaretic acid), a non-selective lipoxygenase inhibitor. TMNDGA showed the strongest anti-HIV activity.
In vitro: In Vero cells, TMNDGA inhibited Sp1 transcription factor binding at the HIV long terminal repeat promoter and at the α-ICP4 promoter with IC50 values of 11 and 43.5 μM, respectively. The IC50 of TMNDGA varied between 11.7 and 4 μM in 10 passages of HSV-1 and 4 passages of HSV-2 . TMNDGA inhibited Sp1-dependent Cdc2 gene expression. In M4N-treated transformed C3 cells, TMNDGA induced growth arrest and apoptosis by suppressing Sp1-dependent Cdc2 and survivin gene expression giving rise to its antitumorigenic activity . TMNDGA treatment suppressed expression of the Sp1-dependent survivin gene. In transiently and stably survivin-transfected C3 cells, TMNDGA reduced caspase-3 activation by 50% and 75%, respectively . TMNDGA inhibited the growth of a number of tumor cell lines by inducing apoptosis in a non-schedule-dependent manner . TMNDGA inhibited the synthesis of DNA by melanoma cells and causes cell cycle arrest in G0/G1 and G2/M phases of the cell cycle .
In vivo: TMNDGA effectively inhibited the growth of human tumors in nude mice . TMNDGA inhibited the growth of both murine and human melanomas and human colon cancer without apparent hepatic or renal toxicity . In nude (nu/nu) mice bearing xenografts of human tumor types (Hep 3B, LNCaP, HT-29, MCF7, and K-562), treatment with TMNDGA (i.v. or i.p.) down-regulated Cdc2 and survivin genes expression .
 Hwu J R, Tseng W N, Gnabre J, et al. Antiviral activities of methylated nordihydroguaiaretic acids. 1. Synthesis, structure identification, and inhibition of tat-regulated HIV transactivation[J]. Journal of medicinal chemistry, 1998, 41(16): 2994-3000.
 Chen H, Teng L, Li J N, et al. Antiviral activities of methylated nordihydroguaiaretic acids. 2. Targeting herpes simplex virus replication by the mutation insensitive transcription inhibitor tetra-O-methyl-NDGA[J]. Journal of medicinal chemistry, 1998, 41(16): 3001-3007.
 Chang C C, Heller J D, Kuo J, et al. Tetra-O-methyl nordihydroguaiaretic acid induces growth arrest and cellular apoptosis by inhibiting Cdc2 and survivin expression[J]. Proceedings of the National Academy of Sciences of the United States of America, 2004, 101(36): 13239-13244.
 Lambert J D, Meyers R O, Timmermann B N, et al. Tetra-O-methylnordihydroguaiaretic acid inhibits melanoma in vivo[J]. Cancer letters, 2001, 171(1): 47-56.
 Park R, Chang C C, Liang Y C, et al. Systemic treatment with tetra-O-methyl nordihydroguaiaretic acid suppresses the growth of human xenograft tumors[J]. Clinical Cancer Research, 2005, 11(12): 4601-4609.