LSD1 Inhibitor

A bisguanidine polyamine analogue that exhibits noncompetitive and specific LSD1 inhibition, with 14.1% remaining LSD1 activity at 10 µM in vitro, and is shown to significantly increase methylation at the histone 3 lysine 4 chromatin mark (H3K4me1 and H3K4me2) dose-dependently from 0.25 µM to 10 µM, without affecting global H3K9me2 (which is not a LSD1 substrate) levels in HCT116 human colon carcinoma cells. This compound induces reexpression of several epigenetically silenced genes including SFRP1, SFRP4, SFRP5, and GATA5 more effectively when compared with siRNA treatment, particularly in the case of SFRP4 and SFRP5.

A bisguanidine polyamine analogue that exhibits noncompetitive and specific LSD1 inhibition, with 14.1% remaining LSD1 activity at 10 µM in vitro, and is shown to significantly increase methylation at the histone 3 lysine 4 chromatin mark (H3K4me1 and H3K4me2) dose-dependently from 0.25 µM to 10 µM, without affecting global H3K9me2 (which is not a LSD1 substrate) levels in HCT116 human colon carcinoma cells. This compound induces reexpression of several epigenetically silenced genes including SFRP1, SFRP4, SFRP5, and GATA5 more effectively when compared with siRNA treatment, particularly in the case of SFRP4 and SFRP5.

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sharma, SK., et al. 2010 J. Med. Chem.53, 5197.
Huang, Y., et al. 2007. Proc. Natl. Acad. Sci.104, 8023.
Bi, X., et al. 2006. Bioorg. Med. Chem. Lett.16, 3229.

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