Table 1 Effects of 2-PCPA-based cell-permeable LSD1 inhibitors against FAD-dependent enzymes.

From: Novel pharmacologic inhibition of lysine-specific demethylase 1 as a potential therapeutic for glioblastoma

Compound

In vitro inhibition parameters Ki (µM)

LSD1

LSD2

MAO-A

MAO-B

2-PCPA*

100 ± 22 [23]

>250 [25]

5.0 ± 0.70 [23]

26 ± 0.082 [23]

S2101*

0.61 ± 0.13 [23]

>250 [25]

110 ± 11 [23]

17 ± 2.5 [23]

S2157*

0.37 ± 0.08 [25]

>250 [25]

>250 [25]

>250 [25]

S2172

0.27 ± 0.06

>250

>250

>250

  1. *, Values reported in Mimasu et al. [23] and Niwa et al. [25] are indicated by literature number. 2-PCPA trans-2-phenylcyclopropylamine (also known as tranylcypromine). Technical replicates, n = 3.
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