ARN5187 - Calbiochem

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.

Cell permeable: yes

Primary Target
REV-ERBβ

Packaged under inert gas

De Mei, C., et al. 2015. Oncogene.34, 2597.

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

Toxicity: Standard Handling (A)