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S 2101
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
S 2101图片
CAS NO:1239262-36-2
规格:98%
分子量:311.75
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
S2101是一个赖氨酸特异性去甲基化酶1(LSD1)抑制剂,其IC50值为0.99μM,Ki值为0.61μM,Kinact/Ki值为4560M/s。
CAS:1239262-36-2
分子式:C16H16ClF2NO
分子量:311.75
纯度:98%
存储:Store at -20°C

Background:

S 2101 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.


S 2101 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. S 2101 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 S 2101 results in a dose-dependent increase in the level of H3K4me2, which must have accumulated by the inactivation of LSD1. During the course of S 2101 treatment, the amounts of histone H3 and LSD1 in the nuclear extracts remain essentially unaffected. Because the treatment with 1 μM S 2101 generates a level of H3K4me2 similar to that elicited by 50 μM 2-PCPA, S 2101 is assumed to have approximately 50-fold stronger LSD1 inhibition activity than 2-PCPA in human cells[1].



[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.