489476-M

LSD1 Inhibitor

The LSD1 Inhibitor, also referenced under CAS 927019-63-4, controls the biological activity of LSD1. This small molecule/inhibitor is primarily used for Cell Signaling applications.

• Synonym(s): LSD1 Inhibitor, LSD Inhibitor I, BHC110 Inhibitor I, Histone Lysine Demethylase Inhibitor III, KDM1 Inhibitor I
• Empirical Formula (Hill Notation): C₁₅H₄₀Cl₄N₈
• CAS Number: 927019-63-4
• Molecular Weight: 474.34
• UNSPSC Code: 12352200

Properties

• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: pale yellow to yellow
• solubility: water: 50 mg/mL
• storage temp.: −20°C

Description

General description

A bisguanidine polyamine analogue that exhibits noncompetitive and specific LSD1 inhibition, with 14.1% remaining LSD1 activity at 10 µM in vitro, and is shown to significantly increase methylation at the histone 3 lysine 4 chromatin mark (H3K4me1 and H3K4me2) dose-dependently from 0.25 µM to 10 µM, without affecting global H3K9me2 (which is not a LSD1 substrate) levels in HCT116 human colon carcinoma cells. This compound induces reexpression of several epigenetically silenced genes including SFRP1, SFRP4, SFRP5, and GATA5 more effectively when compared with siRNA treatment, particularly in the case of SFRP4 and SFRP5.

A bisguanidine polyamine analogue that exhibits noncompetitive and specific LSD1 inhibition, with 14.1% remaining LSD1 activity at 10 µM in vitro, and is shown to significantly increase methylation at the histone 3 lysine 4 chromatin mark (H3K4me1 and H3K4me2) dose-dependently from 0.25 µM to 10 µM, without affecting global H3K9me2 (which is not a LSD1 substrate) levels in HCT116 human colon carcinoma cells. This compound induces reexpression of several epigenetically silenced genes including SFRP1, SFRP4, SFRP5, and GATA5 more effectively when compared with siRNA treatment, particularly in the case of SFRP4 and SFRP5.

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Sharma, SK., et al. 2010 J. Med. Chem.53, 5197.
Huang, Y., et al. 2007. Proc. Natl. Acad. Sci.104, 8023.
Bi, X., et al. 2006. Bioorg. Med. Chem. Lett.16, 3229.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(C): Not applicable