LSD1 Inhibitor III, CBB1007

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).

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).

Packaged under inert gas

Toxicity: Standard Handling (A)

Supplied as a trifluoroacetate salt.

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

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

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