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Chromatin/Epigenetic Epigenetic Reader Domain ARV-825

ARV-825

Catalog No. T5434   CAS 1818885-28-7

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.

ARV-825, CAS 1818885-28-7
Pack Size Availability Price/USD Quantity
1 mg In stock 70.00
2 mg In stock 87.00
5 mg In stock 163.00
10 mg In stock 244.00
25 mg In stock 458.00
50 mg In stock 688.00
1 mL * 10 mM (in DMSO) In stock 229.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Targets&IC50 BRD4,  
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.
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.
Molecular Weight 923.43
Formula C46H47ClN8O9S
CAS No. 1818885-28-7

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 50 mg/mL (54.15 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.

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