All Photos(2)
Synonym(s):
ARN5187 - Calbiochem, 4-(((1-(2-Fluorophenyl)cyclopentyl)-amino)methyl)-2-((4-methylpiperazin-1-yl)methyl)phenol, 3HCl
Empirical Formula (Hill Notation):
C24H32FN3O · 3HCl
Molecular Weight:
506.91
UNSPSC Code:
12352200
Recommended Products
Assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
color
off-white
solubility
water: 50 mg/mL
storage temp.
−20°C
General description
A cell-permeable piperazinylmethylphenol compound that exhibits dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. Shown to directly interact with the LBD of REV-ERBβ, activate the RevRE reporter (EC50 = 15.0 µM for REV-ERβ) and dose-dependently enhance BMAL1, PER1 and PEPCK expression. Disrupts lysosomal function, blocks autophagy at a late stage, and reduces cancer cell viability (EC50 = 23.5, 14.4 & 29.8 µM in BT-474, HEP-G2 & LNCaP cells, respectively). Elicits stronger apoptotic induction and significantly more cytotoxic than chloroquine.
A cell-permeable piperazinylmethylphenol compound that exhibits dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. Shown to directly interact with the LBD of REV-ERBβ, activate the RevRE reporter (EC50 = 15.0 µM for REV-ERβ) and dose-dependently enhance BMAL1, PER1 and PEPCK expression. Disrupts lysosomal function, blocks autophagy at a late stage, and reduces cancer cell viability (EC50 = 23.5, 14.4 & 29.8 µM in BT-474, HEP-G2 & LNCaP cells, respectively). Elicits stronger apoptotic induction and significantly more cytotoxic than chloroquine.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
REV-ERBβ
REV-ERBβ
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Other Notes
De Mei, C., et al. 2015. Oncogene.34, 2597.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
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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