General description

A cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC₅₀ = 5.27 µM for hLSD1) and efficiently blocks LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC₅₀ ≤ 5 µM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC₅₀ ≤ 5 µM), and causes activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC50 ≤ 3.74 µM). Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC₅₀ >100 µM). r>Note: the molecular weight is lot-specific and can be found on the vial label.

A cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC₅₀ = 5.27 µM for hLSD1) and efficiently blocks LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC₅₀ ≤ 5 µM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC₅₀ ≤ 5 µM), and causes activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC₅₀ ≤ 3.74 µM). Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC₅₀ >100 µM).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Wang, J., et al. 2011. Cancer Res.71, 7238.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)