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Merck

5.05770

LSD1 Inhibitor VI, Cpd 2d

Synonym(s):

LSD1 Inhibitor VI, Cpd 2d, 1,15-bis{N5-[3,3-(diphenyl)propyl]-N1-biguanido}-4,12-diazapentadecane

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About This Item

Empirical Formula (Hill Notation):
C47H68N12
Molecular Weight:
801.12
UNSPSC Code:
12352200

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

off-white

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

Quality Level

Biochem/physiol Actions

Primary Target
LSD1

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable polyamine derivative that acts as an inhibitor of lysine-specific demethylase-1 (LSD1, KDM1) and increases levels of mono- and di-methylated histone H3K4, H3K9 proteins in acute myeloid leukemia (AML) cancer cells in a dose-dependent manner. Shown to cause significant growth inhibition in different AML cell lines (HL-60, KG1a, HNT-34, and ML-1 cells) at low micromolar concentrations (5 to 10 µM) over a period of 96 hours. Induces re-expression of cancer suppressing E-caherin gene and CDH-1 mRNA in tumor cells (˜10 µM). Also, displays anti-trypanosomal properties and inhibits trypanothione reductase activity (IC50 = 950 nM) in Trypanosoma brucei brucei.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Other Notes

Murray-Stewart, T., et al. 2013, Amino Acids44, in press.

Bi, X. et al. 2006, Bioorg. Med. Chem. Lett.16,3229.

Packaging

Packaged under inert gas

Preparation Note

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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