1. Epigenetics
  2. Histone Demethylase
  3. S2101

S2101 

Cat. No.: HY-110277
Handling Instructions

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.

For research use only. We do not sell to patients.

S2101 Chemical Structure

S2101 Chemical Structure

CAS No. : 1239262-36-2

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Description

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].

IC50 & Target

IC50: 0.99 μM (LSD1)[1]
Ki: 0.61 μM (LSD1)[1]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

311.75

Formula

C₁₆H₁₆ClF₂NO

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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S2101
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