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.

Product information

CAS Number: 1239262-36-2

Molecular Weight: 311.75

Formula: C16H16ClF2NO

Chemical Name: (1R,2S)-2-[2-(benzyloxy)-3,5-difluorophenyl]cyclopropan-1-amine hydrochloride

Smiles: Cl.N[C@@H]1C[C@H]1C1C=C(F)C=C(F)C=1OCC1C=CC=CC=1

InChiKey: CTSUZAFTJVLOIX-SBKWZQTDSA-N

InChi: InChI=1S/C16H15F2NO.ClH/c17-11-6-13(12-8-15(12)19)16(14(18)7-11)20-9-10-4-2-1-3-5-10;/h1-7,12,15H,8-9,19H2;1H/t12-,15+;/m0./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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