tetramethyl Nordihydroguaiaretic Acid

tetramethyl Nordihydroguaiaretic acid is a derivative of the lipoxygenase inhibitor nordihydroguaiaretic acid (Item No. 70300).^1,2 It inhibits Tat-regulated HIV promoter transactivation in COS-1 cells in a reporter assay with an IC₅₀ value of 11 µM and inhibits the replication of acyclovir-sensitive and -resistant strains of herpes simplex virus (HSV-1) in Vero cells in a reporter assay with IC₅₀ values of 5.6 and 8.9 µM, respectively.^1,3 tetramethyl Nordihydroguaiaretic acid (50 µM) induces cell cycle arrest at the G₁/G₀ phase in A375 melanoma cells and inhibits tumor growth in an A375 mouse xenograft model when administered at a dose of 250 mg/kg.² tetramethyl Nordihydroguaiaretic acid (166 mg/kg) also reduces tumor growth in a B16 murine melanoma model.

WARNING This product is not for human or veterinary use.

1. 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. Med. Chem. 41, 2994-3000 (1998).

2. Lambert, J.D., Meyers, R.O., Timmermann, B.N., et al. Tetra-O-methylnordihydroguaiaretic acid inhibits melanoma in vivo. Cancer Lett. 171, 47-56 (2001).

3. 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. Med. Chem. 41, 3001-3007 (1998).