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ARN5187 is a lysosomal compound, REV-ERB β Ligand. ARN5187 inhibits REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomal efficacy and cytotoxicity, and can induce apoptosis.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 6-8 weeks | 6-8 weeks | |
| 50 mg | $1,980 | 6-8 weeks | 6-8 weeks | |
| 100 mg | $2,500 | 6-8 weeks | 6-8 weeks |
| Description | ARN5187 is a lysosomal compound, REV-ERB β Ligand. ARN5187 inhibits REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomal efficacy and cytotoxicity, and can induce apoptosis. |
| In vitro | ARN5187 (compound 1) (0-100 μM; 48 h) demonstrates cytotoxicity with an EC50 of 23.5 μM in BT-474 cells and IC50 values of 30.14 μM and >100 μM in BT-474 and HMEC cells, respectively [1][2]. In HEK-293 cells, ARN5187 (0-100 μM) activates the RevRE reporter in a concentration-dependent manner [1]. ARN5187 (25, 50 μM) exhibits lysosomotropic-independent REV-ERB antagonistic activity [1], and at 50 μM (24 h), it shows autophagy inhibition and affects autophagy formation and maturation [1]. In BT-474 cells, ARN5187 significantly enhances the expression of BMAL1, PER1, and PEPCK in a dose-dependent manner (25, 50 μM), and at 50 μM (24 h), significantly increases the expression of α-LC3-II, α-p62, and α-Cleaved PARP [1]. |
| Molecular Weight | 397.53 |
| Formula | C24H32FN3O |
| Cas No. | 1287451-26-6 |
| Smiles | N(CC1=CC(CN2CCN(C)CC2)=C(O)C=C1)C3(CCCC3)C4=C(F)C=CC=C4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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