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)
Quality Segment
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
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.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Primary Target
LSD1
LSD1
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.
Other Notes
Murray-Stewart, T., et al. 2013, Amino Acids44, in press.
Bi, X. et al. 2006, Bioorg. Med. Chem. Lett.16,3229.
Bi, X. et al. 2006, Bioorg. Med. Chem. Lett.16,3229.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
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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