Chemical Structure : ARN14988
CAS No.:
1502027-70-4
ARN14988
(ARN-14988)
Catalog No.: PC-25425Not For Human Use, Lab Use Only.
ARN14988 is a potent, selective inhibitor of acid ceramidase (ACDase, ASAH1) with IC50 of 12.8 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
ARN14988 is a potent, selective inhibitor of acid ceramidase (ACDase, ASAH1) with IC50 of 12.8 nM.
ARN14988 (2-20 uM) induces elevations in the levels of ceramide (d18:1/16:0) and its precursor dihydroceramide (d18:0/16:0) in A375 cells.
ARN14988 has little or no effect on the intracellular levels of sphingomyelin (d18:1/16:0) and glucosylceramide (d18:1/16:0).
ARN14988 modestly affected melanoma cell viability with EC50 of 51.9 uM in A375 cells and 77.3 uM in G361 cells.
ARN14988 is a potent and effective inhibitor of intracellular AC activity, which displays chemosensitizing properties in proliferative, but not invasive, melanoma cells.
ARN14988 normalized ceramide levels and concomitantly sensitized proliferative melanoma cells to the cytotoxic actions of various anti-tumoral agents.
Physicochemical Properties
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M.Wt
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373.83
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Formula
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C16H24ClN3O5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1(2H)-Pyrimidinecarboxylic acid, 5-chloro-3-[(hexylamino)carbonyl]-3,6-dihydro-2,6-dioxo-, 2-methylpropyl ester
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References
1. Realini N, et al. J Biol Chem. 2016 Jan 29;291(5):2422-34.
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