S2101

• CAT Number: I011279
• CAS Number: 1239262-36-2
• Molecular Formula: C16H16ClF2NO
• Molecular Weight: 311.76
• Purity: ≥95%

S2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s[1].
S2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s. S2101 also displays much lower inhibition activity toward MAO-B (Ki=17 µM, Kinact/Ki=18 M/s) and MAO-A (Ki=110 µM, Kinact/Ki=60 M/s). The treatment of HEK293T cells with S2101 results in a dose-dependent increase in the level of H3K4me2, which must have accumulated by the inactivation of LSD1. During the course of S2101 treatment, the amounts of histone H3 and LSD1 in the nuclear extracts remain essentially unaffected. Because the treatment with 1 μM S2101 generates a level of H3K4me2 similar to that elicited by 50 μM 2-PCPA, S2101 is assumed to have approximately 50-fold stronger LSD1 inhibition activity than 2-PCPA in human cells[1].

Reference

[1]. Mimasu S, et al. Structurally designed trans-2-phenylcyclopropylamine derivatives potently inhibit histone demethylase LSD1/KDM1 . Biochemistry. 2010 Aug 3;49(30):6494-503.
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