| Name | ARV-825 |
| Description | ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested. |
| Cell Research | Cells (50000/100ul) were seeded in 96-well tissue culture plates followed by addition of ARV-825?at indicated concentration.?After 72 hours, 100 μL per well of reconstituted CellTiter-Glo reagent was added and read on Cytation 3 imaging reader.?Relative cell growth was determined by comparing assay readings of treated cells with control DMSO treated cells.?For apoptosis induction, Caspase-Glo 3/7 Assay was used following manufacturer s instruction. |
| In vitro | ARV-825 more effectively suppresses c-MYC levels and downstream signaling than small molecule BRD4 inhibitors resulting in more effective cell proliferation inhibition and apoptosis induction in BL.In Burkitt's lymphoma cells, ARV-825 reduces c-Myc levels, blocks cell proliferation, and induces apoptosis. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 127.5 mg/mL (138.07 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (2.17 mM), Sonication is recommended.
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| Keywords | PROTACs | Inhibitor | inhibit | EpigeneticReaderDomain | Epigenetic Reader Domain | BRD4 | ARV-825 | ARV825 | ARV 825 |
| Inhibitors Related | ABBV-744 | SNDX-5613 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | 5-Ph-IAA | Bavdegalutamide | Curcumin | Naphthol AS-E | Vepdegestrant | JQ-1 (carboxylic acid) | Bisdemethoxycurcumin |
| Related Compound Libraries | Reprogramming Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Ubiquitination Compound Library | Epigenetics Compound Library | Multi-Target Compound Library | NO PAINS Compound Library | PPI Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-COVID-19 Compound Library | Anti-Cancer Compound Library |