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About This Item
Empirical Formula (Hill Notation):
C27H34N8O4 · 3C2HF3O2
CAS Number:
Molecular Weight:
876.68
UNSPSC Code:
12352200
MDL number:
Assay:
≥99% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
Quality Level
assay
≥99% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
white
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
−20°C
SMILES string
NC(N1CCN(CC2=CC(C(N3CCN(C(C4=CC=C(C(N)=N)C=C4)=O)CC3)=O)=CC(C(OC)=O)=C2)CC1)=N
General description
A cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 µM for hLSD1) and efficiently blocks LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ≤ 5 µM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC50 ≤ 5 µM), and causes activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC50 ≤ 3.74 µM). Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC50 >100 µM).
Note: the molecular weight is lot-specific and can be found on the vial label.
Note: the molecular weight is lot-specific and can be found on the vial label.
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Wang, J., et al. 2011. Cancer Res.71, 7238.
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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