Drug intelligence / Profile preview

S2101

Development stage
Unknown
Lead developer
Nagoya City University
Modality
Small Molecules
01

Overview

S2101 (also known as LSD1 Inhibitor II) is a selective, cell-permeable, small-molecule irreversible inhibitor of lysine-specific demethylase 1A (KDM1A/LSD1). Developed by researchers at RIKEN and Nagoya City University, S2101 is a derivative of trans-2-phenylcyclopropylamine (2-PCPA) designed to exhibit enhanced potency and selectivity for LSD1 over monoamine oxidases A and B (MAO-A and MAO-B). It exerts its inhibitory effect by forming a covalent adduct with the flavin adenine dinucleotide (FAD) cofactor of LSD1. S2101 is widely utilized as a chemical biology research tool to investigate the role of epigenetic regulation in cancer stem cell maintenance, cellular differentiation, and viral reactivation, particularly in models of leukemia, glioblastoma, and ovarian cancer.

Other names
BHC110 Inhibitor IIBHC-110 Inhibitor IIBHC 110 Inhibitor IIHistone Lysine Demethylase Inhibitor IVKDM1 Inhibitor IIKDM-1 Inhibitor IIKDM 1 Inhibitor IILSD1 Inhibitor IILSD-1 Inhibitor IILSD 1 Inhibitor IIMOA Inhibitor IIS 2101S2101S-2101rac-(1R,2S)-2-(2-(benzyloxy)-3,5-difluorophenyl)cyclopropan-1-amine hydrochloride
02

Targets

KDM1A (LSD1)MAOB (Monoamine oxidase B)MAOA (Monoamine oxidase A)

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