GSK-LSD1

GSK-LSD1 : Inhibitor of KDM1A

Structure

SERP Rating

Probe GSK-LSD1 is in the process of SERP review.

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Information

KDM1A

Inhibitor

100 nM

Additional Data

SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: O60341

Target Class: Epigenetic

Target SubClass: --

Potency Value: Kiapp 160 nM

Potency Assay: Kinetic characterization of the inhibition of LSD1 by GSK-LSD1 is consistent with a reversible binding step followed by time-dependent irreversible inactivation. (kinact = 0.13 ± 0.01 min−1, kinact/ KIapp = 0.81 ± 5.95 × 10−2 min−1 μM−1)

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Lysine-specific histone demethylase 1A, LSD1, KIAA ...

DOI Reference: 10.1016/j.ccell.2015.06.002

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B).

Probe Selectivity in Vitro:

LSD-1 at 10 µM showed no activity against 55 human recombinant receptors in the CEREP ExpresSProfile selectivity/specificity profile (GPCR, transporters, ion channels), except 5-HT1A (49% inhibition) 5-HT transporter (74% inhibition) and dopamine transporter (39 % inhibition). Selective against all families tested (D-amino acid oxidase and glutathione reductase, non-FAD dependent oxidase (LOXL2), GPCRs, ion channels, nuclear receptors, kinases, and transporters)

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