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S2101

CAS No. : 1239262-36-2

MCE 站：S2101

产品活性：S2101 是一个赖氨酸特异性去甲基化酶 1 (LSD1) 抑制剂，其 IC₅₀ 值为 0.99 μM， K_i 值为 0.61 μM，K_inact/K_i 值为 4560 M/s。

研究领域：Epigenetics

作用靶点：Histone Demethylase

In Vitro: S2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 0.99 μM, K_i of 0.61 μM and K_inact/K_i of 4560 M/s. S2101 also displays much lower inhibition activity toward MAO-B (K_i=17 ?M, K_inact/K_i=18 M/s) and MAO-A (K_i=110 ?M, K_inact/K_i=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.

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