ARN-5187

Research use only, not for human use.

A novel lysosomotropic REV-ERB ligand that has a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy.

A novel lysosomotropic REV-ERB ligand that has a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy; relieves REV-ERB-mediated transcriptional repression, significantly increases autophagy-associated protein p62 in treated cells; disrupts lysosomal function, blocks the autophagy process at the late stage, and reduces cancer cell viability; a novel dual autophagy/REV-ERB inhibitor more cytotoxic than chloroquine.

ARN5187 (compound 1) (0-100 μM; 48 h) shows cytotoxicity with EC50 of 23.5 μM in BT-474 cells and IC50 of 30.14 μM, >100 μM for BT-474 and HMEC cells, respectively.ARN5187 (0-100 μM) activates the RevRE reporter in a concentration-dependent manner in HEK-293 cells.ARN5187 (25, 50 μM) is a lysosomotropic-independent REV-ERB antagonistic activity.ARN5187 (50 μM; 24 h) shows autophagy inhibition.ARN5187 (50 μM; 2, 8, 24 h) effects autophagy formation and maturation. Cell Cytotoxicity Assay Cell Line:BT-474 cells Concentration:0-100 μM Incubation Time:48 h Result:Showed cytotoxicity with EC50 of 23.5 μM.RT-PCR Cell Line:BT-474 cells Concentration: 25, 50 μM Incubation Time:Result:Significantly enhanced the expression of BMAL1, PER1 and PEPCK in a dose-dependent manner.Western Blot Analysis Cell Line:BT-474 cells Concentration:50 μM Incubation Time:24 h Result:Significantly increased the expression of α-LC3-II, α-p62, α-Cleaved PARP.

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ARN5187 | ARN 5187

Autophagy

Autophagy

Autophagy

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1287451-26-6

397.538

C24H32FN3O

>98% (HPLC)

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4-[[[1-(2-Fluorophenyl)cyclopentyl]amino]methyl]-2-[(4-methyl-1-piperazinyl)methyl]phenol

(-20℃)

With Ice Pack

≥ 2 years